Cayman

Showing 39001–39150 of 45550 results

  • SBE 13 is a potent inhibitor of polo-like kinase 1 (Plk1) (IC50 = 0.2 nM) that targets the inactive conformation of the enzyme {33293,33294}. It exhibits no activity against aurora A kinase and less effectively inhibits Plk2 (IC50 > 66 µM) and Plk3 (IC50 = 875 nM). SBE 13 induces cell cycle arrest, reduces cell proliferation (EC50 = 5-60 µM), and induces apoptosis in a broad range of human cancer cell lines.{33294,33295}  

     

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    Cayman
    SKU:21241 -

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  • SBE 13 is a potent inhibitor of polo-like kinase 1 (Plk1) (IC50 = 0.2 nM) that targets the inactive conformation of the enzyme {33293,33294}. It exhibits no activity against aurora A kinase and less effectively inhibits Plk2 (IC50 > 66 µM) and Plk3 (IC50 = 875 nM). SBE 13 induces cell cycle arrest, reduces cell proliferation (EC50 = 5-60 µM), and induces apoptosis in a broad range of human cancer cell lines.{33294,33295}  

     

    Brand:
    Cayman
    SKU:21241 -

    Out of stock

  • SBE 13 is a potent inhibitor of polo-like kinase 1 (Plk1) (IC50 = 0.2 nM) that targets the inactive conformation of the enzyme {33293,33294}. It exhibits no activity against aurora A kinase and less effectively inhibits Plk2 (IC50 > 66 µM) and Plk3 (IC50 = 875 nM). SBE 13 induces cell cycle arrest, reduces cell proliferation (EC50 = 5-60 µM), and induces apoptosis in a broad range of human cancer cell lines.{33294,33295}  

     

    Brand:
    Cayman
    SKU:21241 -

    Out of stock

  • SBFI AM is a membrane-permeant, fluorescent Na+ indicator dye. It is selective for Na+ over K+ with Kd values of 20 and 120 mM for these ions, respectively.{30208} Increasing concentration of Na+ increases the ratio of excitation efficiency at 330-345 nm to that at 370-390 nm with emission collected at 450-550 nm.{30208} Therefore, ratio fluorometry and imaging can be performed with the same wavelengths. SBF AM is suitable for single intracellular dye injection and is typically used for high-resolution measurements of Na+ concentration in intact tissue through two-photon confocal imaging.{30207}  

     

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  • ULK1 is a serine/threonine kinase that acts upstream of phosphatidylinositol 3-kinase (PI3K) to regulate the formation of autophagophores, the precursors of autophagosomes, in response to nutrient deprivation. It is activated by phosphorylation by AMPK and, in turn, phosphorylates and inhibits AMPK. SBI-0206965 is an inhibitor of ULK1 (IC50 = 108 nM) that is less effective against ULK2 (IC50 = 711 nM).{29597} It is selective for ULK1 and ULK2 over a panel of 456 additional kinases, showing activity against a few kinases in vitro but not in cells.{29597} SBI-0206965 suppresses autophagy induced by mTOR inhibition via AZD 8055 (Item No. 16978). It also blocks ULK1-dependent cell survival following nutrient deprivation.{29597}  

     

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  • ULK1 is a serine/threonine kinase that acts upstream of phosphatidylinositol 3-kinase (PI3K) to regulate the formation of autophagophores, the precursors of autophagosomes, in response to nutrient deprivation. It is activated by phosphorylation by AMPK and, in turn, phosphorylates and inhibits AMPK. SBI-0206965 is an inhibitor of ULK1 (IC50 = 108 nM) that is less effective against ULK2 (IC50 = 711 nM).{29597} It is selective for ULK1 and ULK2 over a panel of 456 additional kinases, showing activity against a few kinases in vitro but not in cells.{29597} SBI-0206965 suppresses autophagy induced by mTOR inhibition via AZD 8055 (Item No. 16978). It also blocks ULK1-dependent cell survival following nutrient deprivation.{29597}  

     

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    Cayman
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  • ULK1 is a serine/threonine kinase that acts upstream of phosphatidylinositol 3-kinase (PI3K) to regulate the formation of autophagophores, the precursors of autophagosomes, in response to nutrient deprivation. It is activated by phosphorylation by AMPK and, in turn, phosphorylates and inhibits AMPK. SBI-0206965 is an inhibitor of ULK1 (IC50 = 108 nM) that is less effective against ULK2 (IC50 = 711 nM).{29597} It is selective for ULK1 and ULK2 over a panel of 456 additional kinases, showing activity against a few kinases in vitro but not in cells.{29597} SBI-0206965 suppresses autophagy induced by mTOR inhibition via AZD 8055 (Item No. 16978). It also blocks ULK1-dependent cell survival following nutrient deprivation.{29597}  

     

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    Cayman
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  • ULK1 is a serine/threonine kinase that acts upstream of phosphatidylinositol 3-kinase (PI3K) to regulate the formation of autophagophores, the precursors of autophagosomes, in response to nutrient deprivation. It is activated by phosphorylation by AMPK and, in turn, phosphorylates and inhibits AMPK. SBI-0206965 is an inhibitor of ULK1 (IC50 = 108 nM) that is less effective against ULK2 (IC50 = 711 nM).{29597} It is selective for ULK1 and ULK2 over a panel of 456 additional kinases, showing activity against a few kinases in vitro but not in cells.{29597} SBI-0206965 suppresses autophagy induced by mTOR inhibition via AZD 8055 (Item No. 16978). It also blocks ULK1-dependent cell survival following nutrient deprivation.{29597}  

     

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    Cayman
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  • The enzyme Δ6 desaturase mediates the conversion of linoleic acid to γ-linolenic acid (GLA), which can then be elongated to dihomo-γ-linolenic acid (DGLA). DGLA can then be used as a substrate for Δ5 desaturase to produce arachidonic acid (AA), the fatty acid that is used to generate eicosanoids. SC 26196 is an inhibitor of Δ6 desaturase (IC50 = 0.2 µM in a rat liver microsomal assay) that completely blocks the conversion of linoleic acid to arachidonic acid (AA).{29588} It is selective for Δ6 desaturase, as IC50 values for Δ5 and Δ9 desaturases exceed 200 µM and it has no effect on the conversion of dihomo-γ-linolenic acid to AA.{29588,29586} SC 26196 is orally active in vivo, decreasing edema in the carrageenan paw edema model in mice.{29588} It also blocks aging-related increases in AA in myocardial cardiolipin in mice, attenuating contractile dysfunction without impacting mitochondrial oxidative stress.{29587}  

     

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    Cayman
    SKU:10792 - 1 mg

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  • The enzyme Δ6 desaturase mediates the conversion of linoleic acid to γ-linolenic acid (GLA), which can then be elongated to dihomo-γ-linolenic acid (DGLA). DGLA can then be used as a substrate for Δ5 desaturase to produce arachidonic acid (AA), the fatty acid that is used to generate eicosanoids. SC 26196 is an inhibitor of Δ6 desaturase (IC50 = 0.2 µM in a rat liver microsomal assay) that completely blocks the conversion of linoleic acid to arachidonic acid (AA).{29588} It is selective for Δ6 desaturase, as IC50 values for Δ5 and Δ9 desaturases exceed 200 µM and it has no effect on the conversion of dihomo-γ-linolenic acid to AA.{29588,29586} SC 26196 is orally active in vivo, decreasing edema in the carrageenan paw edema model in mice.{29588} It also blocks aging-related increases in AA in myocardial cardiolipin in mice, attenuating contractile dysfunction without impacting mitochondrial oxidative stress.{29587}  

     

    Brand:
    Cayman
    SKU:10792 - 10 mg

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  • The enzyme Δ6 desaturase mediates the conversion of linoleic acid to γ-linolenic acid (GLA), which can then be elongated to dihomo-γ-linolenic acid (DGLA). DGLA can then be used as a substrate for Δ5 desaturase to produce arachidonic acid (AA), the fatty acid that is used to generate eicosanoids. SC 26196 is an inhibitor of Δ6 desaturase (IC50 = 0.2 µM in a rat liver microsomal assay) that completely blocks the conversion of linoleic acid to arachidonic acid (AA).{29588} It is selective for Δ6 desaturase, as IC50 values for Δ5 and Δ9 desaturases exceed 200 µM and it has no effect on the conversion of dihomo-γ-linolenic acid to AA.{29588,29586} SC 26196 is orally active in vivo, decreasing edema in the carrageenan paw edema model in mice.{29588} It also blocks aging-related increases in AA in myocardial cardiolipin in mice, attenuating contractile dysfunction without impacting mitochondrial oxidative stress.{29587}  

     

    Brand:
    Cayman
    SKU:10792 - 25 mg

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  • The enzyme Δ6 desaturase mediates the conversion of linoleic acid to γ-linolenic acid (GLA), which can then be elongated to dihomo-γ-linolenic acid (DGLA). DGLA can then be used as a substrate for Δ5 desaturase to produce arachidonic acid (AA), the fatty acid that is used to generate eicosanoids. SC 26196 is an inhibitor of Δ6 desaturase (IC50 = 0.2 µM in a rat liver microsomal assay) that completely blocks the conversion of linoleic acid to arachidonic acid (AA).{29588} It is selective for Δ6 desaturase, as IC50 values for Δ5 and Δ9 desaturases exceed 200 µM and it has no effect on the conversion of dihomo-γ-linolenic acid to AA.{29588,29586} SC 26196 is orally active in vivo, decreasing edema in the carrageenan paw edema model in mice.{29588} It also blocks aging-related increases in AA in myocardial cardiolipin in mice, attenuating contractile dysfunction without impacting mitochondrial oxidative stress.{29587}  

     

    Brand:
    Cayman
    SKU:10792 - 5 mg

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  • The maintenance of embryonic stem cells in culture typically requires feeder cells and various exogenous factors found in serum. Murine embryonic stem (mES) cells can be maintained in the absence of feeder cells and serum but require the leukemia inhibitor factor (LIF) and bone morphogenic protein (BMP) to prevent differentiation and promote self-renewal. SC-1 is a small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state.{14533} The activity of SC-1 is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM, respectively.{14533} Inhibition of RasGAP increases Ras signaling via the PI3-kinase pathway which promotes self-renewal, whereas inhibition of ERK blocks differentiation.  

     

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    Cayman
    SKU:10009557 - 1 mg

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  • The maintenance of embryonic stem cells in culture typically requires feeder cells and various exogenous factors found in serum. Murine embryonic stem (mES) cells can be maintained in the absence of feeder cells and serum but require the leukemia inhibitor factor (LIF) and bone morphogenic protein (BMP) to prevent differentiation and promote self-renewal. SC-1 is a small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state.{14533} The activity of SC-1 is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM, respectively.{14533} Inhibition of RasGAP increases Ras signaling via the PI3-kinase pathway which promotes self-renewal, whereas inhibition of ERK blocks differentiation.  

     

    Brand:
    Cayman
    SKU:10009557 - 10 mg

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  • The maintenance of embryonic stem cells in culture typically requires feeder cells and various exogenous factors found in serum. Murine embryonic stem (mES) cells can be maintained in the absence of feeder cells and serum but require the leukemia inhibitor factor (LIF) and bone morphogenic protein (BMP) to prevent differentiation and promote self-renewal. SC-1 is a small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state.{14533} The activity of SC-1 is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM, respectively.{14533} Inhibition of RasGAP increases Ras signaling via the PI3-kinase pathway which promotes self-renewal, whereas inhibition of ERK blocks differentiation.  

     

    Brand:
    Cayman
    SKU:10009557 - 25 mg

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  • The maintenance of embryonic stem cells in culture typically requires feeder cells and various exogenous factors found in serum. Murine embryonic stem (mES) cells can be maintained in the absence of feeder cells and serum but require the leukemia inhibitor factor (LIF) and bone morphogenic protein (BMP) to prevent differentiation and promote self-renewal. SC-1 is a small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state.{14533} The activity of SC-1 is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM, respectively.{14533} Inhibition of RasGAP increases Ras signaling via the PI3-kinase pathway which promotes self-renewal, whereas inhibition of ERK blocks differentiation.  

     

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    Cayman
    SKU:10009557 - 5 mg

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  • The prostaglandin E2 (PGE2) receptor EP1 is involved in triggering PGE2-mediated pain, neuronal survival and growth as well as the suppression of tumor metastasis. SC-19220 is a dibenzoxazepine that acts as a selective antagonist of PGE2 at the EP1 receptor.{6742,2681} At doses between 0.3-300 µM, SC-19220 acts as a competitive antagonist of PGE2-induced smooth muscle contractions of guinea pig ileum and stomach.{6911,6856} SC-19220 also acts as a PGE2 antagonist in the EP1 receptor-mediated contraction of guinea pig trachea.{6294} SC-19220 displaces radiolabeled PGE2 from the cloned human EP1 receptor with an IC50 of 6.7 µM and exhibits no binding at the human EP2 receptor.{3176,3186} It binds with apparent low affinity to the cloned mouse EP1 receptor expressed in CHO cells.{6640} In a model of bone resorption, 3-150 μM SC-19220 inhibited both 1,25 dihydroxy vitamin D3- and PGE2-stimulated osteoclastogenesis in mouse osteoclast precursors.{23818} Antagonism of EP1 with 1 μM SC-19220 has been shown to promote metastasis in a mouse model of metastatic breast cancer.{18890} In a rodent model of Parkinson’s disease, 1.5 μM SC-19220 prevented PGE2-mediated loss of dopaminergic neurons from rat substantia nigra.{15975}  

     

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  • The prostaglandin E2 (PGE2) receptor EP1 is involved in triggering PGE2-mediated pain, neuronal survival and growth as well as the suppression of tumor metastasis. SC-19220 is a dibenzoxazepine that acts as a selective antagonist of PGE2 at the EP1 receptor.{6742,2681} At doses between 0.3-300 µM, SC-19220 acts as a competitive antagonist of PGE2-induced smooth muscle contractions of guinea pig ileum and stomach.{6911,6856} SC-19220 also acts as a PGE2 antagonist in the EP1 receptor-mediated contraction of guinea pig trachea.{6294} SC-19220 displaces radiolabeled PGE2 from the cloned human EP1 receptor with an IC50 of 6.7 µM and exhibits no binding at the human EP2 receptor.{3176,3186} It binds with apparent low affinity to the cloned mouse EP1 receptor expressed in CHO cells.{6640} In a model of bone resorption, 3-150 μM SC-19220 inhibited both 1,25 dihydroxy vitamin D3- and PGE2-stimulated osteoclastogenesis in mouse osteoclast precursors.{23818} Antagonism of EP1 with 1 μM SC-19220 has been shown to promote metastasis in a mouse model of metastatic breast cancer.{18890} In a rodent model of Parkinson’s disease, 1.5 μM SC-19220 prevented PGE2-mediated loss of dopaminergic neurons from rat substantia nigra.{15975}  

     

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    Cayman
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  • The prostaglandin E2 (PGE2) receptor EP1 is involved in triggering PGE2-mediated pain, neuronal survival and growth as well as the suppression of tumor metastasis. SC-19220 is a dibenzoxazepine that acts as a selective antagonist of PGE2 at the EP1 receptor.{6742,2681} At doses between 0.3-300 µM, SC-19220 acts as a competitive antagonist of PGE2-induced smooth muscle contractions of guinea pig ileum and stomach.{6911,6856} SC-19220 also acts as a PGE2 antagonist in the EP1 receptor-mediated contraction of guinea pig trachea.{6294} SC-19220 displaces radiolabeled PGE2 from the cloned human EP1 receptor with an IC50 of 6.7 µM and exhibits no binding at the human EP2 receptor.{3176,3186} It binds with apparent low affinity to the cloned mouse EP1 receptor expressed in CHO cells.{6640} In a model of bone resorption, 3-150 μM SC-19220 inhibited both 1,25 dihydroxy vitamin D3- and PGE2-stimulated osteoclastogenesis in mouse osteoclast precursors.{23818} Antagonism of EP1 with 1 μM SC-19220 has been shown to promote metastasis in a mouse model of metastatic breast cancer.{18890} In a rodent model of Parkinson’s disease, 1.5 μM SC-19220 prevented PGE2-mediated loss of dopaminergic neurons from rat substantia nigra.{15975}  

     

    Brand:
    Cayman
    SKU:-
  • The prostaglandin E2 (PGE2) receptor EP1 is involved in triggering PGE2-mediated pain, neuronal survival and growth as well as the suppression of tumor metastasis. SC-19220 is a dibenzoxazepine that acts as a selective antagonist of PGE2 at the EP1 receptor.{6742,2681} At doses between 0.3-300 µM, SC-19220 acts as a competitive antagonist of PGE2-induced smooth muscle contractions of guinea pig ileum and stomach.{6911,6856} SC-19220 also acts as a PGE2 antagonist in the EP1 receptor-mediated contraction of guinea pig trachea.{6294} SC-19220 displaces radiolabeled PGE2 from the cloned human EP1 receptor with an IC50 of 6.7 µM and exhibits no binding at the human EP2 receptor.{3176,3186} It binds with apparent low affinity to the cloned mouse EP1 receptor expressed in CHO cells.{6640} In a model of bone resorption, 3-150 μM SC-19220 inhibited both 1,25 dihydroxy vitamin D3- and PGE2-stimulated osteoclastogenesis in mouse osteoclast precursors.{23818} Antagonism of EP1 with 1 μM SC-19220 has been shown to promote metastasis in a mouse model of metastatic breast cancer.{18890} In a rodent model of Parkinson’s disease, 1.5 μM SC-19220 prevented PGE2-mediated loss of dopaminergic neurons from rat substantia nigra.{15975}  

     

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    Cayman
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  • The physiologic roles and importance of constitutive COX-1 and inducible COX-2 have been reviewed.{11295,10878} SC-236 is a potent, selective, orally active inhibitor of COX-2 with an IC50 of 10 nM and approximately 18,000-fold COX-2 selectivity.{12282} SC-236 has a long plasma half-life and can be dosed once daily (20 mg/kg) in rodents to achieve lasting inhibition of COX-2.{11450}  

     

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    Cayman
    SKU:10004219 - 1 mg

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  • The physiologic roles and importance of constitutive COX-1 and inducible COX-2 have been reviewed.{11295,10878} SC-236 is a potent, selective, orally active inhibitor of COX-2 with an IC50 of 10 nM and approximately 18,000-fold COX-2 selectivity.{12282} SC-236 has a long plasma half-life and can be dosed once daily (20 mg/kg) in rodents to achieve lasting inhibition of COX-2.{11450}  

     

    Brand:
    Cayman
    SKU:10004219 - 10 mg

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  • The physiologic roles and importance of constitutive COX-1 and inducible COX-2 have been reviewed.{11295,10878} SC-236 is a potent, selective, orally active inhibitor of COX-2 with an IC50 of 10 nM and approximately 18,000-fold COX-2 selectivity.{12282} SC-236 has a long plasma half-life and can be dosed once daily (20 mg/kg) in rodents to achieve lasting inhibition of COX-2.{11450}  

     

    Brand:
    Cayman
    SKU:10004219 - 5 mg

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  • The physiologic roles and importance of constitutive COX-1 and inducible COX-2 have been reviewed.{11295,10878} SC-236 is a potent, selective, orally active inhibitor of COX-2 with an IC50 of 10 nM and approximately 18,000-fold COX-2 selectivity.{12282} SC-236 has a long plasma half-life and can be dosed once daily (20 mg/kg) in rodents to achieve lasting inhibition of COX-2.{11450}  

     

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    Cayman
    SKU:10004219 - 50 mg

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  • The prostaglandin E2 (PGE2) receptor EP1 is involved in triggering PGE2-mediated pain as well as neuronal survival and growth. SC-51089 is a selective EP1 antagonist, first shown to have in vivo analgesic activity in mice (ED50 = 6.3 mg/kg when given subcutaneously) and in the rat.{17835,17836} SC-51089 also inhibits the growth of glioma cell lines in vitro (IC50 = ~1 μM) and slows tumor growth in vivo.{17837} In addition, SC-51089 is neuroprotective, attenuating neuronal cell death in response to oxidative stress, an effect that is also found in EP1-/- mice and mediated by PGE2.{15975,17838}  

     

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    Cayman
    SKU:10011561 - 1 mg

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  • The prostaglandin E2 (PGE2) receptor EP1 is involved in triggering PGE2-mediated pain as well as neuronal survival and growth. SC-51089 is a selective EP1 antagonist, first shown to have in vivo analgesic activity in mice (ED50 = 6.3 mg/kg when given subcutaneously) and in the rat.{17835,17836} SC-51089 also inhibits the growth of glioma cell lines in vitro (IC50 = ~1 μM) and slows tumor growth in vivo.{17837} In addition, SC-51089 is neuroprotective, attenuating neuronal cell death in response to oxidative stress, an effect that is also found in EP1-/- mice and mediated by PGE2.{15975,17838}  

     

    Brand:
    Cayman
    SKU:10011561 - 10 mg

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  • The prostaglandin E2 (PGE2) receptor EP1 is involved in triggering PGE2-mediated pain as well as neuronal survival and growth. SC-51089 is a selective EP1 antagonist, first shown to have in vivo analgesic activity in mice (ED50 = 6.3 mg/kg when given subcutaneously) and in the rat.{17835,17836} SC-51089 also inhibits the growth of glioma cell lines in vitro (IC50 = ~1 μM) and slows tumor growth in vivo.{17837} In addition, SC-51089 is neuroprotective, attenuating neuronal cell death in response to oxidative stress, an effect that is also found in EP1-/- mice and mediated by PGE2.{15975,17838}  

     

    Brand:
    Cayman
    SKU:10011561 - 25 mg

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  • The prostaglandin E2 (PGE2) receptor EP1 is involved in triggering PGE2-mediated pain as well as neuronal survival and growth. SC-51089 is a selective EP1 antagonist, first shown to have in vivo analgesic activity in mice (ED50 = 6.3 mg/kg when given subcutaneously) and in the rat.{17835,17836} SC-51089 also inhibits the growth of glioma cell lines in vitro (IC50 = ~1 μM) and slows tumor growth in vivo.{17837} In addition, SC-51089 is neuroprotective, attenuating neuronal cell death in response to oxidative stress, an effect that is also found in EP1-/- mice and mediated by PGE2.{15975,17838}  

     

    Brand:
    Cayman
    SKU:10011561 - 5 mg

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  • The prostaglandin E2 (PGE2) receptor (EP1) is involved in triggering PGE2-mediated pain as well as neuronal survival and growth. SC-51322 is a selective EP1 antagonist that inhibits PGE2 signaling in a guinea pig ileum muscle strip assay with a pA2 value of 8.1 and demonstrates analgesic activity in a mouse writhing assay with an ED50 value of 0.9 mg/kg.{10094} It is pharmacologically similar to SC-51089, but does not release hydrazine, a known carcinogen to rats, as does SC-51089.{10094} SC-51322 potentiates the vasorelaxation of human pulmonary vein induced by PGE2 with an EC50 value of 7.75 µM.{16074}  

     

    Brand:
    Cayman
    SKU:10010744 - 1 mg

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  • The prostaglandin E2 (PGE2) receptor (EP1) is involved in triggering PGE2-mediated pain as well as neuronal survival and growth. SC-51322 is a selective EP1 antagonist that inhibits PGE2 signaling in a guinea pig ileum muscle strip assay with a pA2 value of 8.1 and demonstrates analgesic activity in a mouse writhing assay with an ED50 value of 0.9 mg/kg.{10094} It is pharmacologically similar to SC-51089, but does not release hydrazine, a known carcinogen to rats, as does SC-51089.{10094} SC-51322 potentiates the vasorelaxation of human pulmonary vein induced by PGE2 with an EC50 value of 7.75 µM.{16074}  

     

    Brand:
    Cayman
    SKU:10010744 - 10 mg

    Available on backorder

  • The prostaglandin E2 (PGE2) receptor (EP1) is involved in triggering PGE2-mediated pain as well as neuronal survival and growth. SC-51322 is a selective EP1 antagonist that inhibits PGE2 signaling in a guinea pig ileum muscle strip assay with a pA2 value of 8.1 and demonstrates analgesic activity in a mouse writhing assay with an ED50 value of 0.9 mg/kg.{10094} It is pharmacologically similar to SC-51089, but does not release hydrazine, a known carcinogen to rats, as does SC-51089.{10094} SC-51322 potentiates the vasorelaxation of human pulmonary vein induced by PGE2 with an EC50 value of 7.75 µM.{16074}  

     

    Brand:
    Cayman
    SKU:10010744 - 25 mg

    Available on backorder

  • The prostaglandin E2 (PGE2) receptor (EP1) is involved in triggering PGE2-mediated pain as well as neuronal survival and growth. SC-51322 is a selective EP1 antagonist that inhibits PGE2 signaling in a guinea pig ileum muscle strip assay with a pA2 value of 8.1 and demonstrates analgesic activity in a mouse writhing assay with an ED50 value of 0.9 mg/kg.{10094} It is pharmacologically similar to SC-51089, but does not release hydrazine, a known carcinogen to rats, as does SC-51089.{10094} SC-51322 potentiates the vasorelaxation of human pulmonary vein induced by PGE2 with an EC50 value of 7.75 µM.{16074}  

     

    Brand:
    Cayman
    SKU:10010744 - 5 mg

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  • SC-514 is a selective and reversible inhibitor of IκB kinase 2 (IKK2) (IC50 = 3-12 μM) that displays greater than 10-fold selectivity over 28 other kinases, including JNK, p38, MK2, and ERK.{17344,17345} In synovial fibroblasts stimulated with interleukin (IL)-1β, SC-514 attenuates NF-κB-mediated expression of IL-6, IL-8, and cyclooxygenase-2 (IC50s = 20, 20, and 8 μM, respectively).{17344} SC-514 also reduces NF-κB-mediated expression of other genes, including iNOS in LPS-stimulated smooth muscle cells{17346} and TLR2 in TNF-activated astrocytes.{17347}  

     

    Brand:
    Cayman
    SKU:10010267 - 10 mg

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  • SC-514 is a selective and reversible inhibitor of IκB kinase 2 (IKK2) (IC50 = 3-12 μM) that displays greater than 10-fold selectivity over 28 other kinases, including JNK, p38, MK2, and ERK.{17344,17345} In synovial fibroblasts stimulated with interleukin (IL)-1β, SC-514 attenuates NF-κB-mediated expression of IL-6, IL-8, and cyclooxygenase-2 (IC50s = 20, 20, and 8 μM, respectively).{17344} SC-514 also reduces NF-κB-mediated expression of other genes, including iNOS in LPS-stimulated smooth muscle cells{17346} and TLR2 in TNF-activated astrocytes.{17347}  

     

    Brand:
    Cayman
    SKU:10010267 - 25 mg

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  • SC-514 is a selective and reversible inhibitor of IκB kinase 2 (IKK2) (IC50 = 3-12 μM) that displays greater than 10-fold selectivity over 28 other kinases, including JNK, p38, MK2, and ERK.{17344,17345} In synovial fibroblasts stimulated with interleukin (IL)-1β, SC-514 attenuates NF-κB-mediated expression of IL-6, IL-8, and cyclooxygenase-2 (IC50s = 20, 20, and 8 μM, respectively).{17344} SC-514 also reduces NF-κB-mediated expression of other genes, including iNOS in LPS-stimulated smooth muscle cells{17346} and TLR2 in TNF-activated astrocytes.{17347}  

     

    Brand:
    Cayman
    SKU:10010267 - 5 mg

    Available on backorder

  • SC-514 is a selective and reversible inhibitor of IκB kinase 2 (IKK2) (IC50 = 3-12 μM) that displays greater than 10-fold selectivity over 28 other kinases, including JNK, p38, MK2, and ERK.{17344,17345} In synovial fibroblasts stimulated with interleukin (IL)-1β, SC-514 attenuates NF-κB-mediated expression of IL-6, IL-8, and cyclooxygenase-2 (IC50s = 20, 20, and 8 μM, respectively).{17344} SC-514 also reduces NF-κB-mediated expression of other genes, including iNOS in LPS-stimulated smooth muscle cells{17346} and TLR2 in TNF-activated astrocytes.{17347}  

     

    Brand:
    Cayman
    SKU:10010267 - 50 mg

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  • SC-560 is a member of the diaryl heterocycle class of cyclooxygenase (COX) inhibitors which includes celecoxib (Celebrex™) and rofecoxib (Vioxx™). However, unlike these selective COX-2 inhibitors, SC-560 is a selective inhibitor of COX-1. Using human recombinant enzymes, the IC50 value for SC-560 with respect to COX-1 is 9 nM, while the corresponding IC50 value for COX-2 is 6.3 µM.{7675} Thus, SC-560 shows 700-fold selectivity for the COX-1 enzyme. SC-560 is orally active in the rat, where 10 mg/kg completely abolishes the ionophore-induced production of thromboxane B2 in whole blood. However, SC-560 is ineffective in the treatment of inflammation in models such as the LPS-induced rat air-pouch model, in which the COX-2 generated prostaglandins play a significant role in the inflammatory process.{1282} In whole cells, however, SC-560 appears to act as a non-selective COX inhibitor.{14472} The mechanism of the selective versus non-selective effects of SC-560 in a cell-free environment compared whole cells has not been elucidated.  

     

    Brand:
    Cayman
    SKU:70340 - 1 mg

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  • SC-560 is a member of the diaryl heterocycle class of cyclooxygenase (COX) inhibitors which includes celecoxib (Celebrex™) and rofecoxib (Vioxx™). However, unlike these selective COX-2 inhibitors, SC-560 is a selective inhibitor of COX-1. Using human recombinant enzymes, the IC50 value for SC-560 with respect to COX-1 is 9 nM, while the corresponding IC50 value for COX-2 is 6.3 µM.{7675} Thus, SC-560 shows 700-fold selectivity for the COX-1 enzyme. SC-560 is orally active in the rat, where 10 mg/kg completely abolishes the ionophore-induced production of thromboxane B2 in whole blood. However, SC-560 is ineffective in the treatment of inflammation in models such as the LPS-induced rat air-pouch model, in which the COX-2 generated prostaglandins play a significant role in the inflammatory process.{1282} In whole cells, however, SC-560 appears to act as a non-selective COX inhibitor.{14472} The mechanism of the selective versus non-selective effects of SC-560 in a cell-free environment compared whole cells has not been elucidated.  

     

    Brand:
    Cayman
    SKU:70340 - 10 mg

    Available on backorder

  • SC-560 is a member of the diaryl heterocycle class of cyclooxygenase (COX) inhibitors which includes celecoxib (Celebrex™) and rofecoxib (Vioxx™). However, unlike these selective COX-2 inhibitors, SC-560 is a selective inhibitor of COX-1. Using human recombinant enzymes, the IC50 value for SC-560 with respect to COX-1 is 9 nM, while the corresponding IC50 value for COX-2 is 6.3 µM.{7675} Thus, SC-560 shows 700-fold selectivity for the COX-1 enzyme. SC-560 is orally active in the rat, where 10 mg/kg completely abolishes the ionophore-induced production of thromboxane B2 in whole blood. However, SC-560 is ineffective in the treatment of inflammation in models such as the LPS-induced rat air-pouch model, in which the COX-2 generated prostaglandins play a significant role in the inflammatory process.{1282} In whole cells, however, SC-560 appears to act as a non-selective COX inhibitor.{14472} The mechanism of the selective versus non-selective effects of SC-560 in a cell-free environment compared whole cells has not been elucidated.  

     

    Brand:
    Cayman
    SKU:70340 - 25 mg

    Available on backorder

  • SC-560 is a member of the diaryl heterocycle class of cyclooxygenase (COX) inhibitors which includes celecoxib (Celebrex™) and rofecoxib (Vioxx™). However, unlike these selective COX-2 inhibitors, SC-560 is a selective inhibitor of COX-1. Using human recombinant enzymes, the IC50 value for SC-560 with respect to COX-1 is 9 nM, while the corresponding IC50 value for COX-2 is 6.3 µM.{7675} Thus, SC-560 shows 700-fold selectivity for the COX-1 enzyme. SC-560 is orally active in the rat, where 10 mg/kg completely abolishes the ionophore-induced production of thromboxane B2 in whole blood. However, SC-560 is ineffective in the treatment of inflammation in models such as the LPS-induced rat air-pouch model, in which the COX-2 generated prostaglandins play a significant role in the inflammatory process.{1282} In whole cells, however, SC-560 appears to act as a non-selective COX inhibitor.{14472} The mechanism of the selective versus non-selective effects of SC-560 in a cell-free environment compared whole cells has not been elucidated.  

     

    Brand:
    Cayman
    SKU:70340 - 5 mg

    Available on backorder

  • Brand:
    Cayman
    SKU:760159 - 1 ea

    Available on backorder

  • Leukotriene A4 (LTA4) hydrolase/aminopeptidase is a bifunctional zinc metalloenzyme that both catalyzes the synthesis of LTB4 (Item No. 20110) from LTA4 and cleaves the chemotactic peptide Pro-Gly-Pro.{12673,20329} SC-57461A is a potent, orally active inhibitor of LTA4 hydrolase that blocks ionophore-stimulated LTB4 synthesis in whole blood (IC50 = 49 nM).{31025,31023} It blocks both the hydrolase and aminopeptidase activity in vitro.{31023} SC-57461A is without effect against other enzymes of the arachidonic acid cascade, including 5-lipoxygenase, LTC4 synthase, COX-1, and COX-2. In a rat model of ionophore-induced peritoneal eicosanoid production, SC-57461A inhibits LTB4 biosynthesis without affecting LTC4 (Item No. 20210) or 6-keto prostaglandin F1α production (Item No. 15210).{31024} Oral or topical pretreatment with SC-57461A before challenge with arachidonic acid blocks ear edema in mice.{31024}  

     

    Brand:
    Cayman
    SKU:10108 - 1 mg

    Available on backorder

  • Leukotriene A4 (LTA4) hydrolase/aminopeptidase is a bifunctional zinc metalloenzyme that both catalyzes the synthesis of LTB4 (Item No. 20110) from LTA4 and cleaves the chemotactic peptide Pro-Gly-Pro.{12673,20329} SC-57461A is a potent, orally active inhibitor of LTA4 hydrolase that blocks ionophore-stimulated LTB4 synthesis in whole blood (IC50 = 49 nM).{31025,31023} It blocks both the hydrolase and aminopeptidase activity in vitro.{31023} SC-57461A is without effect against other enzymes of the arachidonic acid cascade, including 5-lipoxygenase, LTC4 synthase, COX-1, and COX-2. In a rat model of ionophore-induced peritoneal eicosanoid production, SC-57461A inhibits LTB4 biosynthesis without affecting LTC4 (Item No. 20210) or 6-keto prostaglandin F1α production (Item No. 15210).{31024} Oral or topical pretreatment with SC-57461A before challenge with arachidonic acid blocks ear edema in mice.{31024}  

     

    Brand:
    Cayman
    SKU:10108 - 10 mg

    Available on backorder

  • Leukotriene A4 (LTA4) hydrolase/aminopeptidase is a bifunctional zinc metalloenzyme that both catalyzes the synthesis of LTB4 (Item No. 20110) from LTA4 and cleaves the chemotactic peptide Pro-Gly-Pro.{12673,20329} SC-57461A is a potent, orally active inhibitor of LTA4 hydrolase that blocks ionophore-stimulated LTB4 synthesis in whole blood (IC50 = 49 nM).{31025,31023} It blocks both the hydrolase and aminopeptidase activity in vitro.{31023} SC-57461A is without effect against other enzymes of the arachidonic acid cascade, including 5-lipoxygenase, LTC4 synthase, COX-1, and COX-2. In a rat model of ionophore-induced peritoneal eicosanoid production, SC-57461A inhibits LTB4 biosynthesis without affecting LTC4 (Item No. 20210) or 6-keto prostaglandin F1α production (Item No. 15210).{31024} Oral or topical pretreatment with SC-57461A before challenge with arachidonic acid blocks ear edema in mice.{31024}  

     

    Brand:
    Cayman
    SKU:10108 - 25 mg

    Available on backorder

  • Leukotriene A4 (LTA4) hydrolase/aminopeptidase is a bifunctional zinc metalloenzyme that both catalyzes the synthesis of LTB4 (Item No. 20110) from LTA4 and cleaves the chemotactic peptide Pro-Gly-Pro.{12673,20329} SC-57461A is a potent, orally active inhibitor of LTA4 hydrolase that blocks ionophore-stimulated LTB4 synthesis in whole blood (IC50 = 49 nM).{31025,31023} It blocks both the hydrolase and aminopeptidase activity in vitro.{31023} SC-57461A is without effect against other enzymes of the arachidonic acid cascade, including 5-lipoxygenase, LTC4 synthase, COX-1, and COX-2. In a rat model of ionophore-induced peritoneal eicosanoid production, SC-57461A inhibits LTB4 biosynthesis without affecting LTC4 (Item No. 20210) or 6-keto prostaglandin F1α production (Item No. 15210).{31024} Oral or topical pretreatment with SC-57461A before challenge with arachidonic acid blocks ear edema in mice.{31024}  

     

    Brand:
    Cayman
    SKU:10108 - 5 mg

    Available on backorder

  • SC-58125 is a member of the diaryl heterocycle group of selective COX-2 inhibitors which includes MK 966 (rofecoxib), DUP-697, and celecoxib. SC-58125 is a potent and time-dependent inhibitor of COX-2.{1299} When tested on the isolated recombinant enzymes, SC-58125 is at least 150 times more potent in the inhibition of COX-2 as COX-1.{3464} In cultured HUVEC cells, SC-58125 inhibits COX-2 with an IC50 of 70 nM.{5498} It also inhibits the growth of the COX-2 expressing cell line HCA-7 in nude mice at 5-10 mg/kg when given intraperitoneally.{6465}  

     

    Brand:
    Cayman
    SKU:70655 - 1 mg

    Available on backorder

  • SC-58125 is a member of the diaryl heterocycle group of selective COX-2 inhibitors which includes MK 966 (rofecoxib), DUP-697, and celecoxib. SC-58125 is a potent and time-dependent inhibitor of COX-2.{1299} When tested on the isolated recombinant enzymes, SC-58125 is at least 150 times more potent in the inhibition of COX-2 as COX-1.{3464} In cultured HUVEC cells, SC-58125 inhibits COX-2 with an IC50 of 70 nM.{5498} It also inhibits the growth of the COX-2 expressing cell line HCA-7 in nude mice at 5-10 mg/kg when given intraperitoneally.{6465}  

     

    Brand:
    Cayman
    SKU:70655 - 10 mg

    Available on backorder

  • SC-58125 is a member of the diaryl heterocycle group of selective COX-2 inhibitors which includes MK 966 (rofecoxib), DUP-697, and celecoxib. SC-58125 is a potent and time-dependent inhibitor of COX-2.{1299} When tested on the isolated recombinant enzymes, SC-58125 is at least 150 times more potent in the inhibition of COX-2 as COX-1.{3464} In cultured HUVEC cells, SC-58125 inhibits COX-2 with an IC50 of 70 nM.{5498} It also inhibits the growth of the COX-2 expressing cell line HCA-7 in nude mice at 5-10 mg/kg when given intraperitoneally.{6465}  

     

    Brand:
    Cayman
    SKU:70655 - 25 mg

    Available on backorder

  • SC-58125 is a member of the diaryl heterocycle group of selective COX-2 inhibitors which includes MK 966 (rofecoxib), DUP-697, and celecoxib. SC-58125 is a potent and time-dependent inhibitor of COX-2.{1299} When tested on the isolated recombinant enzymes, SC-58125 is at least 150 times more potent in the inhibition of COX-2 as COX-1.{3464} In cultured HUVEC cells, SC-58125 inhibits COX-2 with an IC50 of 70 nM.{5498} It also inhibits the growth of the COX-2 expressing cell line HCA-7 in nude mice at 5-10 mg/kg when given intraperitoneally.{6465}  

     

    Brand:
    Cayman
    SKU:70655 - 5 mg

    Available on backorder

  • Akt activation requires binding of its pleckstrin homology domain (PHD) to membrane-associated phosphatidylinositol-3,4,5-trisphosphate (PIP3) or phosphatidylinositol-3,4-bisphosphate (PIP2).{13740} Increased Akt activity, e.g., through a gain-of-function mutation in the PHD of Akt1, is pivotal to many types of cancer.{15097} Activated Akt may be regulated by various events, including ubiquitination-mediated deactivation. SC-66 is an allosteric inhibitor of Akt that facilitates both ubiquitination and deactivation of Akt.{19437} At 4 μg/ml, SC-66 inhibits Akt activity in HEK293T cells and in HEK293 cells stably expressing Akt with the gain-of-function pleckstrin homology domain mutation, promoting cell death.{19437} In nude mice inoculated with HEK293T cells, SC-66 (15 mg/kg) suppresses tumor growth.{19437}  

     

    Brand:
    Cayman
    SKU:10876 - 10 mg

    Available on backorder

  • Akt activation requires binding of its pleckstrin homology domain (PHD) to membrane-associated phosphatidylinositol-3,4,5-trisphosphate (PIP3) or phosphatidylinositol-3,4-bisphosphate (PIP2).{13740} Increased Akt activity, e.g., through a gain-of-function mutation in the PHD of Akt1, is pivotal to many types of cancer.{15097} Activated Akt may be regulated by various events, including ubiquitination-mediated deactivation. SC-66 is an allosteric inhibitor of Akt that facilitates both ubiquitination and deactivation of Akt.{19437} At 4 μg/ml, SC-66 inhibits Akt activity in HEK293T cells and in HEK293 cells stably expressing Akt with the gain-of-function pleckstrin homology domain mutation, promoting cell death.{19437} In nude mice inoculated with HEK293T cells, SC-66 (15 mg/kg) suppresses tumor growth.{19437}  

     

    Brand:
    Cayman
    SKU:10876 - 100 mg

    Available on backorder

  • Akt activation requires binding of its pleckstrin homology domain (PHD) to membrane-associated phosphatidylinositol-3,4,5-trisphosphate (PIP3) or phosphatidylinositol-3,4-bisphosphate (PIP2).{13740} Increased Akt activity, e.g., through a gain-of-function mutation in the PHD of Akt1, is pivotal to many types of cancer.{15097} Activated Akt may be regulated by various events, including ubiquitination-mediated deactivation. SC-66 is an allosteric inhibitor of Akt that facilitates both ubiquitination and deactivation of Akt.{19437} At 4 μg/ml, SC-66 inhibits Akt activity in HEK293T cells and in HEK293 cells stably expressing Akt with the gain-of-function pleckstrin homology domain mutation, promoting cell death.{19437} In nude mice inoculated with HEK293T cells, SC-66 (15 mg/kg) suppresses tumor growth.{19437}  

     

    Brand:
    Cayman
    SKU:10876 - 25 mg

    Available on backorder

  • Akt activation requires binding of its pleckstrin homology domain (PHD) to membrane-associated phosphatidylinositol-3,4,5-trisphosphate (PIP3) or phosphatidylinositol-3,4-bisphosphate (PIP2).{13740} Increased Akt activity, e.g., through a gain-of-function mutation in the PHD of Akt1, is pivotal to many types of cancer.{15097} Activated Akt may be regulated by various events, including ubiquitination-mediated deactivation. SC-66 is an allosteric inhibitor of Akt that facilitates both ubiquitination and deactivation of Akt.{19437} At 4 μg/ml, SC-66 inhibits Akt activity in HEK293T cells and in HEK293 cells stably expressing Akt with the gain-of-function pleckstrin homology domain mutation, promoting cell death.{19437} In nude mice inoculated with HEK293T cells, SC-66 (15 mg/kg) suppresses tumor growth.{19437}  

     

    Brand:
    Cayman
    SKU:10876 - 5 mg

    Available on backorder

  • SC-75741 is an inhibitor of NF-κB (EC50 = 0.1 μM in an NF-κB reporter gene assay).{39637} It inhibits replication of human, avian, and swine influenza virus strains in MDCK cells in a concentration-dependent manner.{39638} It also reversibly inhibits replication of H5N1 and H7N7 avian influenza virus strains in human A549 cells. In vivo, SC-75741 (15 mg/kg, i.p.) reduces viral mRNA and production of IL-6 and CXCL10/IP-10 in the lungs of H5N1 infected mice. SC-75741 is also protective against H5N1 and H7N7 infection in mice when administered for 7 days prior to or up to 4 days post infection.{39639}  

     

    Brand:
    Cayman
    SKU:21818 -

    Out of stock

  • SC-75741 is an inhibitor of NF-κB (EC50 = 0.1 μM in an NF-κB reporter gene assay).{39637} It inhibits replication of human, avian, and swine influenza virus strains in MDCK cells in a concentration-dependent manner.{39638} It also reversibly inhibits replication of H5N1 and H7N7 avian influenza virus strains in human A549 cells. In vivo, SC-75741 (15 mg/kg, i.p.) reduces viral mRNA and production of IL-6 and CXCL10/IP-10 in the lungs of H5N1 infected mice. SC-75741 is also protective against H5N1 and H7N7 infection in mice when administered for 7 days prior to or up to 4 days post infection.{39639}  

     

    Brand:
    Cayman
    SKU:21818 -

    Out of stock

  • SC-75741 is an inhibitor of NF-κB (EC50 = 0.1 μM in an NF-κB reporter gene assay).{39637} It inhibits replication of human, avian, and swine influenza virus strains in MDCK cells in a concentration-dependent manner.{39638} It also reversibly inhibits replication of H5N1 and H7N7 avian influenza virus strains in human A549 cells. In vivo, SC-75741 (15 mg/kg, i.p.) reduces viral mRNA and production of IL-6 and CXCL10/IP-10 in the lungs of H5N1 infected mice. SC-75741 is also protective against H5N1 and H7N7 infection in mice when administered for 7 days prior to or up to 4 days post infection.{39639}  

     

    Brand:
    Cayman
    SKU:21818 -

    Out of stock

  • SC-79 is an activator of Akt that blocks its membrane translocation while allowing its phosphorylation, in the cytosol, by upstream kinases.{31840} For example, both Thr308 and Ser473 on Akt are phosphorylated in serum starved HeLa cells treated for 1 hour with insulin growth factor and SC-79 (4 µg/ml).{31840} SC-79 permits phosphorylation and activation of all isoforms of Akt, it is active in multiple cell types, and works in both receptor tyrosine kinase- and G protein-coupled receptor-mediated signaling.{31840} SC-79 has been used to elucidate the role of Akt signaling in neuronal survival, glucose-mediated apoptosis in podocytes, and miR-221-regulated cancer cell proliferation.{31841,31840,31842}  

     

    Brand:
    Cayman
    SKU:-
  • SC-79 is an activator of Akt that blocks its membrane translocation while allowing its phosphorylation, in the cytosol, by upstream kinases.{31840} For example, both Thr308 and Ser473 on Akt are phosphorylated in serum starved HeLa cells treated for 1 hour with insulin growth factor and SC-79 (4 µg/ml).{31840} SC-79 permits phosphorylation and activation of all isoforms of Akt, it is active in multiple cell types, and works in both receptor tyrosine kinase- and G protein-coupled receptor-mediated signaling.{31840} SC-79 has been used to elucidate the role of Akt signaling in neuronal survival, glucose-mediated apoptosis in podocytes, and miR-221-regulated cancer cell proliferation.{31841,31840,31842}  

     

    Brand:
    Cayman
    SKU:-
  • SC-79 is an activator of Akt that blocks its membrane translocation while allowing its phosphorylation, in the cytosol, by upstream kinases.{31840} For example, both Thr308 and Ser473 on Akt are phosphorylated in serum starved HeLa cells treated for 1 hour with insulin growth factor and SC-79 (4 µg/ml).{31840} SC-79 permits phosphorylation and activation of all isoforms of Akt, it is active in multiple cell types, and works in both receptor tyrosine kinase- and G protein-coupled receptor-mediated signaling.{31840} SC-79 has been used to elucidate the role of Akt signaling in neuronal survival, glucose-mediated apoptosis in podocytes, and miR-221-regulated cancer cell proliferation.{31841,31840,31842}  

     

    Brand:
    Cayman
    SKU:-
  • SC-9 is an activator of protein kinase C (PKC).{52559} It is selective for PKC over myosin light-chain kinase (MLCK), PKA, and PKG at 300 µM. SC-9 (200 µM) increases PKC-induced MLC phosphorylation in the presence of calcium.{52561} It induces proliferation of quiescent primary neonatal mouse epidermal melanoblasts when used at a concentration of 10 µM.{52560} SC-9 (2.5-20 µM) reduces the motility of isolated intact chicken sperm.{52562}  

     

    Brand:
    Cayman
    SKU:30910 - 1 mg

    Available on backorder

  • SC-9 is an activator of protein kinase C (PKC).{52559} It is selective for PKC over myosin light-chain kinase (MLCK), PKA, and PKG at 300 µM. SC-9 (200 µM) increases PKC-induced MLC phosphorylation in the presence of calcium.{52561} It induces proliferation of quiescent primary neonatal mouse epidermal melanoblasts when used at a concentration of 10 µM.{52560} SC-9 (2.5-20 µM) reduces the motility of isolated intact chicken sperm.{52562}  

     

    Brand:
    Cayman
    SKU:30910 - 10 mg

    Available on backorder

  • SC-9 is an activator of protein kinase C (PKC).{52559} It is selective for PKC over myosin light-chain kinase (MLCK), PKA, and PKG at 300 µM. SC-9 (200 µM) increases PKC-induced MLC phosphorylation in the presence of calcium.{52561} It induces proliferation of quiescent primary neonatal mouse epidermal melanoblasts when used at a concentration of 10 µM.{52560} SC-9 (2.5-20 µM) reduces the motility of isolated intact chicken sperm.{52562}  

     

    Brand:
    Cayman
    SKU:30910 - 5 mg

    Available on backorder

  • SC144 is an orally bioavailable gp130 inhibitor.{46760} It inhibits phosphorylation of STAT1, STAT3, and Akt induced by leukemia inhibitory factor (LIF) and IL-6, but not IFN-γ, in OVCAR-8 ovarian cancer cells when used at a concentration of 20 µM. SC144 induces cell cycle arrest at the G0/G1 phase in MDA-MB-435 breast and HT-29 colorectal cancer cells and inhibits proliferation of 14 cancer cell lines, including prostate, ovarian, lung, breast, and colorectal cancer cells, with IC50 values ranging from 0.4 to 4 µM.{46761} It reduces tumor growth in OVCAR-8 and MDA-MB-435 mouse xenograft models.{46760,46761}  

     

    Brand:
    Cayman
    SKU:29714 - 1 mg

    Available on backorder

  • SC144 is an orally bioavailable gp130 inhibitor.{46760} It inhibits phosphorylation of STAT1, STAT3, and Akt induced by leukemia inhibitory factor (LIF) and IL-6, but not IFN-γ, in OVCAR-8 ovarian cancer cells when used at a concentration of 20 µM. SC144 induces cell cycle arrest at the G0/G1 phase in MDA-MB-435 breast and HT-29 colorectal cancer cells and inhibits proliferation of 14 cancer cell lines, including prostate, ovarian, lung, breast, and colorectal cancer cells, with IC50 values ranging from 0.4 to 4 µM.{46761} It reduces tumor growth in OVCAR-8 and MDA-MB-435 mouse xenograft models.{46760,46761}  

     

    Brand:
    Cayman
    SKU:29714 - 10 mg

    Available on backorder

  • SC144 is an orally bioavailable gp130 inhibitor.{46760} It inhibits phosphorylation of STAT1, STAT3, and Akt induced by leukemia inhibitory factor (LIF) and IL-6, but not IFN-γ, in OVCAR-8 ovarian cancer cells when used at a concentration of 20 µM. SC144 induces cell cycle arrest at the G0/G1 phase in MDA-MB-435 breast and HT-29 colorectal cancer cells and inhibits proliferation of 14 cancer cell lines, including prostate, ovarian, lung, breast, and colorectal cancer cells, with IC50 values ranging from 0.4 to 4 µM.{46761} It reduces tumor growth in OVCAR-8 and MDA-MB-435 mouse xenograft models.{46760,46761}  

     

    Brand:
    Cayman
    SKU:29714 - 25 mg

    Available on backorder

  • SC144 is an orally bioavailable gp130 inhibitor.{46760} It inhibits phosphorylation of STAT1, STAT3, and Akt induced by leukemia inhibitory factor (LIF) and IL-6, but not IFN-γ, in OVCAR-8 ovarian cancer cells when used at a concentration of 20 µM. SC144 induces cell cycle arrest at the G0/G1 phase in MDA-MB-435 breast and HT-29 colorectal cancer cells and inhibits proliferation of 14 cancer cell lines, including prostate, ovarian, lung, breast, and colorectal cancer cells, with IC50 values ranging from 0.4 to 4 µM.{46761} It reduces tumor growth in OVCAR-8 and MDA-MB-435 mouse xenograft models.{46760,46761}  

     

    Brand:
    Cayman
    SKU:29714 - 5 mg

    Available on backorder

  • SCH 202676 is a reversible inhibitor of both agonist and antagonist binding to diverse G protein-coupled receptors (GPCRs).{27649} It blocks the binding of radiolabeled ligands to human opioid, adrenergic, muscarinic, dopaminergic, adenosine, and purinergic receptors.{27649,27648,27647} It displays IC50 values of 0.1 to 1.8 µM for modulating ligand binding.{27649,27648} SCH 202676 may modulate GPCRs via thiol modification.{27646}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • SCH 202676 is a reversible inhibitor of both agonist and antagonist binding to diverse G protein-coupled receptors (GPCRs).{27649} It blocks the binding of radiolabeled ligands to human opioid, adrenergic, muscarinic, dopaminergic, adenosine, and purinergic receptors.{27649,27648,27647} It displays IC50 values of 0.1 to 1.8 µM for modulating ligand binding.{27649,27648} SCH 202676 may modulate GPCRs via thiol modification.{27646}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • SCH 202676 is a reversible inhibitor of both agonist and antagonist binding to diverse G protein-coupled receptors (GPCRs).{27649} It blocks the binding of radiolabeled ligands to human opioid, adrenergic, muscarinic, dopaminergic, adenosine, and purinergic receptors.{27649,27648,27647} It displays IC50 values of 0.1 to 1.8 µM for modulating ligand binding.{27649,27648} SCH 202676 may modulate GPCRs via thiol modification.{27646}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • SCH 202676 is a reversible inhibitor of both agonist and antagonist binding to diverse G protein-coupled receptors (GPCRs).{27649} It blocks the binding of radiolabeled ligands to human opioid, adrenergic, muscarinic, dopaminergic, adenosine, and purinergic receptors.{27649,27648,27647} It displays IC50 values of 0.1 to 1.8 µM for modulating ligand binding.{27649,27648} SCH 202676 may modulate GPCRs via thiol modification.{27646}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • SCH 23390 is a halobenzazepine that acts as a selective antagonist of the dopamine D1-like receptor subtypes D1 and D5 (Kis = 0.2 and 0.3 nM, respectively).{25563} In vivo studies have demonstrated that SCH 23390 can abolish pharmacologically-induced seizures.{25563} This compound is useful for studying the role of the dopamine system in normal brain function and neurological disorders.{24104,17607,11498,20951}  

     

    Brand:
    Cayman
    SKU:-
  • SCH 23390 is a halobenzazepine that acts as a selective antagonist of the dopamine D1-like receptor subtypes D1 and D5 (Kis = 0.2 and 0.3 nM, respectively).{25563} In vivo studies have demonstrated that SCH 23390 can abolish pharmacologically-induced seizures.{25563} This compound is useful for studying the role of the dopamine system in normal brain function and neurological disorders.{24104,17607,11498,20951}  

     

    Brand:
    Cayman
    SKU:-
  • SCH 28080 is a reversible K+-competitive inhibitor of H+/K+-ATPases that is best known for its ability to block acid secretion through its action against the gastric H+/K+-ATPase (IC50 = 1.3 µM).{29478,29482,29481} It is effective against gastric H+/K+-ATPases from a variety of species and can inhibit colonic H+/K+-ATPases, but this activity appears to be species-dependent.{29480} SCH 28080 is also used to investigate the role of H+/K+-ATPases in non-mammalian organisms and to distinguish the actions of H+/K+-ATPases from other ATP-dependent transporters.{29477,29479}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • SCH 28080 is a reversible K+-competitive inhibitor of H+/K+-ATPases that is best known for its ability to block acid secretion through its action against the gastric H+/K+-ATPase (IC50 = 1.3 µM).{29478,29482,29481} It is effective against gastric H+/K+-ATPases from a variety of species and can inhibit colonic H+/K+-ATPases, but this activity appears to be species-dependent.{29480} SCH 28080 is also used to investigate the role of H+/K+-ATPases in non-mammalian organisms and to distinguish the actions of H+/K+-ATPases from other ATP-dependent transporters.{29477,29479}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • SCH 28080 is a reversible K+-competitive inhibitor of H+/K+-ATPases that is best known for its ability to block acid secretion through its action against the gastric H+/K+-ATPase (IC50 = 1.3 µM).{29478,29482,29481} It is effective against gastric H+/K+-ATPases from a variety of species and can inhibit colonic H+/K+-ATPases, but this activity appears to be species-dependent.{29480} SCH 28080 is also used to investigate the role of H+/K+-ATPases in non-mammalian organisms and to distinguish the actions of H+/K+-ATPases from other ATP-dependent transporters.{29477,29479}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • SCH 28080 is a reversible K+-competitive inhibitor of H+/K+-ATPases that is best known for its ability to block acid secretion through its action against the gastric H+/K+-ATPase (IC50 = 1.3 µM).{29478,29482,29481} It is effective against gastric H+/K+-ATPases from a variety of species and can inhibit colonic H+/K+-ATPases, but this activity appears to be species-dependent.{29480} SCH 28080 is also used to investigate the role of H+/K+-ATPases in non-mammalian organisms and to distinguish the actions of H+/K+-ATPases from other ATP-dependent transporters.{29477,29479}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • SCH 38519 is an isochromanequinone fungal metabolite originally isolated from Thermomonospora.{42785} It inhibits aggregation induced by thrombin (Item No. 13188), as well as inhibits serotonin secretion in human platelets (IC50s = 68 and 61 µg/ml, respectively).{42786} It inhibits the growth of various Gram-negative and Gram-positive bacteria (mean MICs = 122.1 and 0.92 µg/ml, respectively).  

     

    Brand:
    Cayman
    SKU:28092 - 2.5 mg

    Available on backorder

  • SCH 38519 is an isochromanequinone fungal metabolite originally isolated from Thermomonospora.{42785} It inhibits aggregation induced by thrombin (Item No. 13188), as well as inhibits serotonin secretion in human platelets (IC50s = 68 and 61 µg/ml, respectively).{42786} It inhibits the growth of various Gram-negative and Gram-positive bacteria (mean MICs = 122.1 and 0.92 µg/ml, respectively).  

     

    Brand:
    Cayman
    SKU:28092 - 500 µg

    Available on backorder

  • SCH 39166 is a dopamine D1 receptor antagonist (Ki = 5 nM).{39925} It is selective for D1 over D2-4 receptors (Kis = 3,751, >1,000, and 5,934 nM, respectively), however, it also binds to D5 receptors (Ki = 4.4 nM). SCH 39166 inhibits food intake in a dose-dependent manner in rats (ED50 = 0.84 mg/kg).{39926} It reduces ethanol intake in Sardinian alcohol-preferring rats and sucrose intake in water-deprived and water-sated rats without affecting food or total fluid intake.{39927} SCH 39166 also suppresses cocaine-induced arrhythmias in anesthetized dogs.{39928}  

     

    Brand:
    Cayman
    SKU:25331 - 1 mg

    Available on backorder

  • SCH 39166 is a dopamine D1 receptor antagonist (Ki = 5 nM).{39925} It is selective for D1 over D2-4 receptors (Kis = 3,751, >1,000, and 5,934 nM, respectively), however, it also binds to D5 receptors (Ki = 4.4 nM). SCH 39166 inhibits food intake in a dose-dependent manner in rats (ED50 = 0.84 mg/kg).{39926} It reduces ethanol intake in Sardinian alcohol-preferring rats and sucrose intake in water-deprived and water-sated rats without affecting food or total fluid intake.{39927} SCH 39166 also suppresses cocaine-induced arrhythmias in anesthetized dogs.{39928}  

     

    Brand:
    Cayman
    SKU:25331 - 10 mg

    Available on backorder

  • SCH 39166 is a dopamine D1 receptor antagonist (Ki = 5 nM).{39925} It is selective for D1 over D2-4 receptors (Kis = 3,751, >1,000, and 5,934 nM, respectively), however, it also binds to D5 receptors (Ki = 4.4 nM). SCH 39166 inhibits food intake in a dose-dependent manner in rats (ED50 = 0.84 mg/kg).{39926} It reduces ethanol intake in Sardinian alcohol-preferring rats and sucrose intake in water-deprived and water-sated rats without affecting food or total fluid intake.{39927} SCH 39166 also suppresses cocaine-induced arrhythmias in anesthetized dogs.{39928}  

     

    Brand:
    Cayman
    SKU:25331 - 5 mg

    Available on backorder

  • SCH 442416 is a potent, brain-permeable, and selective adenosine A2A receptor (A2AR) antagonist.{40048} It is selective for A2AR with a Ki value of 0.048 nM compared to 1,111, >10,000, and >10,000 nM for A1R, A2BR, and A3R, respectively, using human recombinant protein in a radioligand binding assay. It is also selective for A2AR (Ki = 0.50 nM) in rat cerebral membranes over A1R and A3R (Kis = 1,815 and >10,000, respectively). Biodistribution in rats demonstrates preferential uptake by liver, adrenal gland, kidney, and lungs, and by the striatum in the brain. SCH 442416 (10 μM) attenuates adenosine-mediated and A2AR agonist-induced arteriole dilation.{40049}  

     

    Brand:
    Cayman
    SKU:22233 -

    Out of stock

  • SCH 442416 is a potent, brain-permeable, and selective adenosine A2A receptor (A2AR) antagonist.{40048} It is selective for A2AR with a Ki value of 0.048 nM compared to 1,111, >10,000, and >10,000 nM for A1R, A2BR, and A3R, respectively, using human recombinant protein in a radioligand binding assay. It is also selective for A2AR (Ki = 0.50 nM) in rat cerebral membranes over A1R and A3R (Kis = 1,815 and >10,000, respectively). Biodistribution in rats demonstrates preferential uptake by liver, adrenal gland, kidney, and lungs, and by the striatum in the brain. SCH 442416 (10 μM) attenuates adenosine-mediated and A2AR agonist-induced arteriole dilation.{40049}  

     

    Brand:
    Cayman
    SKU:22233 -

    Out of stock

  • SCH 442416 is a potent, brain-permeable, and selective adenosine A2A receptor (A2AR) antagonist.{40048} It is selective for A2AR with a Ki value of 0.048 nM compared to 1,111, >10,000, and >10,000 nM for A1R, A2BR, and A3R, respectively, using human recombinant protein in a radioligand binding assay. It is also selective for A2AR (Ki = 0.50 nM) in rat cerebral membranes over A1R and A3R (Kis = 1,815 and >10,000, respectively). Biodistribution in rats demonstrates preferential uptake by liver, adrenal gland, kidney, and lungs, and by the striatum in the brain. SCH 442416 (10 μM) attenuates adenosine-mediated and A2AR agonist-induced arteriole dilation.{40049}  

     

    Brand:
    Cayman
    SKU:22233 -

    Out of stock

  • SCH 442416 is a potent, brain-permeable, and selective adenosine A2A receptor (A2AR) antagonist.{40048} It is selective for A2AR with a Ki value of 0.048 nM compared to 1,111, >10,000, and >10,000 nM for A1R, A2BR, and A3R, respectively, using human recombinant protein in a radioligand binding assay. It is also selective for A2AR (Ki = 0.50 nM) in rat cerebral membranes over A1R and A3R (Kis = 1,815 and >10,000, respectively). Biodistribution in rats demonstrates preferential uptake by liver, adrenal gland, kidney, and lungs, and by the striatum in the brain. SCH 442416 (10 μM) attenuates adenosine-mediated and A2AR agonist-induced arteriole dilation.{40049}  

     

    Brand:
    Cayman
    SKU:22233 -

    Out of stock

  • SCH 51344 is a pyrazolo-quinoline derivative that inhibits Ras-induced malignant transformation and prevents anchorage-independent growth of oncogene transformed fibroblasts.{28957} At 5-25 µM, it has been shown to dose-dependently block Ras/Rac-induced membrane ruffling in REF-52 fibroblasts with little effect on Ras-induced ERK and JNK kinase activity.{28958} SCH 51344 is also reported to be a potent inhibitor of human mutT homolog MTH1, a nucleotide pool sanitizing enzyme that cleaves oxidized nucleotides (Kd = 49 nM).{28959}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • SCH 51344 is a pyrazolo-quinoline derivative that inhibits Ras-induced malignant transformation and prevents anchorage-independent growth of oncogene transformed fibroblasts.{28957} At 5-25 µM, it has been shown to dose-dependently block Ras/Rac-induced membrane ruffling in REF-52 fibroblasts with little effect on Ras-induced ERK and JNK kinase activity.{28958} SCH 51344 is also reported to be a potent inhibitor of human mutT homolog MTH1, a nucleotide pool sanitizing enzyme that cleaves oxidized nucleotides (Kd = 49 nM).{28959}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • SCH 51344 is a pyrazolo-quinoline derivative that inhibits Ras-induced malignant transformation and prevents anchorage-independent growth of oncogene transformed fibroblasts.{28957} At 5-25 µM, it has been shown to dose-dependently block Ras/Rac-induced membrane ruffling in REF-52 fibroblasts with little effect on Ras-induced ERK and JNK kinase activity.{28958} SCH 51344 is also reported to be a potent inhibitor of human mutT homolog MTH1, a nucleotide pool sanitizing enzyme that cleaves oxidized nucleotides (Kd = 49 nM).{28959}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • SCH 527123 is an allosteric antagonist of C-X-C chemokine receptor type 1 (CXCR1; IC50 = 43 nM in Ba/F3 cells) and CXCR2 (IC50 = 0.97 nM in HTS cells).{45387} It inhibits calcium flux induced by CXCL8 in Ba/F3 cells expressing human recombinant CXCR1 or CXCR2. SCH 527123 (3 nM) inhibits CXCL8-induced chemotaxis of Ba/F3 cells expressing human recombinant CXCR2 and CXCL1-induced chemotaxis of isolated human polymorphonuclear cells (PMNs). It also inhibits LPS-induced neutrophil infiltration into the lung (ED50 = 1.8 mg/kg) and increases mucin levels in bronchoalveolar lavage fluid (BALF) in a rat model of airway inflammation.{45388} SCH 527123 inhibits proliferation of wild-type (IC50s = 28.95 and 18.78 µM, respectively) and IL-8 overexpressing HCT116 and Caco-2 cells (IC50s = 39.45 and 25.45 µM, respectively).{45389} It reduces tumor growth in an HCT116 mouse xenograft model when administered at a dose of 50 mg/kg per day.  

     

    Brand:
    Cayman
    SKU:27800 - 1 mg

    Available on backorder

  • SCH 527123 is an allosteric antagonist of C-X-C chemokine receptor type 1 (CXCR1; IC50 = 43 nM in Ba/F3 cells) and CXCR2 (IC50 = 0.97 nM in HTS cells).{45387} It inhibits calcium flux induced by CXCL8 in Ba/F3 cells expressing human recombinant CXCR1 or CXCR2. SCH 527123 (3 nM) inhibits CXCL8-induced chemotaxis of Ba/F3 cells expressing human recombinant CXCR2 and CXCL1-induced chemotaxis of isolated human polymorphonuclear cells (PMNs). It also inhibits LPS-induced neutrophil infiltration into the lung (ED50 = 1.8 mg/kg) and increases mucin levels in bronchoalveolar lavage fluid (BALF) in a rat model of airway inflammation.{45388} SCH 527123 inhibits proliferation of wild-type (IC50s = 28.95 and 18.78 µM, respectively) and IL-8 overexpressing HCT116 and Caco-2 cells (IC50s = 39.45 and 25.45 µM, respectively).{45389} It reduces tumor growth in an HCT116 mouse xenograft model when administered at a dose of 50 mg/kg per day.  

     

    Brand:
    Cayman
    SKU:27800 - 10 mg

    Available on backorder

  • SCH 527123 is an allosteric antagonist of C-X-C chemokine receptor type 1 (CXCR1; IC50 = 43 nM in Ba/F3 cells) and CXCR2 (IC50 = 0.97 nM in HTS cells).{45387} It inhibits calcium flux induced by CXCL8 in Ba/F3 cells expressing human recombinant CXCR1 or CXCR2. SCH 527123 (3 nM) inhibits CXCL8-induced chemotaxis of Ba/F3 cells expressing human recombinant CXCR2 and CXCL1-induced chemotaxis of isolated human polymorphonuclear cells (PMNs). It also inhibits LPS-induced neutrophil infiltration into the lung (ED50 = 1.8 mg/kg) and increases mucin levels in bronchoalveolar lavage fluid (BALF) in a rat model of airway inflammation.{45388} SCH 527123 inhibits proliferation of wild-type (IC50s = 28.95 and 18.78 µM, respectively) and IL-8 overexpressing HCT116 and Caco-2 cells (IC50s = 39.45 and 25.45 µM, respectively).{45389} It reduces tumor growth in an HCT116 mouse xenograft model when administered at a dose of 50 mg/kg per day.  

     

    Brand:
    Cayman
    SKU:27800 - 25 mg

    Available on backorder

  • SCH 527123 is an allosteric antagonist of C-X-C chemokine receptor type 1 (CXCR1; IC50 = 43 nM in Ba/F3 cells) and CXCR2 (IC50 = 0.97 nM in HTS cells).{45387} It inhibits calcium flux induced by CXCL8 in Ba/F3 cells expressing human recombinant CXCR1 or CXCR2. SCH 527123 (3 nM) inhibits CXCL8-induced chemotaxis of Ba/F3 cells expressing human recombinant CXCR2 and CXCL1-induced chemotaxis of isolated human polymorphonuclear cells (PMNs). It also inhibits LPS-induced neutrophil infiltration into the lung (ED50 = 1.8 mg/kg) and increases mucin levels in bronchoalveolar lavage fluid (BALF) in a rat model of airway inflammation.{45388} SCH 527123 inhibits proliferation of wild-type (IC50s = 28.95 and 18.78 µM, respectively) and IL-8 overexpressing HCT116 and Caco-2 cells (IC50s = 39.45 and 25.45 µM, respectively).{45389} It reduces tumor growth in an HCT116 mouse xenograft model when administered at a dose of 50 mg/kg per day.  

     

    Brand:
    Cayman
    SKU:27800 - 5 mg

    Available on backorder

  • SCH 529074 is a small molecule activator of p53, a tumor suppressor that is mutated or non-functional in 50% of human tumors.{41050} SCH 529074 restores DNA binding activity and increases DNA binding affinity of two recombinant GST fusion mutant p53 DNA binding domains (R273H and R249S) in an electrophoretic mobility shift assay with Kd values of 0.6740 and 0.4313, respectively. It also stimulates DNA binding activity and prevents human double minute-2 (Hdm-2) ubiquitination of wild-type p53 in vitro. SCH 29074 reduces proliferation of tumor cell lines with mutant and wild-type p53 (EC50s = 400-3,700 nM), with the p53 mutant cell lines being the most sensitive. In vivo, SCH 529074 reduces tumor growth in a DLD-1 human colorectal cancer xenograft model in mice in a dose-dependent manner.  

     

    Brand:
    Cayman
    SKU:21552 -

    Out of stock

  • SCH 529074 is a small molecule activator of p53, a tumor suppressor that is mutated or non-functional in 50% of human tumors.{41050} SCH 529074 restores DNA binding activity and increases DNA binding affinity of two recombinant GST fusion mutant p53 DNA binding domains (R273H and R249S) in an electrophoretic mobility shift assay with Kd values of 0.6740 and 0.4313, respectively. It also stimulates DNA binding activity and prevents human double minute-2 (Hdm-2) ubiquitination of wild-type p53 in vitro. SCH 29074 reduces proliferation of tumor cell lines with mutant and wild-type p53 (EC50s = 400-3,700 nM), with the p53 mutant cell lines being the most sensitive. In vivo, SCH 529074 reduces tumor growth in a DLD-1 human colorectal cancer xenograft model in mice in a dose-dependent manner.  

     

    Brand:
    Cayman
    SKU:21552 -

    Out of stock

  • SCH 529074 is a small molecule activator of p53, a tumor suppressor that is mutated or non-functional in 50% of human tumors.{41050} SCH 529074 restores DNA binding activity and increases DNA binding affinity of two recombinant GST fusion mutant p53 DNA binding domains (R273H and R249S) in an electrophoretic mobility shift assay with Kd values of 0.6740 and 0.4313, respectively. It also stimulates DNA binding activity and prevents human double minute-2 (Hdm-2) ubiquitination of wild-type p53 in vitro. SCH 29074 reduces proliferation of tumor cell lines with mutant and wild-type p53 (EC50s = 400-3,700 nM), with the p53 mutant cell lines being the most sensitive. In vivo, SCH 529074 reduces tumor growth in a DLD-1 human colorectal cancer xenograft model in mice in a dose-dependent manner.  

     

    Brand:
    Cayman
    SKU:21552 -

    Out of stock

  • SCH 529074 is a small molecule activator of p53, a tumor suppressor that is mutated or non-functional in 50% of human tumors.{41050} SCH 529074 restores DNA binding activity and increases DNA binding affinity of two recombinant GST fusion mutant p53 DNA binding domains (R273H and R249S) in an electrophoretic mobility shift assay with Kd values of 0.6740 and 0.4313, respectively. It also stimulates DNA binding activity and prevents human double minute-2 (Hdm-2) ubiquitination of wild-type p53 in vitro. SCH 29074 reduces proliferation of tumor cell lines with mutant and wild-type p53 (EC50s = 400-3,700 nM), with the p53 mutant cell lines being the most sensitive. In vivo, SCH 529074 reduces tumor growth in a DLD-1 human colorectal cancer xenograft model in mice in a dose-dependent manner.  

     

    Brand:
    Cayman
    SKU:21552 -

    Out of stock

  • SCH 58261 is a competitive antagonist of the adenosine A2A receptor (Kis = 2.3 and 2.0 nM in rat and bovine brain, respectively).{32363} It is selective for the A2A subtype, displaying an A1/A2A selectivity ratio of 50-100-fold and does not interact with A2B or A3 receptors.{32363} SCH 58261 has been used to improve 6-hydroxy dopamine-induced motor deficits in a rat model of Parkinson’s disease.{32362}  

     

    Brand:
    Cayman
    SKU:19676 -

    Available on backorder

  • SCH 58261 is a competitive antagonist of the adenosine A2A receptor (Kis = 2.3 and 2.0 nM in rat and bovine brain, respectively).{32363} It is selective for the A2A subtype, displaying an A1/A2A selectivity ratio of 50-100-fold and does not interact with A2B or A3 receptors.{32363} SCH 58261 has been used to improve 6-hydroxy dopamine-induced motor deficits in a rat model of Parkinson’s disease.{32362}  

     

    Brand:
    Cayman
    SKU:19676 -

    Available on backorder

  • SCH 58261 is a competitive antagonist of the adenosine A2A receptor (Kis = 2.3 and 2.0 nM in rat and bovine brain, respectively).{32363} It is selective for the A2A subtype, displaying an A1/A2A selectivity ratio of 50-100-fold and does not interact with A2B or A3 receptors.{32363} SCH 58261 has been used to improve 6-hydroxy dopamine-induced motor deficits in a rat model of Parkinson’s disease.{32362}  

     

    Brand:
    Cayman
    SKU:19676 -

    Available on backorder

  • SCH 58261 is a competitive antagonist of the adenosine A2A receptor (Kis = 2.3 and 2.0 nM in rat and bovine brain, respectively).{32363} It is selective for the A2A subtype, displaying an A1/A2A selectivity ratio of 50-100-fold and does not interact with A2B or A3 receptors.{32363} SCH 58261 has been used to improve 6-hydroxy dopamine-induced motor deficits in a rat model of Parkinson’s disease.{32362}  

     

    Brand:
    Cayman
    SKU:19676 -

    Available on backorder

  • SCH 60057 is a fungal metabolite that has been found in Acremonium and a neurokinin receptor (NK) antagonist (IC50s = 6 and 12 µM for NK1 and NK2, respectively).{53566}  

     

    Brand:
    Cayman
    SKU:29239 - 1 mg

    Available on backorder

  • SCH 725674 is an antifungal macrolide originally isolated from Aspergillus.{45036} It inhibits the growth of S. cerevisiae and C. albicans in vitro (MICs = 8 and 32 μg/ml, respectively).  

     

    Brand:
    Cayman
    SKU:25743 - 1 mg

    Available on backorder

  • SCH 725674 is an antifungal macrolide originally isolated from Aspergillus.{45036} It inhibits the growth of S. cerevisiae and C. albicans in vitro (MICs = 8 and 32 μg/ml, respectively).  

     

    Brand:
    Cayman
    SKU:25743 - 5 mg

    Available on backorder

  • The extracellular regulated kinases 1 and 2 (ERK1/2) are functionally redundant kinases activated by a variety of growth factors and mitogens.{17806} SCH 772984 is a potent inhibitor of ERK1 and ERK2 (IC50s = 4 and 1 nM, respectively).{30913} It is highly selective, with only seven kinases of 300 tested showing more than 50% inhibition at a concentration of 1 µM. SCH 772984 has nanomolar cytotoxicity in tumor cells with mutations in BRAF, NRAS, or KRAS.{30913} It is effective in vivo, inducing regression of xenograft tumors in mice. SCH 772984 displays slow binding kinetics, binding to a novel binding pocket in inactive ERK isoforms.{30912}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • The extracellular regulated kinases 1 and 2 (ERK1/2) are functionally redundant kinases activated by a variety of growth factors and mitogens.{17806} SCH 772984 is a potent inhibitor of ERK1 and ERK2 (IC50s = 4 and 1 nM, respectively).{30913} It is highly selective, with only seven kinases of 300 tested showing more than 50% inhibition at a concentration of 1 µM. SCH 772984 has nanomolar cytotoxicity in tumor cells with mutations in BRAF, NRAS, or KRAS.{30913} It is effective in vivo, inducing regression of xenograft tumors in mice. SCH 772984 displays slow binding kinetics, binding to a novel binding pocket in inactive ERK isoforms.{30912}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • The extracellular regulated kinases 1 and 2 (ERK1/2) are functionally redundant kinases activated by a variety of growth factors and mitogens.{17806} SCH 772984 is a potent inhibitor of ERK1 and ERK2 (IC50s = 4 and 1 nM, respectively).{30913} It is highly selective, with only seven kinases of 300 tested showing more than 50% inhibition at a concentration of 1 µM. SCH 772984 has nanomolar cytotoxicity in tumor cells with mutations in BRAF, NRAS, or KRAS.{30913} It is effective in vivo, inducing regression of xenograft tumors in mice. SCH 772984 displays slow binding kinetics, binding to a novel binding pocket in inactive ERK isoforms.{30912}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • SCH 79797 is a non-peptide antagonist of proteinase-activated receptor 1 (PAR1).{23247} It blocks binding of the high affinity thrombin receptor-activating peptide (haTRAP) (IC50 = 70 nM) as well as platelet aggregation induced by either haTRAP or α-thrombin (IC50 = 0.3 and 3 µM, respectively).{23246} SCH 79797 has no activity against PAR2, PAR4, or other receptors involved in platelet activation.{23246} It also blocks PAR1 activation on vascular smooth muscle cells and endothelial cells.{23246,23245}  

     

    Brand:
    Cayman
    SKU:-
  • SCH 79797 is a non-peptide antagonist of proteinase-activated receptor 1 (PAR1).{23247} It blocks binding of the high affinity thrombin receptor-activating peptide (haTRAP) (IC50 = 70 nM) as well as platelet aggregation induced by either haTRAP or α-thrombin (IC50 = 0.3 and 3 µM, respectively).{23246} SCH 79797 has no activity against PAR2, PAR4, or other receptors involved in platelet activation.{23246} It also blocks PAR1 activation on vascular smooth muscle cells and endothelial cells.{23246,23245}  

     

    Brand:
    Cayman
    SKU:-
  • SCH 79797 is a non-peptide antagonist of proteinase-activated receptor 1 (PAR1).{23247} It blocks binding of the high affinity thrombin receptor-activating peptide (haTRAP) (IC50 = 70 nM) as well as platelet aggregation induced by either haTRAP or α-thrombin (IC50 = 0.3 and 3 µM, respectively).{23246} SCH 79797 has no activity against PAR2, PAR4, or other receptors involved in platelet activation.{23246} It also blocks PAR1 activation on vascular smooth muscle cells and endothelial cells.{23246,23245}  

     

    Brand:
    Cayman
    SKU:-
  • Checkpoint kinase 1 (Chk1) regulates S and G2-M phase cell cycle checkpoints in response to DNA damage. SCH 900776 is a functionally selective inhibitor of Chk1 (Kd = 2 nM; IC50 = 3 nM).{29242} In comparison, 18-fold and 500-fold higher concentrations of this compound are required to inhibit CDK2 and Chk2.{29242} At 5-50 mg/kg, SCH 900776 dose-dependently interacts synergistically with DNA antimetabolite agents in vitro and in vivo to selectively induce double-strand DNA breaks and cell death in tumor cells.{29242}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Checkpoint kinase 1 (Chk1) regulates S and G2-M phase cell cycle checkpoints in response to DNA damage. SCH 900776 is a functionally selective inhibitor of Chk1 (Kd = 2 nM; IC50 = 3 nM).{29242} In comparison, 18-fold and 500-fold higher concentrations of this compound are required to inhibit CDK2 and Chk2.{29242} At 5-50 mg/kg, SCH 900776 dose-dependently interacts synergistically with DNA antimetabolite agents in vitro and in vivo to selectively induce double-strand DNA breaks and cell death in tumor cells.{29242}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Checkpoint kinase 1 (Chk1) regulates S and G2-M phase cell cycle checkpoints in response to DNA damage. SCH 900776 is a functionally selective inhibitor of Chk1 (Kd = 2 nM; IC50 = 3 nM).{29242} In comparison, 18-fold and 500-fold higher concentrations of this compound are required to inhibit CDK2 and Chk2.{29242} At 5-50 mg/kg, SCH 900776 dose-dependently interacts synergistically with DNA antimetabolite agents in vitro and in vivo to selectively induce double-strand DNA breaks and cell death in tumor cells.{29242}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Checkpoint kinase 1 (Chk1) regulates S and G2-M phase cell cycle checkpoints in response to DNA damage. SCH 900776 is a functionally selective inhibitor of Chk1 (Kd = 2 nM; IC50 = 3 nM).{29242} In comparison, 18-fold and 500-fold higher concentrations of this compound are required to inhibit CDK2 and Chk2.{29242} At 5-50 mg/kg, SCH 900776 dose-dependently interacts synergistically with DNA antimetabolite agents in vitro and in vivo to selectively induce double-strand DNA breaks and cell death in tumor cells.{29242}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Schaftoside is a flavonoid C-glycoside that has been found in C. annum and has diverse biological activities including antioxidant, anti-inflammatory, and anthelmintic properties.{48469,48470,48471} It inhibits xanthine oxidase with an IC50 value of 51.4 μM and has antioxidant activity in a β-carotene-linoleic acid bleaching assay (IC50 = 46.3 μM).{48469} Schaftoside (400 μg/kg) inhibits neutrophil influx into mouse lung by 62% in a model of airway inflammation induced by aerosol administration of LPS.{48470} Schaftoside is also active against the root-knot nematode (M. incognita) with an LC50 value of 114.66 μg/ml.{48471}  

     

    Brand:
    Cayman
    SKU:27950 - 1 mg

    Available on backorder

  • Schaftoside is a flavonoid C-glycoside that has been found in C. annum and has diverse biological activities including antioxidant, anti-inflammatory, and anthelmintic properties.{48469,48470,48471} It inhibits xanthine oxidase with an IC50 value of 51.4 μM and has antioxidant activity in a β-carotene-linoleic acid bleaching assay (IC50 = 46.3 μM).{48469} Schaftoside (400 μg/kg) inhibits neutrophil influx into mouse lung by 62% in a model of airway inflammation induced by aerosol administration of LPS.{48470} Schaftoside is also active against the root-knot nematode (M. incognita) with an LC50 value of 114.66 μg/ml.{48471}  

     

    Brand:
    Cayman
    SKU:27950 - 10 mg

    Available on backorder

  • Schaftoside is a flavonoid C-glycoside that has been found in C. annum and has diverse biological activities including antioxidant, anti-inflammatory, and anthelmintic properties.{48469,48470,48471} It inhibits xanthine oxidase with an IC50 value of 51.4 μM and has antioxidant activity in a β-carotene-linoleic acid bleaching assay (IC50 = 46.3 μM).{48469} Schaftoside (400 μg/kg) inhibits neutrophil influx into mouse lung by 62% in a model of airway inflammation induced by aerosol administration of LPS.{48470} Schaftoside is also active against the root-knot nematode (M. incognita) with an LC50 value of 114.66 μg/ml.{48471}  

     

    Brand:
    Cayman
    SKU:27950 - 25 mg

    Available on backorder

  • Schaftoside is a flavonoid C-glycoside that has been found in C. annum and has diverse biological activities including antioxidant, anti-inflammatory, and anthelmintic properties.{48469,48470,48471} It inhibits xanthine oxidase with an IC50 value of 51.4 μM and has antioxidant activity in a β-carotene-linoleic acid bleaching assay (IC50 = 46.3 μM).{48469} Schaftoside (400 μg/kg) inhibits neutrophil influx into mouse lung by 62% in a model of airway inflammation induced by aerosol administration of LPS.{48470} Schaftoside is also active against the root-knot nematode (M. incognita) with an LC50 value of 114.66 μg/ml.{48471}  

     

    Brand:
    Cayman
    SKU:27950 - 5 mg

    Available on backorder

  • Schisandrin A is a lignan that has been found in Schisandra and has diverse biological activities.{31774,31773,53949,53950} It binds to adiponectin receptor 2 (IC50 = 3.2 µM).{31774} Schisandrin A (10, 20, and 50 µM) reduces LPS-induced production of nitric oxide (NO), IL-6, and TNF-α and apoptosis in primary mouse microglial cells.{31773} It reverses P-glycoprotein-mediated doxorubicin resistance in MCF-7/dox cells when used at a concentration of 20 µM.{53949} Schisandrin A (4, 12, and 36 mg/kg) reverses short-term and spatial memory deficits, as well as decreases in cerebral superoxide dismutase (SOD) and glutathione peroxidase (GPX) activities induced by amyloid β (1-42) (Aβ42; Item No. 20574) in a mouse model of Alzheimer’s disease.{53950}  

     

    Brand:
    Cayman
    SKU:19849 -

    Available on backorder

  • Schisandrin A is a lignan that has been found in Schisandra and has diverse biological activities.{31774,31773,53949,53950} It binds to adiponectin receptor 2 (IC50 = 3.2 µM).{31774} Schisandrin A (10, 20, and 50 µM) reduces LPS-induced production of nitric oxide (NO), IL-6, and TNF-α and apoptosis in primary mouse microglial cells.{31773} It reverses P-glycoprotein-mediated doxorubicin resistance in MCF-7/dox cells when used at a concentration of 20 µM.{53949} Schisandrin A (4, 12, and 36 mg/kg) reverses short-term and spatial memory deficits, as well as decreases in cerebral superoxide dismutase (SOD) and glutathione peroxidase (GPX) activities induced by amyloid β (1-42) (Aβ42; Item No. 20574) in a mouse model of Alzheimer’s disease.{53950}  

     

    Brand:
    Cayman
    SKU:19849 -

    Available on backorder

  • Schisandrin A is a lignan that has been found in Schisandra and has diverse biological activities.{31774,31773,53949,53950} It binds to adiponectin receptor 2 (IC50 = 3.2 µM).{31774} Schisandrin A (10, 20, and 50 µM) reduces LPS-induced production of nitric oxide (NO), IL-6, and TNF-α and apoptosis in primary mouse microglial cells.{31773} It reverses P-glycoprotein-mediated doxorubicin resistance in MCF-7/dox cells when used at a concentration of 20 µM.{53949} Schisandrin A (4, 12, and 36 mg/kg) reverses short-term and spatial memory deficits, as well as decreases in cerebral superoxide dismutase (SOD) and glutathione peroxidase (GPX) activities induced by amyloid β (1-42) (Aβ42; Item No. 20574) in a mouse model of Alzheimer’s disease.{53950}  

     

    Brand:
    Cayman
    SKU:19849 -

    Available on backorder

  • Schisandrin A is a lignan that has been found in Schisandra and has diverse biological activities.{31774,31773,53949,53950} It binds to adiponectin receptor 2 (IC50 = 3.2 µM).{31774} Schisandrin A (10, 20, and 50 µM) reduces LPS-induced production of nitric oxide (NO), IL-6, and TNF-α and apoptosis in primary mouse microglial cells.{31773} It reverses P-glycoprotein-mediated doxorubicin resistance in MCF-7/dox cells when used at a concentration of 20 µM.{53949} Schisandrin A (4, 12, and 36 mg/kg) reverses short-term and spatial memory deficits, as well as decreases in cerebral superoxide dismutase (SOD) and glutathione peroxidase (GPX) activities induced by amyloid β (1-42) (Aβ42; Item No. 20574) in a mouse model of Alzheimer’s disease.{53950}  

     

    Brand:
    Cayman
    SKU:19849 -

    Available on backorder

  • Schisandrin C is a lignan originally isolated from Schizandrae that has diverse biological activities.{30124,35736,47582,47583,47584} It decreases viability of U937 cells in a concentration-dependent manner and induces cell cycle arrest at the G1 phase when used at a concentration of 100 μM.{35736} Schisandrin C (5-20 μM) decreases hydrogen peroxide-induced cell death and production of reactive oxygen species (ROS) in C2C12 skeletal muscle cells.{47582} It also decreases levels of matrix metalloproteinase-2 (MMP-2), MMP-9, COX-2, VCAM-1, IL-1β, and TNF-α in hydrogen peroxide-stimulated C2C12 cells. Schisandrin C decreases lipoteichoic acid-induced production of nitric oxide (NO), prostaglandin E2 (PGE2; Item No. 14010), TNF-α, IL-1β, and IL-6 in mouse primary microglia.{47583} In vivo, schisandrin C (200 mg/kg) decreases serum alanine amino transferase (ALT) and aspartate amino transferase (AST) activity, increases hepatic mitochondrial and total glutathione (GSH) levels, and reduces liver injury in a mouse model of acetaminophen-induced liver injury partially via inhibition of the cytochrome P450 (CYP) isoforms CYP2E1, CYP1A2, and CYP3A11.{47584}  

     

    Brand:
    Cayman
    SKU:27475 - 1 mg

    Available on backorder

  • Schisandrin C is a lignan originally isolated from Schizandrae that has diverse biological activities.{30124,35736,47582,47583,47584} It decreases viability of U937 cells in a concentration-dependent manner and induces cell cycle arrest at the G1 phase when used at a concentration of 100 μM.{35736} Schisandrin C (5-20 μM) decreases hydrogen peroxide-induced cell death and production of reactive oxygen species (ROS) in C2C12 skeletal muscle cells.{47582} It also decreases levels of matrix metalloproteinase-2 (MMP-2), MMP-9, COX-2, VCAM-1, IL-1β, and TNF-α in hydrogen peroxide-stimulated C2C12 cells. Schisandrin C decreases lipoteichoic acid-induced production of nitric oxide (NO), prostaglandin E2 (PGE2; Item No. 14010), TNF-α, IL-1β, and IL-6 in mouse primary microglia.{47583} In vivo, schisandrin C (200 mg/kg) decreases serum alanine amino transferase (ALT) and aspartate amino transferase (AST) activity, increases hepatic mitochondrial and total glutathione (GSH) levels, and reduces liver injury in a mouse model of acetaminophen-induced liver injury partially via inhibition of the cytochrome P450 (CYP) isoforms CYP2E1, CYP1A2, and CYP3A11.{47584}  

     

    Brand:
    Cayman
    SKU:27475 - 10 mg

    Available on backorder

  • Schisandrin C is a lignan originally isolated from Schizandrae that has diverse biological activities.{30124,35736,47582,47583,47584} It decreases viability of U937 cells in a concentration-dependent manner and induces cell cycle arrest at the G1 phase when used at a concentration of 100 μM.{35736} Schisandrin C (5-20 μM) decreases hydrogen peroxide-induced cell death and production of reactive oxygen species (ROS) in C2C12 skeletal muscle cells.{47582} It also decreases levels of matrix metalloproteinase-2 (MMP-2), MMP-9, COX-2, VCAM-1, IL-1β, and TNF-α in hydrogen peroxide-stimulated C2C12 cells. Schisandrin C decreases lipoteichoic acid-induced production of nitric oxide (NO), prostaglandin E2 (PGE2; Item No. 14010), TNF-α, IL-1β, and IL-6 in mouse primary microglia.{47583} In vivo, schisandrin C (200 mg/kg) decreases serum alanine amino transferase (ALT) and aspartate amino transferase (AST) activity, increases hepatic mitochondrial and total glutathione (GSH) levels, and reduces liver injury in a mouse model of acetaminophen-induced liver injury partially via inhibition of the cytochrome P450 (CYP) isoforms CYP2E1, CYP1A2, and CYP3A11.{47584}  

     

    Brand:
    Cayman
    SKU:27475 - 25 mg

    Available on backorder

  • Schisandrin C is a lignan originally isolated from Schizandrae that has diverse biological activities.{30124,35736,47582,47583,47584} It decreases viability of U937 cells in a concentration-dependent manner and induces cell cycle arrest at the G1 phase when used at a concentration of 100 μM.{35736} Schisandrin C (5-20 μM) decreases hydrogen peroxide-induced cell death and production of reactive oxygen species (ROS) in C2C12 skeletal muscle cells.{47582} It also decreases levels of matrix metalloproteinase-2 (MMP-2), MMP-9, COX-2, VCAM-1, IL-1β, and TNF-α in hydrogen peroxide-stimulated C2C12 cells. Schisandrin C decreases lipoteichoic acid-induced production of nitric oxide (NO), prostaglandin E2 (PGE2; Item No. 14010), TNF-α, IL-1β, and IL-6 in mouse primary microglia.{47583} In vivo, schisandrin C (200 mg/kg) decreases serum alanine amino transferase (ALT) and aspartate amino transferase (AST) activity, increases hepatic mitochondrial and total glutathione (GSH) levels, and reduces liver injury in a mouse model of acetaminophen-induced liver injury partially via inhibition of the cytochrome P450 (CYP) isoforms CYP2E1, CYP1A2, and CYP3A11.{47584}  

     

    Brand:
    Cayman
    SKU:27475 - 5 mg

    Available on backorder

  • Schisandrol B is a lignan originally isolated from S. chinensis that has hepatoprotective activity.{43493} It increases the expression of pregnane X receptor (PXR) target genes involved in bile acid metabolism, including Cyp3a11, Ugt1a1, Oatp2, and Mrp3 in mouse liver and CYP3A4, UGT1A1, and OATP2 in HEK293T cells.{43494} It also protects against lithocholic acid-induced hepatic necrosis and intrahepatic cholestasis in wild-type, but not Pxr-null, mice and decreases mortality in a mouse model of cholestasis when administered at a dose of 100 mg/kg twice per day. It also promotes liver regeneration following partial hepatectomy and protects against hepatotoxicity induced by acetaminophen (Item No. 10024).{43496,43495}  

     

    Brand:
    Cayman
    SKU:25149 - 1 mg

    Available on backorder

  • Schisandrol B is a lignan originally isolated from S. chinensis that has hepatoprotective activity.{43493} It increases the expression of pregnane X receptor (PXR) target genes involved in bile acid metabolism, including Cyp3a11, Ugt1a1, Oatp2, and Mrp3 in mouse liver and CYP3A4, UGT1A1, and OATP2 in HEK293T cells.{43494} It also protects against lithocholic acid-induced hepatic necrosis and intrahepatic cholestasis in wild-type, but not Pxr-null, mice and decreases mortality in a mouse model of cholestasis when administered at a dose of 100 mg/kg twice per day. It also promotes liver regeneration following partial hepatectomy and protects against hepatotoxicity induced by acetaminophen (Item No. 10024).{43496,43495}  

     

    Brand:
    Cayman
    SKU:25149 - 10 mg

    Available on backorder

  • Schisandrol B is a lignan originally isolated from S. chinensis that has hepatoprotective activity.{43493} It increases the expression of pregnane X receptor (PXR) target genes involved in bile acid metabolism, including Cyp3a11, Ugt1a1, Oatp2, and Mrp3 in mouse liver and CYP3A4, UGT1A1, and OATP2 in HEK293T cells.{43494} It also protects against lithocholic acid-induced hepatic necrosis and intrahepatic cholestasis in wild-type, but not Pxr-null, mice and decreases mortality in a mouse model of cholestasis when administered at a dose of 100 mg/kg twice per day. It also promotes liver regeneration following partial hepatectomy and protects against hepatotoxicity induced by acetaminophen (Item No. 10024).{43496,43495}  

     

    Brand:
    Cayman
    SKU:25149 - 25 mg

    Available on backorder

  • Schisandrol B is a lignan originally isolated from S. chinensis that has hepatoprotective activity.{43493} It increases the expression of pregnane X receptor (PXR) target genes involved in bile acid metabolism, including Cyp3a11, Ugt1a1, Oatp2, and Mrp3 in mouse liver and CYP3A4, UGT1A1, and OATP2 in HEK293T cells.{43494} It also protects against lithocholic acid-induced hepatic necrosis and intrahepatic cholestasis in wild-type, but not Pxr-null, mice and decreases mortality in a mouse model of cholestasis when administered at a dose of 100 mg/kg twice per day. It also promotes liver regeneration following partial hepatectomy and protects against hepatotoxicity induced by acetaminophen (Item No. 10024).{43496,43495}  

     

    Brand:
    Cayman
    SKU:25149 - 5 mg

    Available on backorder

  • Schisanhenol is a debenzocyclooctene lignan that has been found in Schisandraceae and has diverse biological activities.{54063,54064,54065,54066} It completely inhibits iron and cysteine-induced malondialdehyde (MDA) formation in rat liver microsomes when used at a concentration of 1 mM.{54063} Schisanhenol reduces HIV-1 viral titers in H9 T cells (EC50 = 5.7 µM).{54064} Schisanhenol is protective against tobacco mosaic virus (TMV) infection in N. glutinosa when applied to leaves at concentrations ranging from 0.15 to 0.5 mM.{54065} Schisanhenol (10, 30, or 100 mg/kg, i.p.) prevents scopolamine-induced increases in hippocampal MDA and acetylcholinesterase (AChE) levels and decreases hippocampal superoxide dismutase (SOD) and glutathione peroxidase (GPX) activities, as well as increases time spent in the target quadrant in the Morris water maze in mice.{54066}  

     

    Brand:
    Cayman
    SKU:30109 - 1 mg

    Available on backorder

  • Schisanhenol is a debenzocyclooctene lignan that has been found in Schisandraceae and has diverse biological activities.{54063,54064,54065,54066} It completely inhibits iron and cysteine-induced malondialdehyde (MDA) formation in rat liver microsomes when used at a concentration of 1 mM.{54063} Schisanhenol reduces HIV-1 viral titers in H9 T cells (EC50 = 5.7 µM).{54064} Schisanhenol is protective against tobacco mosaic virus (TMV) infection in N. glutinosa when applied to leaves at concentrations ranging from 0.15 to 0.5 mM.{54065} Schisanhenol (10, 30, or 100 mg/kg, i.p.) prevents scopolamine-induced increases in hippocampal MDA and acetylcholinesterase (AChE) levels and decreases hippocampal superoxide dismutase (SOD) and glutathione peroxidase (GPX) activities, as well as increases time spent in the target quadrant in the Morris water maze in mice.{54066}  

     

    Brand:
    Cayman
    SKU:30109 - 10 mg

    Available on backorder

  • Schisanhenol is a debenzocyclooctene lignan that has been found in Schisandraceae and has diverse biological activities.{54063,54064,54065,54066} It completely inhibits iron and cysteine-induced malondialdehyde (MDA) formation in rat liver microsomes when used at a concentration of 1 mM.{54063} Schisanhenol reduces HIV-1 viral titers in H9 T cells (EC50 = 5.7 µM).{54064} Schisanhenol is protective against tobacco mosaic virus (TMV) infection in N. glutinosa when applied to leaves at concentrations ranging from 0.15 to 0.5 mM.{54065} Schisanhenol (10, 30, or 100 mg/kg, i.p.) prevents scopolamine-induced increases in hippocampal MDA and acetylcholinesterase (AChE) levels and decreases hippocampal superoxide dismutase (SOD) and glutathione peroxidase (GPX) activities, as well as increases time spent in the target quadrant in the Morris water maze in mice.{54066}  

     

    Brand:
    Cayman
    SKU:30109 - 25 mg

    Available on backorder

  • Schisanhenol is a debenzocyclooctene lignan that has been found in Schisandraceae and has diverse biological activities.{54063,54064,54065,54066} It completely inhibits iron and cysteine-induced malondialdehyde (MDA) formation in rat liver microsomes when used at a concentration of 1 mM.{54063} Schisanhenol reduces HIV-1 viral titers in H9 T cells (EC50 = 5.7 µM).{54064} Schisanhenol is protective against tobacco mosaic virus (TMV) infection in N. glutinosa when applied to leaves at concentrations ranging from 0.15 to 0.5 mM.{54065} Schisanhenol (10, 30, or 100 mg/kg, i.p.) prevents scopolamine-induced increases in hippocampal MDA and acetylcholinesterase (AChE) levels and decreases hippocampal superoxide dismutase (SOD) and glutathione peroxidase (GPX) activities, as well as increases time spent in the target quadrant in the Morris water maze in mice.{54066}  

     

    Brand:
    Cayman
    SKU:30109 - 5 mg

    Available on backorder

  • Schisantherin B (STB) is a lignan originally isolated from S. sphenanthera fruit.{47351} It inhibits formation of advanced glycation end products (AGEs) in vitro.{47352} STB (0.1 mg/kg) decreases escape latency in the Morris water maze and increases spontaneous alternation in the Y-maze in a mouse model of Alzheimer’s disease induced by amyloid-β (1-42) (Item No. 20574).{47353} It increases glial expression of glutamate transporter 1 (GLP-1) and decreases immobility time in the forced swim test (FST) in mice, indicating antidepressant-like activity.{47354} STB also increases spontaneous alternation in the Y-maze in a mouse model of stress-induced short-term learning impairment induced by the FST.  

     

    Brand:
    Cayman
    SKU:26716 - 10 mg

    Available on backorder

  • Schisantherin B (STB) is a lignan originally isolated from S. sphenanthera fruit.{47351} It inhibits formation of advanced glycation end products (AGEs) in vitro.{47352} STB (0.1 mg/kg) decreases escape latency in the Morris water maze and increases spontaneous alternation in the Y-maze in a mouse model of Alzheimer’s disease induced by amyloid-β (1-42) (Item No. 20574).{47353} It increases glial expression of glutamate transporter 1 (GLP-1) and decreases immobility time in the forced swim test (FST) in mice, indicating antidepressant-like activity.{47354} STB also increases spontaneous alternation in the Y-maze in a mouse model of stress-induced short-term learning impairment induced by the FST.  

     

    Brand:
    Cayman
    SKU:26716 - 25 mg

    Available on backorder

  • Schisantherin B (STB) is a lignan originally isolated from S. sphenanthera fruit.{47351} It inhibits formation of advanced glycation end products (AGEs) in vitro.{47352} STB (0.1 mg/kg) decreases escape latency in the Morris water maze and increases spontaneous alternation in the Y-maze in a mouse model of Alzheimer’s disease induced by amyloid-β (1-42) (Item No. 20574).{47353} It increases glial expression of glutamate transporter 1 (GLP-1) and decreases immobility time in the forced swim test (FST) in mice, indicating antidepressant-like activity.{47354} STB also increases spontaneous alternation in the Y-maze in a mouse model of stress-induced short-term learning impairment induced by the FST.  

     

    Brand:
    Cayman
    SKU:26716 - 5 mg

    Available on backorder

  • Schisantherin B (STB) is a lignan originally isolated from S. sphenanthera fruit.{47351} It inhibits formation of advanced glycation end products (AGEs) in vitro.{47352} STB (0.1 mg/kg) decreases escape latency in the Morris water maze and increases spontaneous alternation in the Y-maze in a mouse model of Alzheimer’s disease induced by amyloid-β (1-42) (Item No. 20574).{47353} It increases glial expression of glutamate transporter 1 (GLP-1) and decreases immobility time in the forced swim test (FST) in mice, indicating antidepressant-like activity.{47354} STB also increases spontaneous alternation in the Y-maze in a mouse model of stress-induced short-term learning impairment induced by the FST.  

     

    Brand:
    Cayman
    SKU:26716 - 50 mg

    Available on backorder

  • Schizandrin is a dibenzocyclooctadiene lignan and a major component of S. chinensis and has diverse biological activities.{48362,48363,48364,48365,48366} It induces cell cycle arrest at the G0/G1 phase and inhibits growth of T47D and MDA-MB-231 breast cancer cells when used at a concentration of 100 μM.{48362} Schizandrin (10 and 100 μM) prevents glutamate-induced cytotoxicity, inhibits production of nitric oxide (NO) and reactive oxygen species (ROS), and preserves the mitochondrial membrane potential in isolated rat cortical cells.{48363} It reduces apoptosis induced by cisplatin (Item No. 13119) in HK-2 human kidney cells.{48364} In vivo, schizandrin (1 and 10 mg/kg, p.o.) reverses scopolamine-induced impairment of spatial memory and the passive avoidance response in rats.{48365} It enhances oxotremorine-induced tremors in mice. Schizandrin (10 mg/kg) reduces serum levels of IgE, IgG1, IL-4, and IFN-γ in an ovalbumin-sensitized mouse model of allergy.{48366}  

     

    Brand:
    Cayman
    SKU:27211 - 10 mg

    Available on backorder

  • Schizandrin is a dibenzocyclooctadiene lignan and a major component of S. chinensis and has diverse biological activities.{48362,48363,48364,48365,48366} It induces cell cycle arrest at the G0/G1 phase and inhibits growth of T47D and MDA-MB-231 breast cancer cells when used at a concentration of 100 μM.{48362} Schizandrin (10 and 100 μM) prevents glutamate-induced cytotoxicity, inhibits production of nitric oxide (NO) and reactive oxygen species (ROS), and preserves the mitochondrial membrane potential in isolated rat cortical cells.{48363} It reduces apoptosis induced by cisplatin (Item No. 13119) in HK-2 human kidney cells.{48364} In vivo, schizandrin (1 and 10 mg/kg, p.o.) reverses scopolamine-induced impairment of spatial memory and the passive avoidance response in rats.{48365} It enhances oxotremorine-induced tremors in mice. Schizandrin (10 mg/kg) reduces serum levels of IgE, IgG1, IL-4, and IFN-γ in an ovalbumin-sensitized mouse model of allergy.{48366}  

     

    Brand:
    Cayman
    SKU:27211 - 100 mg

    Available on backorder

  • Schizandrin is a dibenzocyclooctadiene lignan and a major component of S. chinensis and has diverse biological activities.{48362,48363,48364,48365,48366} It induces cell cycle arrest at the G0/G1 phase and inhibits growth of T47D and MDA-MB-231 breast cancer cells when used at a concentration of 100 μM.{48362} Schizandrin (10 and 100 μM) prevents glutamate-induced cytotoxicity, inhibits production of nitric oxide (NO) and reactive oxygen species (ROS), and preserves the mitochondrial membrane potential in isolated rat cortical cells.{48363} It reduces apoptosis induced by cisplatin (Item No. 13119) in HK-2 human kidney cells.{48364} In vivo, schizandrin (1 and 10 mg/kg, p.o.) reverses scopolamine-induced impairment of spatial memory and the passive avoidance response in rats.{48365} It enhances oxotremorine-induced tremors in mice. Schizandrin (10 mg/kg) reduces serum levels of IgE, IgG1, IL-4, and IFN-γ in an ovalbumin-sensitized mouse model of allergy.{48366}  

     

    Brand:
    Cayman
    SKU:27211 - 250 mg

    Available on backorder

  • Schizandrin is a dibenzocyclooctadiene lignan and a major component of S. chinensis and has diverse biological activities.{48362,48363,48364,48365,48366} It induces cell cycle arrest at the G0/G1 phase and inhibits growth of T47D and MDA-MB-231 breast cancer cells when used at a concentration of 100 μM.{48362} Schizandrin (10 and 100 μM) prevents glutamate-induced cytotoxicity, inhibits production of nitric oxide (NO) and reactive oxygen species (ROS), and preserves the mitochondrial membrane potential in isolated rat cortical cells.{48363} It reduces apoptosis induced by cisplatin (Item No. 13119) in HK-2 human kidney cells.{48364} In vivo, schizandrin (1 and 10 mg/kg, p.o.) reverses scopolamine-induced impairment of spatial memory and the passive avoidance response in rats.{48365} It enhances oxotremorine-induced tremors in mice. Schizandrin (10 mg/kg) reduces serum levels of IgE, IgG1, IL-4, and IFN-γ in an ovalbumin-sensitized mouse model of allergy.{48366}  

     

    Brand:
    Cayman
    SKU:27211 - 50 mg

    Available on backorder

  • Schizandrin B is a dibenzocyclooctadiene that has been found in F. schisandrae and S. chinensis with diverse biological activities.{42179,42180,42181} Schizandrin B (50 μM) completely inhibits anti-CD3- and anti-CD28-induced release of the cytokines IL-2, IL-3, IL-4, IL-6, and IFN-γ in T cells.{42182} In A549 adenocarcinoma cells, schizandrin B (1-30 μM) dose-dependently reduces cell survival and UV-induced phosphorylation of p53 and checkpoint kinase 1 (Chk1).{42179} Schizandrin B reduces kinase activity of the serine/threonine-protein kinase ATR with an IC50 value of 7.25 μM for the recombinant enzyme. In vivo, schizandrin B (25-100 mg/kg, p.o.) dose-dependently inhibits lipid peroxidation, formation of DNA strand breaks, and NADPH oxidase-dependent oxygen production induced by doxorubicin (Item No. 15007) in mouse heart.{42180} It also reduces the expression of p53, 3-nitrotyrosine, phosphorylated p38 MAPK and MAPKAPK-2, and matrix metalloproteinase-2 (MMP-2) and MMP-9. Schizandrin B (1 or 2 mmol/kg per day, p.o.) pretreatment reduces tert-butylhydroperoxide-induced mortality and malondialdehyde formation and increases glutathione (GSH) levels and Se-glutathione peroxidase (GSH-Px) activity in brain in mice.{42181}  

     

    Brand:
    Cayman
    SKU:24968 - 1 mg

    Available on backorder

  • Schizandrin B is a dibenzocyclooctadiene that has been found in F. schisandrae and S. chinensis with diverse biological activities.{42179,42180,42181} Schizandrin B (50 μM) completely inhibits anti-CD3- and anti-CD28-induced release of the cytokines IL-2, IL-3, IL-4, IL-6, and IFN-γ in T cells.{42182} In A549 adenocarcinoma cells, schizandrin B (1-30 μM) dose-dependently reduces cell survival and UV-induced phosphorylation of p53 and checkpoint kinase 1 (Chk1).{42179} Schizandrin B reduces kinase activity of the serine/threonine-protein kinase ATR with an IC50 value of 7.25 μM for the recombinant enzyme. In vivo, schizandrin B (25-100 mg/kg, p.o.) dose-dependently inhibits lipid peroxidation, formation of DNA strand breaks, and NADPH oxidase-dependent oxygen production induced by doxorubicin (Item No. 15007) in mouse heart.{42180} It also reduces the expression of p53, 3-nitrotyrosine, phosphorylated p38 MAPK and MAPKAPK-2, and matrix metalloproteinase-2 (MMP-2) and MMP-9. Schizandrin B (1 or 2 mmol/kg per day, p.o.) pretreatment reduces tert-butylhydroperoxide-induced mortality and malondialdehyde formation and increases glutathione (GSH) levels and Se-glutathione peroxidase (GSH-Px) activity in brain in mice.{42181}  

     

    Brand:
    Cayman
    SKU:24968 - 10 mg

    Available on backorder

  • Schizandrin B is a dibenzocyclooctadiene that has been found in F. schisandrae and S. chinensis with diverse biological activities.{42179,42180,42181} Schizandrin B (50 μM) completely inhibits anti-CD3- and anti-CD28-induced release of the cytokines IL-2, IL-3, IL-4, IL-6, and IFN-γ in T cells.{42182} In A549 adenocarcinoma cells, schizandrin B (1-30 μM) dose-dependently reduces cell survival and UV-induced phosphorylation of p53 and checkpoint kinase 1 (Chk1).{42179} Schizandrin B reduces kinase activity of the serine/threonine-protein kinase ATR with an IC50 value of 7.25 μM for the recombinant enzyme. In vivo, schizandrin B (25-100 mg/kg, p.o.) dose-dependently inhibits lipid peroxidation, formation of DNA strand breaks, and NADPH oxidase-dependent oxygen production induced by doxorubicin (Item No. 15007) in mouse heart.{42180} It also reduces the expression of p53, 3-nitrotyrosine, phosphorylated p38 MAPK and MAPKAPK-2, and matrix metalloproteinase-2 (MMP-2) and MMP-9. Schizandrin B (1 or 2 mmol/kg per day, p.o.) pretreatment reduces tert-butylhydroperoxide-induced mortality and malondialdehyde formation and increases glutathione (GSH) levels and Se-glutathione peroxidase (GSH-Px) activity in brain in mice.{42181}  

     

    Brand:
    Cayman
    SKU:24968 - 25 mg

    Available on backorder

  • Schizandrin B is a dibenzocyclooctadiene that has been found in F. schisandrae and S. chinensis with diverse biological activities.{42179,42180,42181} Schizandrin B (50 μM) completely inhibits anti-CD3- and anti-CD28-induced release of the cytokines IL-2, IL-3, IL-4, IL-6, and IFN-γ in T cells.{42182} In A549 adenocarcinoma cells, schizandrin B (1-30 μM) dose-dependently reduces cell survival and UV-induced phosphorylation of p53 and checkpoint kinase 1 (Chk1).{42179} Schizandrin B reduces kinase activity of the serine/threonine-protein kinase ATR with an IC50 value of 7.25 μM for the recombinant enzyme. In vivo, schizandrin B (25-100 mg/kg, p.o.) dose-dependently inhibits lipid peroxidation, formation of DNA strand breaks, and NADPH oxidase-dependent oxygen production induced by doxorubicin (Item No. 15007) in mouse heart.{42180} It also reduces the expression of p53, 3-nitrotyrosine, phosphorylated p38 MAPK and MAPKAPK-2, and matrix metalloproteinase-2 (MMP-2) and MMP-9. Schizandrin B (1 or 2 mmol/kg per day, p.o.) pretreatment reduces tert-butylhydroperoxide-induced mortality and malondialdehyde formation and increases glutathione (GSH) levels and Se-glutathione peroxidase (GSH-Px) activity in brain in mice.{42181}  

     

    Brand:
    Cayman
    SKU:24968 - 5 mg

    Available on backorder

  • Sciadopitysin is a biflavonoid originally isolated from G. biloba and has diverse biological activities.{42865,42866,42867,42868} It reduces cytotoxicity induced by amyloid-β (1-42) (Aβ42; Item No. 20574) in PC12 cells (EC50 = 9.84 μM).{42866} Sciadopitysin (0.1-10 μM) decreases methylglyoxal-induced insulin secretion, production of reactive oxygen species (ROS), cardiolipin peroxidation, and cytotoxicity in RIN-m5F pancreatic β-cells.{42867} It inhibits P-glycoprotein (P-gp; IC50 = 53.42 μM) and increases cellular toxicity of paraquat and paclitaxel (Item No. 10461) in MDR1-MDCKII cells.{47468} Sciadopitysin inhibits RANKL-induced mRNA expression of the osteoclast-specific genes CTSK, TRAP, and MMP-9, activation of NF-κB, and osteoclastogenesis in a mouse model of LPS-induced bone loss.{42868}  

     

    Brand:
    Cayman
    SKU:27900 - 10 mg

    Available on backorder

  • Sciadopitysin is a biflavonoid originally isolated from G. biloba and has diverse biological activities.{42865,42866,42867,42868} It reduces cytotoxicity induced by amyloid-β (1-42) (Aβ42; Item No. 20574) in PC12 cells (EC50 = 9.84 μM).{42866} Sciadopitysin (0.1-10 μM) decreases methylglyoxal-induced insulin secretion, production of reactive oxygen species (ROS), cardiolipin peroxidation, and cytotoxicity in RIN-m5F pancreatic β-cells.{42867} It inhibits P-glycoprotein (P-gp; IC50 = 53.42 μM) and increases cellular toxicity of paraquat and paclitaxel (Item No. 10461) in MDR1-MDCKII cells.{47468} Sciadopitysin inhibits RANKL-induced mRNA expression of the osteoclast-specific genes CTSK, TRAP, and MMP-9, activation of NF-κB, and osteoclastogenesis in a mouse model of LPS-induced bone loss.{42868}  

     

    Brand:
    Cayman
    SKU:27900 - 25 mg

    Available on backorder

  • Sciadopitysin is a biflavonoid originally isolated from G. biloba and has diverse biological activities.{42865,42866,42867,42868} It reduces cytotoxicity induced by amyloid-β (1-42) (Aβ42; Item No. 20574) in PC12 cells (EC50 = 9.84 μM).{42866} Sciadopitysin (0.1-10 μM) decreases methylglyoxal-induced insulin secretion, production of reactive oxygen species (ROS), cardiolipin peroxidation, and cytotoxicity in RIN-m5F pancreatic β-cells.{42867} It inhibits P-glycoprotein (P-gp; IC50 = 53.42 μM) and increases cellular toxicity of paraquat and paclitaxel (Item No. 10461) in MDR1-MDCKII cells.{47468} Sciadopitysin inhibits RANKL-induced mRNA expression of the osteoclast-specific genes CTSK, TRAP, and MMP-9, activation of NF-κB, and osteoclastogenesis in a mouse model of LPS-induced bone loss.{42868}  

     

    Brand:
    Cayman
    SKU:27900 - 5 mg

    Available on backorder

  • Sciadopitysin is a biflavonoid originally isolated from G. biloba and has diverse biological activities.{42865,42866,42867,42868} It reduces cytotoxicity induced by amyloid-β (1-42) (Aβ42; Item No. 20574) in PC12 cells (EC50 = 9.84 μM).{42866} Sciadopitysin (0.1-10 μM) decreases methylglyoxal-induced insulin secretion, production of reactive oxygen species (ROS), cardiolipin peroxidation, and cytotoxicity in RIN-m5F pancreatic β-cells.{42867} It inhibits P-glycoprotein (P-gp; IC50 = 53.42 μM) and increases cellular toxicity of paraquat and paclitaxel (Item No. 10461) in MDR1-MDCKII cells.{47468} Sciadopitysin inhibits RANKL-induced mRNA expression of the osteoclast-specific genes CTSK, TRAP, and MMP-9, activation of NF-κB, and osteoclastogenesis in a mouse model of LPS-induced bone loss.{42868}  

     

    Brand:
    Cayman
    SKU:27900 - 50 mg

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  • SCIO 469 is a p38 MAPK inhibitor (IC50 = 9 nM for p38α).{48745} It is 10-fold selective for p38α over p38β MAPK and 2,000-fold selective over a panel of 20 additional kinases. SCIO 469 inhibits secretion of IL-6 from multiple myeloma patient-derived bone marrow stromal cells (BMSCs) in a concentration-dependent manner. It increases growth inhibition, DNA fragmentation, and caspase-8 and PARP cleavage induced by the proteasome inhibitor PS-341 (bortezomib; Item No. 10008822) in MM.1S cells when used at concentrations of 100 and 200 nM. SCIO 469 (150 and 450 mg/kg) reduces microvessel density and tumor load and increases survival in a 5T33MM murine myeloma model.{48746}  

     

    Brand:
    Cayman
    SKU:29484 - 1 mg

    Available on backorder