Chemicals
Showing 12451–12600 of 41137 results
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BVT 2733 is an inhibitor of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1; Item No. 10007815).{36817} In a mouse model of hyperglycemia and hyperinsulinemia, BVT 2733 (100 mg/kg) inhibits 11β-HSD1 activity in isolated liver and decreases blood glucose and insulin concentrations. It decreases the expression of monocyte chemoattractant protein 1 (MCP-1) and TNF-α in adipose tissue, but not plasma, of mice with high-fat diet-induced obesity and normalizes the expression of adipokines in adipose tissue.{36818} It also reduces body weight and improves glucose tolerance and insulin sensitivity in high-fat diet-induced obese mice. BVT 2733 decreases TNF-α, IL-1β, IL-6, and IL-17 protein levels in serum and reduces severity of collagen-induced arthritis in mice.{36819}
Brand:CaymanSKU:22203 -Out of stock
BVT 948 is a noncompetitive, cell-permeable inhibitor of protein tyrosine phosphatases (PTP; IC50s = 0.09-1.7 µM).{27664} It facilitates the oxidation of the catalytic cysteine residue by hydrogen peroxide.{27664} Similarly, it inhibits redox-sensitive cytochrome P450 (CYP) isoforms, including CYP2C19 and CYP2D6, with IC50 values less than 10 µM.{27664} BVT 948 also inhibits the protein methyltransferases SETD8, SETD2, G9a, SMYD2, CARM1, and PRMT3 with IC50 values from 0.7 to 3.2 µm.{26934} Presumably through its effects on PTPs, BVT 948 enhances insulin signaling in cells and insulin tolerance in ob/ob mice, suppresses the expression of matrix metalloproteinase-9 and invasion in breast cancer cells, and increases NMDA-induced substance P release by spinal cord slices.{27664,27665,27666}
Brand:CaymanSKU:-Out of stock
BVT 948 is a noncompetitive, cell-permeable inhibitor of protein tyrosine phosphatases (PTP; IC50s = 0.09-1.7 µM).{27664} It facilitates the oxidation of the catalytic cysteine residue by hydrogen peroxide.{27664} Similarly, it inhibits redox-sensitive cytochrome P450 (CYP) isoforms, including CYP2C19 and CYP2D6, with IC50 values less than 10 µM.{27664} BVT 948 also inhibits the protein methyltransferases SETD8, SETD2, G9a, SMYD2, CARM1, and PRMT3 with IC50 values from 0.7 to 3.2 µm.{26934} Presumably through its effects on PTPs, BVT 948 enhances insulin signaling in cells and insulin tolerance in ob/ob mice, suppresses the expression of matrix metalloproteinase-9 and invasion in breast cancer cells, and increases NMDA-induced substance P release by spinal cord slices.{27664,27665,27666}
Brand:CaymanSKU:-Out of stock
BVT 948 is a noncompetitive, cell-permeable inhibitor of protein tyrosine phosphatases (PTP; IC50s = 0.09-1.7 µM).{27664} It facilitates the oxidation of the catalytic cysteine residue by hydrogen peroxide.{27664} Similarly, it inhibits redox-sensitive cytochrome P450 (CYP) isoforms, including CYP2C19 and CYP2D6, with IC50 values less than 10 µM.{27664} BVT 948 also inhibits the protein methyltransferases SETD8, SETD2, G9a, SMYD2, CARM1, and PRMT3 with IC50 values from 0.7 to 3.2 µm.{26934} Presumably through its effects on PTPs, BVT 948 enhances insulin signaling in cells and insulin tolerance in ob/ob mice, suppresses the expression of matrix metalloproteinase-9 and invasion in breast cancer cells, and increases NMDA-induced substance P release by spinal cord slices.{27664,27665,27666}
Brand:CaymanSKU:-Out of stock
BVT 948 is a noncompetitive, cell-permeable inhibitor of protein tyrosine phosphatases (PTP; IC50s = 0.09-1.7 µM).{27664} It facilitates the oxidation of the catalytic cysteine residue by hydrogen peroxide.{27664} Similarly, it inhibits redox-sensitive cytochrome P450 (CYP) isoforms, including CYP2C19 and CYP2D6, with IC50 values less than 10 µM.{27664} BVT 948 also inhibits the protein methyltransferases SETD8, SETD2, G9a, SMYD2, CARM1, and PRMT3 with IC50 values from 0.7 to 3.2 µm.{26934} Presumably through its effects on PTPs, BVT 948 enhances insulin signaling in cells and insulin tolerance in ob/ob mice, suppresses the expression of matrix metalloproteinase-9 and invasion in breast cancer cells, and increases NMDA-induced substance P release by spinal cord slices.{27664,27665,27666}
Brand:CaymanSKU:-Out of stock
BW 245C is a selective agonist for the DP1 receptor.{3128,711} The Ki of BW 245C for the inhibition of [3H]-PGD2 binding to isolated human platelet membranes is 0.9 nM.{3128} It has a reported IC50 of 2.5 nM for the inhibition of ADP-induced human platelet aggregation{419} and an IC50 of 250 nM for the inhibition of rat platelet aggregation.{711}
Brand:CaymanSKU:12050 - 1 mgAvailable on backorder
BW 245C is a selective agonist for the DP1 receptor.{3128,711} The Ki of BW 245C for the inhibition of [3H]-PGD2 binding to isolated human platelet membranes is 0.9 nM.{3128} It has a reported IC50 of 2.5 nM for the inhibition of ADP-induced human platelet aggregation{419} and an IC50 of 250 nM for the inhibition of rat platelet aggregation.{711}
Brand:CaymanSKU:12050 - 10 mgAvailable on backorder
BW 245C is a selective agonist for the DP1 receptor.{3128,711} The Ki of BW 245C for the inhibition of [3H]-PGD2 binding to isolated human platelet membranes is 0.9 nM.{3128} It has a reported IC50 of 2.5 nM for the inhibition of ADP-induced human platelet aggregation{419} and an IC50 of 250 nM for the inhibition of rat platelet aggregation.{711}
Brand:CaymanSKU:12050 - 5 mgAvailable on backorder
BW 246C (Item No. 12055) is the less active C-8 diastereomer of the DP receptor agonist BW 245C.{3128,711} The activity of BW 245C is 70-fold greater than that of BW 246C.{4050}
Brand:CaymanSKU:12055 - 1 mgAvailable on backorder
BW 246C (Item No. 12055) is the less active C-8 diastereomer of the DP receptor agonist BW 245C.{3128,711} The activity of BW 245C is 70-fold greater than that of BW 246C.{4050}
Brand:CaymanSKU:12055 - 10 mgAvailable on backorder
BW 246C (Item No. 12055) is the less active C-8 diastereomer of the DP receptor agonist BW 245C.{3128,711} The activity of BW 245C is 70-fold greater than that of BW 246C.{4050}
Brand:CaymanSKU:12055 - 5 mgAvailable on backorder
The transduction of neurobehavioral effects by serotonin (5-hydroxy tryptamine; 5-HT) is mediated via at least 6 major 5-HT receptor subtypes. Non-selective 5-HT receptor agonists, such as mCPP, induce many behavioral responses in rats, including increased anxiety, hypophagia, and hypoactivity. BW 723C86 is in fact anxiolytic, and its only other prominent behavioral effect is hyperphagia.{5255} This effect is likely due to the 10-fold selectivity of BW 723C86 for the HT2B receptor.{5254} Direct infusion of 1-3 µg of BW 723C86 into the cerebral ventricles of rats evokes maximal behavioral responses; the response was attenuated at both higher and lower doses.{5254}
Brand:CaymanSKU:70090 - 1 mgAvailable on backorder
The transduction of neurobehavioral effects by serotonin (5-hydroxy tryptamine; 5-HT) is mediated via at least 6 major 5-HT receptor subtypes. Non-selective 5-HT receptor agonists, such as mCPP, induce many behavioral responses in rats, including increased anxiety, hypophagia, and hypoactivity. BW 723C86 is in fact anxiolytic, and its only other prominent behavioral effect is hyperphagia.{5255} This effect is likely due to the 10-fold selectivity of BW 723C86 for the HT2B receptor.{5254} Direct infusion of 1-3 µg of BW 723C86 into the cerebral ventricles of rats evokes maximal behavioral responses; the response was attenuated at both higher and lower doses.{5254}
Brand:CaymanSKU:70090 - 10 mgAvailable on backorder
The transduction of neurobehavioral effects by serotonin (5-hydroxy tryptamine; 5-HT) is mediated via at least 6 major 5-HT receptor subtypes. Non-selective 5-HT receptor agonists, such as mCPP, induce many behavioral responses in rats, including increased anxiety, hypophagia, and hypoactivity. BW 723C86 is in fact anxiolytic, and its only other prominent behavioral effect is hyperphagia.{5255} This effect is likely due to the 10-fold selectivity of BW 723C86 for the HT2B receptor.{5254} Direct infusion of 1-3 µg of BW 723C86 into the cerebral ventricles of rats evokes maximal behavioral responses; the response was attenuated at both higher and lower doses.{5254}
Brand:CaymanSKU:70090 - 5 mgAvailable on backorder
The transduction of neurobehavioral effects by serotonin (5-hydroxy tryptamine; 5-HT) is mediated via at least 6 major 5-HT receptor subtypes. Non-selective 5-HT receptor agonists, such as mCPP, induce many behavioral responses in rats, including increased anxiety, hypophagia, and hypoactivity. BW 723C86 is in fact anxiolytic, and its only other prominent behavioral effect is hyperphagia.{5255} This effect is likely due to the 10-fold selectivity of BW 723C86 for the HT2B receptor.{5254} Direct infusion of 1-3 µg of BW 723C86 into the cerebral ventricles of rats evokes maximal behavioral responses; the response was attenuated at both higher and lower doses.{5254}
Brand:CaymanSKU:70090 - 50 mgAvailable on backorder
BW 755C is a dual inhibitor of 5-lipoxygenase (5-LO) and cyclooxygenase (COX) pathways, inhibiting 5-LO, COX-1, and COX-2 (IC50s = 0.75 μM, 0.65 μg/ml, and 1.2 μg/ml, respectively).{25336,25335,1287} It may also inhibit other LO pathways in vivo.{67} Through these actions, BW 755C diminishes inflammation.{744,23775}
Brand:CaymanSKU:-BW 755C is a dual inhibitor of 5-lipoxygenase (5-LO) and cyclooxygenase (COX) pathways, inhibiting 5-LO, COX-1, and COX-2 (IC50s = 0.75 μM, 0.65 μg/ml, and 1.2 μg/ml, respectively).{25336,25335,1287} It may also inhibit other LO pathways in vivo.{67} Through these actions, BW 755C diminishes inflammation.{744,23775}
Brand:CaymanSKU:-BW 755C is a dual inhibitor of 5-lipoxygenase (5-LO) and cyclooxygenase (COX) pathways, inhibiting 5-LO, COX-1, and COX-2 (IC50s = 0.75 μM, 0.65 μg/ml, and 1.2 μg/ml, respectively).{25336,25335,1287} It may also inhibit other LO pathways in vivo.{67} Through these actions, BW 755C diminishes inflammation.{744,23775}
Brand:CaymanSKU:-BW 755C is a dual inhibitor of 5-lipoxygenase (5-LO) and cyclooxygenase (COX) pathways, inhibiting 5-LO, COX-1, and COX-2 (IC50s = 0.75 μM, 0.65 μg/ml, and 1.2 μg/ml, respectively).{25336,25335,1287} It may also inhibit other LO pathways in vivo.{67} Through these actions, BW 755C diminishes inflammation.{744,23775}
Brand:CaymanSKU:-BW A868C is a hydantoin compound that is structurally related to the DP receptor agonist BW 245C.{1198,3328} BW A868C antagonizes the prostaglandin D2 and BW 245C-induced activation of human platelet adenylate cyclase. It reverses the anti-aggregatory effects of DP receptor agonists in a dose-dependent manner. Likewise, BW A868C antagonizes the accumulation of cAMP in rabbit non-pigmented ciliary epithelial cells.{3804} It has virtually no effect on human TP, IP, EP1, EP2, and FP receptors. The Ki for BW A868C is approximately 1.7 nM.{1254}
Brand:CaymanSKU:12060 - 1 mgAvailable on backorder
BW A868C is a hydantoin compound that is structurally related to the DP receptor agonist BW 245C.{1198,3328} BW A868C antagonizes the prostaglandin D2 and BW 245C-induced activation of human platelet adenylate cyclase. It reverses the anti-aggregatory effects of DP receptor agonists in a dose-dependent manner. Likewise, BW A868C antagonizes the accumulation of cAMP in rabbit non-pigmented ciliary epithelial cells.{3804} It has virtually no effect on human TP, IP, EP1, EP2, and FP receptors. The Ki for BW A868C is approximately 1.7 nM.{1254}
Brand:CaymanSKU:12060 - 10 mgAvailable on backorder
BW A868C is a hydantoin compound that is structurally related to the DP receptor agonist BW 245C.{1198,3328} BW A868C antagonizes the prostaglandin D2 and BW 245C-induced activation of human platelet adenylate cyclase. It reverses the anti-aggregatory effects of DP receptor agonists in a dose-dependent manner. Likewise, BW A868C antagonizes the accumulation of cAMP in rabbit non-pigmented ciliary epithelial cells.{3804} It has virtually no effect on human TP, IP, EP1, EP2, and FP receptors. The Ki for BW A868C is approximately 1.7 nM.{1254}
Brand:CaymanSKU:12060 - 5 mgAvailable on backorder
The CC chemokine receptor-1 (CCR1), whose ligands include macrophage inflammatory protein-1α (MIP-1α), RANTES, and monocyte chemotactic protein-3 (MCP-3), has a central role in leukocyte trafficking and is highly expressed in certain autoimmune diseases. BX 471 is a nonpeptide CCR1 antagonist that has been shown to displace MIP-1α, RANTES, and MCP-3 with Ki values of 1, 2.8, and 5.5 nM, respectively.{29906} It demonstrates >10,000-fold selectivity for CCR1 over 28 additional G protein-coupled receptors, including related chemokine receptors.{29906} In a rat experimental allergic encephalomyelitis model of multiple sclerosis, BX 471 at 50 mg/kg was shown to significantly reduce the severity of the disease.{29906} BX 471 also decreases the inflammatory response during sepsis, blocks migration of monocytes isolated from rheumatoid arthritis patients, and prevents macrophage and T-cell recruitment in a mouse model of lupus nephritis.{29904,29905,29903}
Brand:CaymanSKU:-Available on backorder
The CC chemokine receptor-1 (CCR1), whose ligands include macrophage inflammatory protein-1α (MIP-1α), RANTES, and monocyte chemotactic protein-3 (MCP-3), has a central role in leukocyte trafficking and is highly expressed in certain autoimmune diseases. BX 471 is a nonpeptide CCR1 antagonist that has been shown to displace MIP-1α, RANTES, and MCP-3 with Ki values of 1, 2.8, and 5.5 nM, respectively.{29906} It demonstrates >10,000-fold selectivity for CCR1 over 28 additional G protein-coupled receptors, including related chemokine receptors.{29906} In a rat experimental allergic encephalomyelitis model of multiple sclerosis, BX 471 at 50 mg/kg was shown to significantly reduce the severity of the disease.{29906} BX 471 also decreases the inflammatory response during sepsis, blocks migration of monocytes isolated from rheumatoid arthritis patients, and prevents macrophage and T-cell recruitment in a mouse model of lupus nephritis.{29904,29905,29903}
Brand:CaymanSKU:-Available on backorder
The CC chemokine receptor-1 (CCR1), whose ligands include macrophage inflammatory protein-1α (MIP-1α), RANTES, and monocyte chemotactic protein-3 (MCP-3), has a central role in leukocyte trafficking and is highly expressed in certain autoimmune diseases. BX 471 is a nonpeptide CCR1 antagonist that has been shown to displace MIP-1α, RANTES, and MCP-3 with Ki values of 1, 2.8, and 5.5 nM, respectively.{29906} It demonstrates >10,000-fold selectivity for CCR1 over 28 additional G protein-coupled receptors, including related chemokine receptors.{29906} In a rat experimental allergic encephalomyelitis model of multiple sclerosis, BX 471 at 50 mg/kg was shown to significantly reduce the severity of the disease.{29906} BX 471 also decreases the inflammatory response during sepsis, blocks migration of monocytes isolated from rheumatoid arthritis patients, and prevents macrophage and T-cell recruitment in a mouse model of lupus nephritis.{29904,29905,29903}
Brand:CaymanSKU:-Available on backorder
The CC chemokine receptor-1 (CCR1), whose ligands include macrophage inflammatory protein-1α (MIP-1α), RANTES, and monocyte chemotactic protein-3 (MCP-3), has a central role in leukocyte trafficking and is highly expressed in certain autoimmune diseases. BX 471 is a nonpeptide CCR1 antagonist that has been shown to displace MIP-1α, RANTES, and MCP-3 with Ki values of 1, 2.8, and 5.5 nM, respectively.{29906} It demonstrates >10,000-fold selectivity for CCR1 over 28 additional G protein-coupled receptors, including related chemokine receptors.{29906} In a rat experimental allergic encephalomyelitis model of multiple sclerosis, BX 471 at 50 mg/kg was shown to significantly reduce the severity of the disease.{29906} BX 471 also decreases the inflammatory response during sepsis, blocks migration of monocytes isolated from rheumatoid arthritis patients, and prevents macrophage and T-cell recruitment in a mouse model of lupus nephritis.{29904,29905,29903}
Brand:CaymanSKU:-Available on backorder
BX-517 is an inhibitor of the serine/threonine kinase 3-phosphoinositide-dependent protein kinase 1 (PDK1; IC50 = 6 nM).{46560} It binds to the ATP binding pocket of PDK1, inhibits Akt2 activation induced by PDK1 in a cell-free assay (IC50 = 20 nM), and inhibits Akt phosphorylation in PC3 cells.{46561}
Brand:CaymanSKU:29238 - 10 mgAvailable on backorder
BX-517 is an inhibitor of the serine/threonine kinase 3-phosphoinositide-dependent protein kinase 1 (PDK1; IC50 = 6 nM).{46560} It binds to the ATP binding pocket of PDK1, inhibits Akt2 activation induced by PDK1 in a cell-free assay (IC50 = 20 nM), and inhibits Akt phosphorylation in PC3 cells.{46561}
Brand:CaymanSKU:29238 - 25 mgAvailable on backorder
BX-517 is an inhibitor of the serine/threonine kinase 3-phosphoinositide-dependent protein kinase 1 (PDK1; IC50 = 6 nM).{46560} It binds to the ATP binding pocket of PDK1, inhibits Akt2 activation induced by PDK1 in a cell-free assay (IC50 = 20 nM), and inhibits Akt phosphorylation in PC3 cells.{46561}
Brand:CaymanSKU:29238 - 5 mgAvailable on backorder
BX-517 is an inhibitor of the serine/threonine kinase 3-phosphoinositide-dependent protein kinase 1 (PDK1; IC50 = 6 nM).{46560} It binds to the ATP binding pocket of PDK1, inhibits Akt2 activation induced by PDK1 in a cell-free assay (IC50 = 20 nM), and inhibits Akt phosphorylation in PC3 cells.{46561}
Brand:CaymanSKU:29238 - 50 mgAvailable on backorder
3-Phosphoinositide-dependent protein kinase 1 (PDK1) is a serine-threonine kinase that phosphorylates and activates a range of other kinases, including PKB, PKA, and certain isoforms of PKC.{24210} BX-795 is a potent, ATP-competitive inhibitor of PDK1 in vitro (IC50 = 11 nM) and in cells (IC50 = 300 nM).{24213} At comparable concentrations, BX-795 also inhibits ERK8, MAPK-interacting kinase 2, Aurora B, Aurora C, MAP/microtubule affinity-regulating kinases 1-4, TNF receptor associated factor-associated NF-κB activator-binding kinase 1, IκB kinase ε, and additional kinases.{17331,24247,24248}
Brand:CaymanSKU:-3-Phosphoinositide-dependent protein kinase 1 (PDK1) is a serine-threonine kinase that phosphorylates and activates a range of other kinases, including PKB, PKA, and certain isoforms of PKC.{24210} BX-795 is a potent, ATP-competitive inhibitor of PDK1 in vitro (IC50 = 11 nM) and in cells (IC50 = 300 nM).{24213} At comparable concentrations, BX-795 also inhibits ERK8, MAPK-interacting kinase 2, Aurora B, Aurora C, MAP/microtubule affinity-regulating kinases 1-4, TNF receptor associated factor-associated NF-κB activator-binding kinase 1, IκB kinase ε, and additional kinases.{17331,24247,24248}
Brand:CaymanSKU:-3-Phosphoinositide-dependent protein kinase 1 (PDK1) is a serine-threonine kinase that phosphorylates and activates a range of other kinases, including PKB, PKA, and certain isoforms of PKC.{24210} BX-795 is a potent, ATP-competitive inhibitor of PDK1 in vitro (IC50 = 11 nM) and in cells (IC50 = 300 nM).{24213} At comparable concentrations, BX-795 also inhibits ERK8, MAPK-interacting kinase 2, Aurora B, Aurora C, MAP/microtubule affinity-regulating kinases 1-4, TNF receptor associated factor-associated NF-κB activator-binding kinase 1, IκB kinase ε, and additional kinases.{17331,24247,24248}
Brand:CaymanSKU:-3-Phosphoinositide-dependent protein kinase 1 (PDK1) is a serine-threonine kinase that phosphorylates and activates a range of other kinases, including PKB, PKA, and certain isoforms of PKC.{24210} BX-795 is a potent, ATP-competitive inhibitor of PDK1 in vitro (IC50 = 11 nM) and in cells (IC50 = 300 nM).{24213} At comparable concentrations, BX-795 also inhibits ERK8, MAPK-interacting kinase 2, Aurora B, Aurora C, MAP/microtubule affinity-regulating kinases 1-4, TNF receptor associated factor-associated NF-κB activator-binding kinase 1, IκB kinase ε, and additional kinases.{17331,24247,24248}
Brand:CaymanSKU:-3-Phosphoinositide-dependent protein kinase 1 (PDK1) is a serine-threonine kinase that phosphorylates and activates a range of other kinases, including protein kinase (PK)B, PKA, and certain isoforms of PKC.{24210} BX-912 is a potent, ATP-competitive inhibitor of PDK1 (IC50 = 26 nM).{24213} It less effectively inhibits a panel of related serine-threonine kinases.{24213} BX-912 has been used to evaluate the role of PDK1 in kinase activation and cell survival.{23909,24212,24211}
Brand:CaymanSKU:-3-Phosphoinositide-dependent protein kinase 1 (PDK1) is a serine-threonine kinase that phosphorylates and activates a range of other kinases, including protein kinase (PK)B, PKA, and certain isoforms of PKC.{24210} BX-912 is a potent, ATP-competitive inhibitor of PDK1 (IC50 = 26 nM).{24213} It less effectively inhibits a panel of related serine-threonine kinases.{24213} BX-912 has been used to evaluate the role of PDK1 in kinase activation and cell survival.{23909,24212,24211}
Brand:CaymanSKU:-3-Phosphoinositide-dependent protein kinase 1 (PDK1) is a serine-threonine kinase that phosphorylates and activates a range of other kinases, including protein kinase (PK)B, PKA, and certain isoforms of PKC.{24210} BX-912 is a potent, ATP-competitive inhibitor of PDK1 (IC50 = 26 nM).{24213} It less effectively inhibits a panel of related serine-threonine kinases.{24213} BX-912 has been used to evaluate the role of PDK1 in kinase activation and cell survival.{23909,24212,24211}
Brand:CaymanSKU:-3-Phosphoinositide-dependent protein kinase 1 (PDK1) is a serine-threonine kinase that phosphorylates and activates a range of other kinases, including protein kinase (PK)B, PKA, and certain isoforms of PKC.{24210} BX-912 is a potent, ATP-competitive inhibitor of PDK1 (IC50 = 26 nM).{24213} It less effectively inhibits a panel of related serine-threonine kinases.{24213} BX-912 has been used to evaluate the role of PDK1 in kinase activation and cell survival.{23909,24212,24211}
Brand:CaymanSKU:-BXL-628 is an analog of vitamin D3 (Item No. 11792) that has diverse biological activities.{40147,40148,40149} It increases death of androgen-stimulated human benign prostatic hyperplasia (BPH) cells via induction of apoptosis in a dose-dependent manner.{40147} In vivo, BXL-628 completely inhibits androgen-stimulated prostate overgrowth in a rat model of BPH. It reduces expression of IL-13 and IgE/mast cell-derived protease 1 (MMCP1) and decreases edema and leukocyte infiltration in the bladder wall in a mouse model of allergen-induced interstitial cystitis.{40148} BXL-628 also reduces the number of adherent endometrial stromal cells and decreases the total weight of endometrial lesions in a mouse model of endometriosis.{40149} Formulations containing BXL-628 are under clinical investigation for the treatment of BPH.
Brand:CaymanSKU:23129 - 1 mgAvailable on backorder
BXL-628 is an analog of vitamin D3 (Item No. 11792) that has diverse biological activities.{40147,40148,40149} It increases death of androgen-stimulated human benign prostatic hyperplasia (BPH) cells via induction of apoptosis in a dose-dependent manner.{40147} In vivo, BXL-628 completely inhibits androgen-stimulated prostate overgrowth in a rat model of BPH. It reduces expression of IL-13 and IgE/mast cell-derived protease 1 (MMCP1) and decreases edema and leukocyte infiltration in the bladder wall in a mouse model of allergen-induced interstitial cystitis.{40148} BXL-628 also reduces the number of adherent endometrial stromal cells and decreases the total weight of endometrial lesions in a mouse model of endometriosis.{40149} Formulations containing BXL-628 are under clinical investigation for the treatment of BPH.
Brand:CaymanSKU:23129 - 5 mgAvailable on backorder
BYK 191023 is an L-arginine competitive and selective inhibitor of inducible nitric oxide synthase (iNOS) with IC50 values of 0.086, 17, and 162 μM for human recombinant iNOS, nNOS, and eNOS, respectively.{36602} It also inhibits murine recombinant iNOS (IC50 = 95 nM). BYK 191023 inhibits iNOS-induced nitrite generation in RMC, RAW, and HEK293 cells (IC50s = 33, 3.1, and 13 μM, respectively). In vivo, BYK 191023 suppresses LPS-induced increases in plasma nitrate and nitrite levels in rats (ED50 = 14.9 μmol/kg per hour).{16676} It prevents development of delayed hypotension in a rat model of LPS-induced endotoxemia when administered at a dose of 50 μmol/kg per hour. BYK 191023 also increases mean arterial pressure and renal blood flow in a sheep model of septic shock.{36603}
Brand:CaymanSKU:-BYK 191023 is an L-arginine competitive and selective inhibitor of inducible nitric oxide synthase (iNOS) with IC50 values of 0.086, 17, and 162 μM for human recombinant iNOS, nNOS, and eNOS, respectively.{36602} It also inhibits murine recombinant iNOS (IC50 = 95 nM). BYK 191023 inhibits iNOS-induced nitrite generation in RMC, RAW, and HEK293 cells (IC50s = 33, 3.1, and 13 μM, respectively). In vivo, BYK 191023 suppresses LPS-induced increases in plasma nitrate and nitrite levels in rats (ED50 = 14.9 μmol/kg per hour).{16676} It prevents development of delayed hypotension in a rat model of LPS-induced endotoxemia when administered at a dose of 50 μmol/kg per hour. BYK 191023 also increases mean arterial pressure and renal blood flow in a sheep model of septic shock.{36603}
Brand:CaymanSKU:-BYK 191023 is an L-arginine competitive and selective inhibitor of inducible nitric oxide synthase (iNOS) with IC50 values of 0.086, 17, and 162 μM for human recombinant iNOS, nNOS, and eNOS, respectively.{36602} It also inhibits murine recombinant iNOS (IC50 = 95 nM). BYK 191023 inhibits iNOS-induced nitrite generation in RMC, RAW, and HEK293 cells (IC50s = 33, 3.1, and 13 μM, respectively). In vivo, BYK 191023 suppresses LPS-induced increases in plasma nitrate and nitrite levels in rats (ED50 = 14.9 μmol/kg per hour).{16676} It prevents development of delayed hypotension in a rat model of LPS-induced endotoxemia when administered at a dose of 50 μmol/kg per hour. BYK 191023 also increases mean arterial pressure and renal blood flow in a sheep model of septic shock.{36603}
Brand:CaymanSKU:-BYK204165 is a selective inhibitor of poly(ADP-ribose) polymerase 1 (PARP1; IC50 = 44.67 nM for human recombinant PARP1 in an enzyme assay).{22587} It is selective for PARP1 over PARP2 (IC50 = 4,168 nM for murine PARP2 in an enzyme assay). BYK204165 inhibits hydrogen peroxide-activated PARP in A549 human lung epithelial, C4I human cervical, and H9c2 rat cardiac myoblast cells with IC50 values of 229.09, 1,778.28, and 123.03 nM, respectively.
Brand:CaymanSKU:21430 -Out of stock
BYK204165 is a selective inhibitor of poly(ADP-ribose) polymerase 1 (PARP1; IC50 = 44.67 nM for human recombinant PARP1 in an enzyme assay).{22587} It is selective for PARP1 over PARP2 (IC50 = 4,168 nM for murine PARP2 in an enzyme assay). BYK204165 inhibits hydrogen peroxide-activated PARP in A549 human lung epithelial, C4I human cervical, and H9c2 rat cardiac myoblast cells with IC50 values of 229.09, 1,778.28, and 123.03 nM, respectively.
Brand:CaymanSKU:21430 -Out of stock
BYK204165 is a selective inhibitor of poly(ADP-ribose) polymerase 1 (PARP1; IC50 = 44.67 nM for human recombinant PARP1 in an enzyme assay).{22587} It is selective for PARP1 over PARP2 (IC50 = 4,168 nM for murine PARP2 in an enzyme assay). BYK204165 inhibits hydrogen peroxide-activated PARP in A549 human lung epithelial, C4I human cervical, and H9c2 rat cardiac myoblast cells with IC50 values of 229.09, 1,778.28, and 123.03 nM, respectively.
Brand:CaymanSKU:21430 -Out of stock
BYK204165 is a selective inhibitor of poly(ADP-ribose) polymerase 1 (PARP1; IC50 = 44.67 nM for human recombinant PARP1 in an enzyme assay).{22587} It is selective for PARP1 over PARP2 (IC50 = 4,168 nM for murine PARP2 in an enzyme assay). BYK204165 inhibits hydrogen peroxide-activated PARP in A549 human lung epithelial, C4I human cervical, and H9c2 rat cardiac myoblast cells with IC50 values of 229.09, 1,778.28, and 123.03 nM, respectively.
Brand:CaymanSKU:21430 -Out of stock
BYL719 is a selective inhibitor of phosphoinositide 3-kinase α (PI3Kα) that is equipotent against both wild type and several mutant isoforms (IC50s = 4.0-4.8 nM).{28003,28002} It is less effective against PI3K isoforms β, γ, and δ (IC50s = 1,156, 250, and 290 nM) as well as a range of related kinases.{28003} BYL719 is effective in vivo, as it dose-dependently inhibits the growth of PI3Kα-dependent xenograft tumors in mice.{28003} Effectiveness against wild type and mutant PI3Kα-dependent tumors may be augmented by combination therapy with inhibitors of other kinases.{28000,28004,28001} Combination therapy may be necessary, as loss of downstream pathway components can confer clinical resistance to BYL719.{28331}
Brand:CaymanSKU:-Out of stock
BYL719 is a selective inhibitor of phosphoinositide 3-kinase α (PI3Kα) that is equipotent against both wild type and several mutant isoforms (IC50s = 4.0-4.8 nM).{28003,28002} It is less effective against PI3K isoforms β, γ, and δ (IC50s = 1,156, 250, and 290 nM) as well as a range of related kinases.{28003} BYL719 is effective in vivo, as it dose-dependently inhibits the growth of PI3Kα-dependent xenograft tumors in mice.{28003} Effectiveness against wild type and mutant PI3Kα-dependent tumors may be augmented by combination therapy with inhibitors of other kinases.{28000,28004,28001} Combination therapy may be necessary, as loss of downstream pathway components can confer clinical resistance to BYL719.{28331}
Brand:CaymanSKU:-Out of stock
BYL719 is a selective inhibitor of phosphoinositide 3-kinase α (PI3Kα) that is equipotent against both wild type and several mutant isoforms (IC50s = 4.0-4.8 nM).{28003,28002} It is less effective against PI3K isoforms β, γ, and δ (IC50s = 1,156, 250, and 290 nM) as well as a range of related kinases.{28003} BYL719 is effective in vivo, as it dose-dependently inhibits the growth of PI3Kα-dependent xenograft tumors in mice.{28003} Effectiveness against wild type and mutant PI3Kα-dependent tumors may be augmented by combination therapy with inhibitors of other kinases.{28000,28004,28001} Combination therapy may be necessary, as loss of downstream pathway components can confer clinical resistance to BYL719.{28331}
Brand:CaymanSKU:-Out of stock
Byssochlamic acid is a mycotoxin that has been found in the agricultural fungal pathogen B. fulva.{52307} It is lethal to mice (LD50 = 94 mg/kg).
Brand:CaymanSKU:29908 - 2.5 mgAvailable on backorder
Byssochlamic acid is a mycotoxin that has been found in the agricultural fungal pathogen B. fulva.{52307} It is lethal to mice (LD50 = 94 mg/kg).
Brand:CaymanSKU:29908 - 500 µgAvailable on backorder
Bz-IEGR-pNA is a colorimetric substrate for Factor Xa.{45397} Factor Xa preferentially binds to and cleaves the Ile-Glu-Gly-Arg (IEGR) peptide sequence to release p-nitroanilide (pNA), which can be quantified by colorimetric detection at 405 nm as a measure of Factor Xa activity.
Brand:CaymanSKU:27567 - 1 mgAvailable on backorder
Bz-IEGR-pNA is a colorimetric substrate for Factor Xa.{45397} Factor Xa preferentially binds to and cleaves the Ile-Glu-Gly-Arg (IEGR) peptide sequence to release p-nitroanilide (pNA), which can be quantified by colorimetric detection at 405 nm as a measure of Factor Xa activity.
Brand:CaymanSKU:27567 - 10 mgAvailable on backorder
Bz-IEGR-pNA is a colorimetric substrate for Factor Xa.{45397} Factor Xa preferentially binds to and cleaves the Ile-Glu-Gly-Arg (IEGR) peptide sequence to release p-nitroanilide (pNA), which can be quantified by colorimetric detection at 405 nm as a measure of Factor Xa activity.
Brand:CaymanSKU:27567 - 25 mgAvailable on backorder
Bz-IEGR-pNA is a colorimetric substrate for Factor Xa.{45397} Factor Xa preferentially binds to and cleaves the Ile-Glu-Gly-Arg (IEGR) peptide sequence to release p-nitroanilide (pNA), which can be quantified by colorimetric detection at 405 nm as a measure of Factor Xa activity.
Brand:CaymanSKU:27567 - 5 mgAvailable on backorder
Bz-Nle-KRR-AMC is a fluorogenic peptide substrate for yellow fever virus (YFV) non-structural 3 (NS3) and dengue virus (DV) NS2B/3 serine proteases.{46461,46462} Upon enzymatic cleavage by YFV NS3 or DV NS2B/3 serine proteases, 7-amino-4-methylcoumarin (AMC) is released and its fluorescence can be used to quantify YFV NS3 or DV NS2B/3 serine protease activity. AMC displays excitation/emission maxima of 340-360/440-460 nm, respectively.
Brand:CaymanSKU:27710 - 1 mgAvailable on backorder
Bz-Nle-KRR-AMC is a fluorogenic peptide substrate for yellow fever virus (YFV) non-structural 3 (NS3) and dengue virus (DV) NS2B/3 serine proteases.{46461,46462} Upon enzymatic cleavage by YFV NS3 or DV NS2B/3 serine proteases, 7-amino-4-methylcoumarin (AMC) is released and its fluorescence can be used to quantify YFV NS3 or DV NS2B/3 serine protease activity. AMC displays excitation/emission maxima of 340-360/440-460 nm, respectively.
Brand:CaymanSKU:27710 - 10 mgAvailable on backorder
Bz-Nle-KRR-AMC is a fluorogenic peptide substrate for yellow fever virus (YFV) non-structural 3 (NS3) and dengue virus (DV) NS2B/3 serine proteases.{46461,46462} Upon enzymatic cleavage by YFV NS3 or DV NS2B/3 serine proteases, 7-amino-4-methylcoumarin (AMC) is released and its fluorescence can be used to quantify YFV NS3 or DV NS2B/3 serine protease activity. AMC displays excitation/emission maxima of 340-360/440-460 nm, respectively.
Brand:CaymanSKU:27710 - 25 mgAvailable on backorder
Bz-Nle-KRR-AMC is a fluorogenic peptide substrate for yellow fever virus (YFV) non-structural 3 (NS3) and dengue virus (DV) NS2B/3 serine proteases.{46461,46462} Upon enzymatic cleavage by YFV NS3 or DV NS2B/3 serine proteases, 7-amino-4-methylcoumarin (AMC) is released and its fluorescence can be used to quantify YFV NS3 or DV NS2B/3 serine protease activity. AMC displays excitation/emission maxima of 340-360/440-460 nm, respectively.
Brand:CaymanSKU:27710 - 5 mgAvailable on backorder
C-170 is an inhibitor of stimulator of interferon genes (STING).{35390,50925} It binds to STING, inhibits its palmitoylation, and prevents the recruitment and phosphorylation of TBK1.{35390} It selectively reduces human and mouse STING-, but not RIG-I- or TBK1-, mediated IFN-β reporter activity in HEK293 cells when used at concentrations ranging from 0.02 to 2 µM.
Brand:CaymanSKU:30157 - 10 mgAvailable on backorder
C-170 is an inhibitor of stimulator of interferon genes (STING).{35390,50925} It binds to STING, inhibits its palmitoylation, and prevents the recruitment and phosphorylation of TBK1.{35390} It selectively reduces human and mouse STING-, but not RIG-I- or TBK1-, mediated IFN-β reporter activity in HEK293 cells when used at concentrations ranging from 0.02 to 2 µM.
Brand:CaymanSKU:30157 - 100 mgAvailable on backorder
C-170 is an inhibitor of stimulator of interferon genes (STING).{35390,50925} It binds to STING, inhibits its palmitoylation, and prevents the recruitment and phosphorylation of TBK1.{35390} It selectively reduces human and mouse STING-, but not RIG-I- or TBK1-, mediated IFN-β reporter activity in HEK293 cells when used at concentrations ranging from 0.02 to 2 µM.
Brand:CaymanSKU:30157 - 25 mgAvailable on backorder
C-170 is an inhibitor of stimulator of interferon genes (STING).{35390,50925} It binds to STING, inhibits its palmitoylation, and prevents the recruitment and phosphorylation of TBK1.{35390} It selectively reduces human and mouse STING-, but not RIG-I- or TBK1-, mediated IFN-β reporter activity in HEK293 cells when used at concentrations ranging from 0.02 to 2 µM.
Brand:CaymanSKU:30157 - 50 mgAvailable on backorder
C-171 is an inhibitor of stimulator of interferon genes (STING).{35390,50925} It binds to STING, inhibits its palmitoylation, and prevents the recruitment and phosphorylation of TBK1.{35390} It selectively reduces human and mouse STING-, but not RIG-I or TBK1-, mediated IFN-β reporter activity in HEK293 cells when used at concentrations ranging from 0.02 to 2 μM.
Brand:CaymanSKU:30159 - 10 mgAvailable on backorder
C-171 is an inhibitor of stimulator of interferon genes (STING).{35390,50925} It binds to STING, inhibits its palmitoylation, and prevents the recruitment and phosphorylation of TBK1.{35390} It selectively reduces human and mouse STING-, but not RIG-I or TBK1-, mediated IFN-β reporter activity in HEK293 cells when used at concentrations ranging from 0.02 to 2 μM.
Brand:CaymanSKU:30159 - 100 mgAvailable on backorder
C-171 is an inhibitor of stimulator of interferon genes (STING).{35390,50925} It binds to STING, inhibits its palmitoylation, and prevents the recruitment and phosphorylation of TBK1.{35390} It selectively reduces human and mouse STING-, but not RIG-I or TBK1-, mediated IFN-β reporter activity in HEK293 cells when used at concentrations ranging from 0.02 to 2 μM.
Brand:CaymanSKU:30159 - 25 mgAvailable on backorder
C-171 is an inhibitor of stimulator of interferon genes (STING).{35390,50925} It binds to STING, inhibits its palmitoylation, and prevents the recruitment and phosphorylation of TBK1.{35390} It selectively reduces human and mouse STING-, but not RIG-I or TBK1-, mediated IFN-β reporter activity in HEK293 cells when used at concentrations ranging from 0.02 to 2 μM.
Brand:CaymanSKU:30159 - 50 mgAvailable on backorder
C-176 is a covalent inhibitor of stimulator of interferon genes (STING).{35390} It selectively reduces STING-, but not RIG-I or TBK1-, mediated IFN-β reporter activity in HEK293 cells when used at concentrations ranging from 0.01 to 5 μM. C-176 reduces serum levels of type-I interferons (IFNs) and cardiac inflammation in the Trex-/- mouse model of multi-organ inflammation.
Brand:CaymanSKU:25859 - 10 mgAvailable on backorder
C-176 is a covalent inhibitor of stimulator of interferon genes (STING).{35390} It selectively reduces STING-, but not RIG-I or TBK1-, mediated IFN-β reporter activity in HEK293 cells when used at concentrations ranging from 0.01 to 5 μM. C-176 reduces serum levels of type-I interferons (IFNs) and cardiac inflammation in the Trex-/- mouse model of multi-organ inflammation.
Brand:CaymanSKU:25859 - 100 mgAvailable on backorder
C-176 is a covalent inhibitor of stimulator of interferon genes (STING).{35390} It selectively reduces STING-, but not RIG-I or TBK1-, mediated IFN-β reporter activity in HEK293 cells when used at concentrations ranging from 0.01 to 5 μM. C-176 reduces serum levels of type-I interferons (IFNs) and cardiac inflammation in the Trex-/- mouse model of multi-organ inflammation.
Brand:CaymanSKU:25859 - 25 mgAvailable on backorder
C-176 is a covalent inhibitor of stimulator of interferon genes (STING).{35390} It selectively reduces STING-, but not RIG-I or TBK1-, mediated IFN-β reporter activity in HEK293 cells when used at concentrations ranging from 0.01 to 5 μM. C-176 reduces serum levels of type-I interferons (IFNs) and cardiac inflammation in the Trex-/- mouse model of multi-organ inflammation.
Brand:CaymanSKU:25859 - 50 mgAvailable on backorder
C-178 is a covalent inhibitor of stimulator of interferon genes (STING).{35390} It binds to Cys91 on STING to block its palmitoylation and prevents recruitment and phosphorylation of TBK1 in HEK293T cells. C-178 (0.01-1.25 µM) selectively reduces STING-, but not RIG-I- or TBK1-, mediated IFN-β reporter activity in HEK293 cells. It also prevents increases in Ifnb1 expression in bone marrow-derived macrophages (BMDMs) induced by cyclic di-GMP (Item No. 17144), double-stranded DNA, and LPS when used at a concentration of 0.5 µM.
Brand:CaymanSKU:25860 - 10 mgAvailable on backorder
C-178 is a covalent inhibitor of stimulator of interferon genes (STING).{35390} It binds to Cys91 on STING to block its palmitoylation and prevents recruitment and phosphorylation of TBK1 in HEK293T cells. C-178 (0.01-1.25 µM) selectively reduces STING-, but not RIG-I- or TBK1-, mediated IFN-β reporter activity in HEK293 cells. It also prevents increases in Ifnb1 expression in bone marrow-derived macrophages (BMDMs) induced by cyclic di-GMP (Item No. 17144), double-stranded DNA, and LPS when used at a concentration of 0.5 µM.
Brand:CaymanSKU:25860 - 25 mgAvailable on backorder
C-178 is a covalent inhibitor of stimulator of interferon genes (STING).{35390} It binds to Cys91 on STING to block its palmitoylation and prevents recruitment and phosphorylation of TBK1 in HEK293T cells. C-178 (0.01-1.25 µM) selectively reduces STING-, but not RIG-I- or TBK1-, mediated IFN-β reporter activity in HEK293 cells. It also prevents increases in Ifnb1 expression in bone marrow-derived macrophages (BMDMs) induced by cyclic di-GMP (Item No. 17144), double-stranded DNA, and LPS when used at a concentration of 0.5 µM.
Brand:CaymanSKU:25860 - 5 mgAvailable on backorder
C-178 is a covalent inhibitor of stimulator of interferon genes (STING).{35390} It binds to Cys91 on STING to block its palmitoylation and prevents recruitment and phosphorylation of TBK1 in HEK293T cells. C-178 (0.01-1.25 µM) selectively reduces STING-, but not RIG-I- or TBK1-, mediated IFN-β reporter activity in HEK293 cells. It also prevents increases in Ifnb1 expression in bone marrow-derived macrophages (BMDMs) induced by cyclic di-GMP (Item No. 17144), double-stranded DNA, and LPS when used at a concentration of 0.5 µM.
Brand:CaymanSKU:25860 - 50 mgAvailable on backorder
C-6 NBD is a derivative of the environmentally sensitive fluorophore nitrobenzoxadiazole (NBD; absorbance 465 nm, emission 535 nm). It is modified with a hexanoic acid tail, which provides a reactive carboxylic acid site. C-6 NBD has been used to synthesize a variety of fluorescently tagged compounds for research purposes.{3461,2814,5478,30431,30432}
Brand:CaymanSKU:-Available on backorder
C-6 NBD is a derivative of the environmentally sensitive fluorophore nitrobenzoxadiazole (NBD; absorbance 465 nm, emission 535 nm). It is modified with a hexanoic acid tail, which provides a reactive carboxylic acid site. C-6 NBD has been used to synthesize a variety of fluorescently tagged compounds for research purposes.{3461,2814,5478,30431,30432}
Brand:CaymanSKU:-Available on backorder
C-7280948 is a protein arginine methyltransferase 1 (PRMT1) inhibitor (IC50 = 12.8 µM, in vitro).{33883,33882} PRMT1 enzymes transfer a methyl group from S-adenosylmethionine to arginine residues on histones, which leads to transcription.{33882} PRMT1 is essential for mixed lineage leukemia oncogenic transformation and thus its inhibition is a potential treatment for these aggressive leukemias.{33884}
Brand:CaymanSKU:21601 -Out of stock
C-7280948 is a protein arginine methyltransferase 1 (PRMT1) inhibitor (IC50 = 12.8 µM, in vitro).{33883,33882} PRMT1 enzymes transfer a methyl group from S-adenosylmethionine to arginine residues on histones, which leads to transcription.{33882} PRMT1 is essential for mixed lineage leukemia oncogenic transformation and thus its inhibition is a potential treatment for these aggressive leukemias.{33884}
Brand:CaymanSKU:21601 -Out of stock
C-7280948 is a protein arginine methyltransferase 1 (PRMT1) inhibitor (IC50 = 12.8 µM, in vitro).{33883,33882} PRMT1 enzymes transfer a methyl group from S-adenosylmethionine to arginine residues on histones, which leads to transcription.{33882} PRMT1 is essential for mixed lineage leukemia oncogenic transformation and thus its inhibition is a potential treatment for these aggressive leukemias.{33884}
Brand:CaymanSKU:21601 -Out of stock