Chemicals

Showing 39901–40050 of 41137 results

  • Vulpinic acid is a lichen metabolite that has been found in L. vulpina and has diverse biological activities.{50292,50293,50294,50295} It is active against C. perfringens, B. vulgatus, B. fragilis, B. loescheii, P. acnes, E. faecium, and methicillin-susceptible and -resistant S. aureus (MICs = 4-16 μg/ml).{50292} Vulpinic acid (25-800 μM) prevents UVB-induced apoptosis, cytotoxicity, and cytoskeletal modifications in HaCaT human keratinocytes.{50293} It also increases scratch wound healing of HaCaT cells.{50294} Vulpinic acid (15 μM) reduces hydrogen peroxide-induced production of reactive oxygen species (ROS) and cytotoxicity in human umbilical vein endothelial cells (HUVECs).{50295}  

     

    Brand:
    Cayman
    SKU:21685 -

    Out of stock

  • Vulpinic acid is a lichen metabolite that has been found in L. vulpina and has diverse biological activities.{50292,50293,50294,50295} It is active against C. perfringens, B. vulgatus, B. fragilis, B. loescheii, P. acnes, E. faecium, and methicillin-susceptible and -resistant S. aureus (MICs = 4-16 μg/ml).{50292} Vulpinic acid (25-800 μM) prevents UVB-induced apoptosis, cytotoxicity, and cytoskeletal modifications in HaCaT human keratinocytes.{50293} It also increases scratch wound healing of HaCaT cells.{50294} Vulpinic acid (15 μM) reduces hydrogen peroxide-induced production of reactive oxygen species (ROS) and cytotoxicity in human umbilical vein endothelial cells (HUVECs).{50295}  

     

    Brand:
    Cayman
    SKU:21685 -

    Out of stock

  • Vulpinic acid is a lichen metabolite that has been found in L. vulpina and has diverse biological activities.{50292,50293,50294,50295} It is active against C. perfringens, B. vulgatus, B. fragilis, B. loescheii, P. acnes, E. faecium, and methicillin-susceptible and -resistant S. aureus (MICs = 4-16 μg/ml).{50292} Vulpinic acid (25-800 μM) prevents UVB-induced apoptosis, cytotoxicity, and cytoskeletal modifications in HaCaT human keratinocytes.{50293} It also increases scratch wound healing of HaCaT cells.{50294} Vulpinic acid (15 μM) reduces hydrogen peroxide-induced production of reactive oxygen species (ROS) and cytotoxicity in human umbilical vein endothelial cells (HUVECs).{50295}  

     

    Brand:
    Cayman
    SKU:21685 -

    Out of stock

  • VX-509 is a selective inhibitor of Janus kinase 3 (JAK3) with a Ki value of 2.5 nM in enzyme assays and an IC50 value of 50-170 nM in cellular assays dependent on JAK3 activity with no measurable activity against other JAK isotypes.{31666} At 10-100 mg/kg, it has been shown to dose dependently reduce proinflammatory responses in a rat collagen-induced arthritis model and a mouse model of oxazolone-induced delayed-type hypersensitivity.{31666}  

     

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    Cayman
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  • VX-509 is a selective inhibitor of Janus kinase 3 (JAK3) with a Ki value of 2.5 nM in enzyme assays and an IC50 value of 50-170 nM in cellular assays dependent on JAK3 activity with no measurable activity against other JAK isotypes.{31666} At 10-100 mg/kg, it has been shown to dose dependently reduce proinflammatory responses in a rat collagen-induced arthritis model and a mouse model of oxazolone-induced delayed-type hypersensitivity.{31666}  

     

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    Cayman
    SKU:-

    Available on backorder

  • VX-509 is a selective inhibitor of Janus kinase 3 (JAK3) with a Ki value of 2.5 nM in enzyme assays and an IC50 value of 50-170 nM in cellular assays dependent on JAK3 activity with no measurable activity against other JAK isotypes.{31666} At 10-100 mg/kg, it has been shown to dose dependently reduce proinflammatory responses in a rat collagen-induced arthritis model and a mouse model of oxazolone-induced delayed-type hypersensitivity.{31666}  

     

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    Cayman
    SKU:-

    Available on backorder

  • VX-509 is a selective inhibitor of Janus kinase 3 (JAK3) with a Ki value of 2.5 nM in enzyme assays and an IC50 value of 50-170 nM in cellular assays dependent on JAK3 activity with no measurable activity against other JAK isotypes.{31666} At 10-100 mg/kg, it has been shown to dose dependently reduce proinflammatory responses in a rat collagen-induced arthritis model and a mouse model of oxazolone-induced delayed-type hypersensitivity.{31666}  

     

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    Cayman
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    Available on backorder

  • VX-661 is an investigational compound that promotes the maturation of delta F508 mutants of the cystic fibrosis transmembrane conductance regulator (CFTR).{34006} Delta F508 CFTR represents a class of CFTR mutation that is characterized by impaired processing of misfolded CFTR proteins and reduced accumulation of the protein at the cell surface.{34006} VX-661 is intended to facilitate trafficking of CFTR to the epithelial cell membrane. It may be combined with the CFTR potentiator ivacaftor (Item No. 15145) to stimulate both CFTR accumulation and opening at the apical epithelial surface.{34006,34007}  

     

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    Cayman
    SKU:21480 -

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  • VX-661 is an investigational compound that promotes the maturation of delta F508 mutants of the cystic fibrosis transmembrane conductance regulator (CFTR).{34006} Delta F508 CFTR represents a class of CFTR mutation that is characterized by impaired processing of misfolded CFTR proteins and reduced accumulation of the protein at the cell surface.{34006} VX-661 is intended to facilitate trafficking of CFTR to the epithelial cell membrane. It may be combined with the CFTR potentiator ivacaftor (Item No. 15145) to stimulate both CFTR accumulation and opening at the apical epithelial surface.{34006,34007}  

     

    Brand:
    Cayman
    SKU:21480 -

    Out of stock

  • VX-661 is an investigational compound that promotes the maturation of delta F508 mutants of the cystic fibrosis transmembrane conductance regulator (CFTR).{34006} Delta F508 CFTR represents a class of CFTR mutation that is characterized by impaired processing of misfolded CFTR proteins and reduced accumulation of the protein at the cell surface.{34006} VX-661 is intended to facilitate trafficking of CFTR to the epithelial cell membrane. It may be combined with the CFTR potentiator ivacaftor (Item No. 15145) to stimulate both CFTR accumulation and opening at the apical epithelial surface.{34006,34007}  

     

    Brand:
    Cayman
    SKU:21480 -

    Out of stock

  • VX-661 is an investigational compound that promotes the maturation of delta F508 mutants of the cystic fibrosis transmembrane conductance regulator (CFTR).{34006} Delta F508 CFTR represents a class of CFTR mutation that is characterized by impaired processing of misfolded CFTR proteins and reduced accumulation of the protein at the cell surface.{34006} VX-661 is intended to facilitate trafficking of CFTR to the epithelial cell membrane. It may be combined with the CFTR potentiator ivacaftor (Item No. 15145) to stimulate both CFTR accumulation and opening at the apical epithelial surface.{34006,34007}  

     

    Brand:
    Cayman
    SKU:21480 -

    Out of stock

  • VX-702 is a third generation inhibitor of p38 mitogen-activated protein (MAP) kinases, binding to both p38α and p38β (Kd = 3.7 and 17 nM, respectively) in an ATP-competitive fashion.{21533} It inhibits IL-6, IL-1β, and TNF-α production in LPS-primed blood with IC50 values of 59, 122, and 99 ng/ml, respectively.{21533} VX-702, at 1 μM, inhibits activation of p38 in platelets by thrombin, U-46619 (Item No. 16450), or collagen but does not block platelet aggregation in response to collagen.{21534} Although orally active, VX-702 provides only transient suppression of biomarkers of inflammation in ongoing rheumatoid arthritis.{21532}  

     

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    Cayman
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  • VX-702 is a third generation inhibitor of p38 mitogen-activated protein (MAP) kinases, binding to both p38α and p38β (Kd = 3.7 and 17 nM, respectively) in an ATP-competitive fashion.{21533} It inhibits IL-6, IL-1β, and TNF-α production in LPS-primed blood with IC50 values of 59, 122, and 99 ng/ml, respectively.{21533} VX-702, at 1 μM, inhibits activation of p38 in platelets by thrombin, U-46619 (Item No. 16450), or collagen but does not block platelet aggregation in response to collagen.{21534} Although orally active, VX-702 provides only transient suppression of biomarkers of inflammation in ongoing rheumatoid arthritis.{21532}  

     

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    Cayman
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  • VX-702 is a third generation inhibitor of p38 mitogen-activated protein (MAP) kinases, binding to both p38α and p38β (Kd = 3.7 and 17 nM, respectively) in an ATP-competitive fashion.{21533} It inhibits IL-6, IL-1β, and TNF-α production in LPS-primed blood with IC50 values of 59, 122, and 99 ng/ml, respectively.{21533} VX-702, at 1 μM, inhibits activation of p38 in platelets by thrombin, U-46619 (Item No. 16450), or collagen but does not block platelet aggregation in response to collagen.{21534} Although orally active, VX-702 provides only transient suppression of biomarkers of inflammation in ongoing rheumatoid arthritis.{21532}  

     

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    Cayman
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  • p38α is a member of the mitogen-activated protein kinase (MAPK) family of serine/threonine protein kinases. It is widely expressed in endothelial, immune, and inflammatory cells and plays a central role in the regulation of proinflammatory cytokine production including TNF-α, IL-1β, and IL-6. VX-745 is a potent inhibitor of p38α MAPK (IC50 = 10 nM) with 20-fold selectivity over p38β and 1000-fold selectivity over closely related kinases, ERK1 and JNK1-3.{29195} It blocks IL-1β and TNF-α release in whole blood in vitro with IC50 values of 150 and 180 nM, respectively.{29195} VX-745 has been shown to demonstrate anti-inflammatory efficacy in an animal model of rheumatoid arthritis, but was discontinued in clinical trial due to adverse central nervous system effects.{21533}  

     

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    Cayman
    SKU:-

    Available on backorder

  • p38α is a member of the mitogen-activated protein kinase (MAPK) family of serine/threonine protein kinases. It is widely expressed in endothelial, immune, and inflammatory cells and plays a central role in the regulation of proinflammatory cytokine production including TNF-α, IL-1β, and IL-6. VX-745 is a potent inhibitor of p38α MAPK (IC50 = 10 nM) with 20-fold selectivity over p38β and 1000-fold selectivity over closely related kinases, ERK1 and JNK1-3.{29195} It blocks IL-1β and TNF-α release in whole blood in vitro with IC50 values of 150 and 180 nM, respectively.{29195} VX-745 has been shown to demonstrate anti-inflammatory efficacy in an animal model of rheumatoid arthritis, but was discontinued in clinical trial due to adverse central nervous system effects.{21533}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • p38α is a member of the mitogen-activated protein kinase (MAPK) family of serine/threonine protein kinases. It is widely expressed in endothelial, immune, and inflammatory cells and plays a central role in the regulation of proinflammatory cytokine production including TNF-α, IL-1β, and IL-6. VX-745 is a potent inhibitor of p38α MAPK (IC50 = 10 nM) with 20-fold selectivity over p38β and 1000-fold selectivity over closely related kinases, ERK1 and JNK1-3.{29195} It blocks IL-1β and TNF-α release in whole blood in vitro with IC50 values of 150 and 180 nM, respectively.{29195} VX-745 has been shown to demonstrate anti-inflammatory efficacy in an animal model of rheumatoid arthritis, but was discontinued in clinical trial due to adverse central nervous system effects.{21533}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • p38α is a member of the mitogen-activated protein kinase (MAPK) family of serine/threonine protein kinases. It is widely expressed in endothelial, immune, and inflammatory cells and plays a central role in the regulation of proinflammatory cytokine production including TNF-α, IL-1β, and IL-6. VX-745 is a potent inhibitor of p38α MAPK (IC50 = 10 nM) with 20-fold selectivity over p38β and 1000-fold selectivity over closely related kinases, ERK1 and JNK1-3.{29195} It blocks IL-1β and TNF-α release in whole blood in vitro with IC50 values of 150 and 180 nM, respectively.{29195} VX-745 has been shown to demonstrate anti-inflammatory efficacy in an animal model of rheumatoid arthritis, but was discontinued in clinical trial due to adverse central nervous system effects.{21533}  

     

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    Cayman
    SKU:-

    Available on backorder

  • VX-765 is a prodrug form of the caspase-1 inhibitor VRT-043198.{45582} VX-765 (50, 100, and 200 mg/kg) inhibits LPS-induced increases in serum IL-1β levels in mice. It also reduces oxazolone-induced ear edema and levels of IL-1β, IL-18, and IFN-γ in ear tissue in an oxazolone-sensitized mouse model of delayed-type hypersensitivity. VX-765 reduces forepaw inflammation in a mouse model of collagen-induced arthritis in a dose-dependent manner. VX-765 (≥50 mg/kg) decreases seizure duration and the number of seizures in a mouse model of acute seizures induced by hippocampal kainic acid injection, as well as delays the onset of seizures when administered at doses of 100 and 200 mg/kg.{45583} It also reduces the aggregated duration of epileptic activity in a mouse model of chronic epilepsy.  

     

    Brand:
    Cayman
    SKU:28825 - 10 mg

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  • VX-765 is a prodrug form of the caspase-1 inhibitor VRT-043198.{45582} VX-765 (50, 100, and 200 mg/kg) inhibits LPS-induced increases in serum IL-1β levels in mice. It also reduces oxazolone-induced ear edema and levels of IL-1β, IL-18, and IFN-γ in ear tissue in an oxazolone-sensitized mouse model of delayed-type hypersensitivity. VX-765 reduces forepaw inflammation in a mouse model of collagen-induced arthritis in a dose-dependent manner. VX-765 (≥50 mg/kg) decreases seizure duration and the number of seizures in a mouse model of acute seizures induced by hippocampal kainic acid injection, as well as delays the onset of seizures when administered at doses of 100 and 200 mg/kg.{45583} It also reduces the aggregated duration of epileptic activity in a mouse model of chronic epilepsy.  

     

    Brand:
    Cayman
    SKU:28825 - 25 mg

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  • VX-765 is a prodrug form of the caspase-1 inhibitor VRT-043198.{45582} VX-765 (50, 100, and 200 mg/kg) inhibits LPS-induced increases in serum IL-1β levels in mice. It also reduces oxazolone-induced ear edema and levels of IL-1β, IL-18, and IFN-γ in ear tissue in an oxazolone-sensitized mouse model of delayed-type hypersensitivity. VX-765 reduces forepaw inflammation in a mouse model of collagen-induced arthritis in a dose-dependent manner. VX-765 (≥50 mg/kg) decreases seizure duration and the number of seizures in a mouse model of acute seizures induced by hippocampal kainic acid injection, as well as delays the onset of seizures when administered at doses of 100 and 200 mg/kg.{45583} It also reduces the aggregated duration of epileptic activity in a mouse model of chronic epilepsy.  

     

    Brand:
    Cayman
    SKU:28825 - 5 mg

    Available on backorder

  • VX-765 is a prodrug form of the caspase-1 inhibitor VRT-043198.{45582} VX-765 (50, 100, and 200 mg/kg) inhibits LPS-induced increases in serum IL-1β levels in mice. It also reduces oxazolone-induced ear edema and levels of IL-1β, IL-18, and IFN-γ in ear tissue in an oxazolone-sensitized mouse model of delayed-type hypersensitivity. VX-765 reduces forepaw inflammation in a mouse model of collagen-induced arthritis in a dose-dependent manner. VX-765 (≥50 mg/kg) decreases seizure duration and the number of seizures in a mouse model of acute seizures induced by hippocampal kainic acid injection, as well as delays the onset of seizures when administered at doses of 100 and 200 mg/kg.{45583} It also reduces the aggregated duration of epileptic activity in a mouse model of chronic epilepsy.  

     

    Brand:
    Cayman
    SKU:28825 - 50 mg

    Available on backorder

  • VX-809 is a small molecule that corrects the processing of cystic fibrosis transmembrane conductance regulator (CFTR) proteins bearing the F508 deletion (F508del) mutation carried by 90% of cystic fibrosis patients.{37102} It enhances F508del-CFTR protein maturation and restores chloride transport function in FRT cells (EC50s = 100 and 500 nM, respectively). VX-809 increases the amount of F508del-CFTR protein exiting the endoplasmic reticulum in HEK293 cells expressing the mutant receptor. It also increases chloride and fluid transport in cultured human bronchial epithelial cells isolated from cystic fibrosis patients carrying the F508del-CFTR mutation. Formulations containing VX-809 are being investigated clinically for the treatment of cystic fibrosis.  

     

    Brand:
    Cayman
    SKU:22196 -

    Out of stock

  • VX-809 is a small molecule that corrects the processing of cystic fibrosis transmembrane conductance regulator (CFTR) proteins bearing the F508 deletion (F508del) mutation carried by 90% of cystic fibrosis patients.{37102} It enhances F508del-CFTR protein maturation and restores chloride transport function in FRT cells (EC50s = 100 and 500 nM, respectively). VX-809 increases the amount of F508del-CFTR protein exiting the endoplasmic reticulum in HEK293 cells expressing the mutant receptor. It also increases chloride and fluid transport in cultured human bronchial epithelial cells isolated from cystic fibrosis patients carrying the F508del-CFTR mutation. Formulations containing VX-809 are being investigated clinically for the treatment of cystic fibrosis.  

     

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    Cayman
    SKU:22196 -

    Out of stock

  • VX-809 is a small molecule that corrects the processing of cystic fibrosis transmembrane conductance regulator (CFTR) proteins bearing the F508 deletion (F508del) mutation carried by 90% of cystic fibrosis patients.{37102} It enhances F508del-CFTR protein maturation and restores chloride transport function in FRT cells (EC50s = 100 and 500 nM, respectively). VX-809 increases the amount of F508del-CFTR protein exiting the endoplasmic reticulum in HEK293 cells expressing the mutant receptor. It also increases chloride and fluid transport in cultured human bronchial epithelial cells isolated from cystic fibrosis patients carrying the F508del-CFTR mutation. Formulations containing VX-809 are being investigated clinically for the treatment of cystic fibrosis.  

     

    Brand:
    Cayman
    SKU:22196 -

    Out of stock

  • VX-809 is a small molecule that corrects the processing of cystic fibrosis transmembrane conductance regulator (CFTR) proteins bearing the F508 deletion (F508del) mutation carried by 90% of cystic fibrosis patients.{37102} It enhances F508del-CFTR protein maturation and restores chloride transport function in FRT cells (EC50s = 100 and 500 nM, respectively). VX-809 increases the amount of F508del-CFTR protein exiting the endoplasmic reticulum in HEK293 cells expressing the mutant receptor. It also increases chloride and fluid transport in cultured human bronchial epithelial cells isolated from cystic fibrosis patients carrying the F508del-CFTR mutation. Formulations containing VX-809 are being investigated clinically for the treatment of cystic fibrosis.  

     

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    Cayman
    SKU:22196 -

    Out of stock

  • W-13 is a naphthalenesulfonamide derivative that acts as a potent antagonist of calmodulin (IC50 = 22 μM) and is widely used to investigate Ca2+/calmodulin-regulated enzyme activities.{22383,22667,22668}  

     

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    Cayman
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  • W-13 is a naphthalenesulfonamide derivative that acts as a potent antagonist of calmodulin (IC50 = 22 μM) and is widely used to investigate Ca2+/calmodulin-regulated enzyme activities.{22383,22667,22668}  

     

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    Cayman
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  • W-13 is a naphthalenesulfonamide derivative that acts as a potent antagonist of calmodulin (IC50 = 22 μM) and is widely used to investigate Ca2+/calmodulin-regulated enzyme activities.{22383,22667,22668}  

     

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    Cayman
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  • W-5 is a chlorine-deficient analog of W-7 (Item No. 14826), a calmodulin antagonist that binds to calmodulin and inhibits Ca2+/calmodulin-regulated enzyme activities (Ki = 11 μM).{22382,22380} W-5 is less active than its calmodulin antagonist counterpart, inhibiting CHO-K1, MCF-7 breast cancer, and human myeloid progenitor cell proliferation with IC50 values greater than 100 μM.{22382,22381,22383} As a weaker antagonist for calmodulin, W-5 is suitable for use as a control compound for understanding the specificity of other calmodulin antagonists.  

     

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    Cayman
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  • W-5 is a chlorine-deficient analog of W-7 (Item No. 14826), a calmodulin antagonist that binds to calmodulin and inhibits Ca2+/calmodulin-regulated enzyme activities (Ki = 11 μM).{22382,22380} W-5 is less active than its calmodulin antagonist counterpart, inhibiting CHO-K1, MCF-7 breast cancer, and human myeloid progenitor cell proliferation with IC50 values greater than 100 μM.{22382,22381,22383} As a weaker antagonist for calmodulin, W-5 is suitable for use as a control compound for understanding the specificity of other calmodulin antagonists.  

     

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  • W-54011 is an orally bioavailable, nonpeptide antagonist of complement component 5a receptor 1 (C5aR), also known as cluster of differentiation 88 (CD88).{34624} W-54011 inhibits 125I-rhC5a binding in neutrophils (Ki = 2.2 nM) and C5a-mediated intracellular Ca2+ mobilization (IC50 = 3.1 nM).{34624} W-54011 is selective and does not affect Ca2+ mobilization mediated by other G protein-coupled receptor (GPCR) ligands, N-Formyl-Met-Leu-Phe (fMLF; Item No. 21495), or IL-8 up to a concentration of 10 μM.{34624} It inhibits Ca2+ mobilization in neutrophils in humans, cynomolgus monkeys, and gerbils, but not in mice, rats, guinea pigs, rabbits, or dogs.{34624} At 10 nM, W-54011 also inhibits C5a-mediated migration and vessel formation of human microvascular endothelial cells (HMEC-1).{34625}  

     

    Brand:
    Cayman
    SKU:21231 -

    Out of stock

  • W-54011 is an orally bioavailable, nonpeptide antagonist of complement component 5a receptor 1 (C5aR), also known as cluster of differentiation 88 (CD88).{34624} W-54011 inhibits 125I-rhC5a binding in neutrophils (Ki = 2.2 nM) and C5a-mediated intracellular Ca2+ mobilization (IC50 = 3.1 nM).{34624} W-54011 is selective and does not affect Ca2+ mobilization mediated by other G protein-coupled receptor (GPCR) ligands, N-Formyl-Met-Leu-Phe (fMLF; Item No. 21495), or IL-8 up to a concentration of 10 μM.{34624} It inhibits Ca2+ mobilization in neutrophils in humans, cynomolgus monkeys, and gerbils, but not in mice, rats, guinea pigs, rabbits, or dogs.{34624} At 10 nM, W-54011 also inhibits C5a-mediated migration and vessel formation of human microvascular endothelial cells (HMEC-1).{34625}  

     

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    Cayman
    SKU:21231 -

    Out of stock

  • W-54011 is an orally bioavailable, nonpeptide antagonist of complement component 5a receptor 1 (C5aR), also known as cluster of differentiation 88 (CD88).{34624} W-54011 inhibits 125I-rhC5a binding in neutrophils (Ki = 2.2 nM) and C5a-mediated intracellular Ca2+ mobilization (IC50 = 3.1 nM).{34624} W-54011 is selective and does not affect Ca2+ mobilization mediated by other G protein-coupled receptor (GPCR) ligands, N-Formyl-Met-Leu-Phe (fMLF; Item No. 21495), or IL-8 up to a concentration of 10 μM.{34624} It inhibits Ca2+ mobilization in neutrophils in humans, cynomolgus monkeys, and gerbils, but not in mice, rats, guinea pigs, rabbits, or dogs.{34624} At 10 nM, W-54011 also inhibits C5a-mediated migration and vessel formation of human microvascular endothelial cells (HMEC-1).{34625}  

     

    Brand:
    Cayman
    SKU:21231 -

    Out of stock

  • W-54011 is an orally bioavailable, nonpeptide antagonist of complement component 5a receptor 1 (C5aR), also known as cluster of differentiation 88 (CD88).{34624} W-54011 inhibits 125I-rhC5a binding in neutrophils (Ki = 2.2 nM) and C5a-mediated intracellular Ca2+ mobilization (IC50 = 3.1 nM).{34624} W-54011 is selective and does not affect Ca2+ mobilization mediated by other G protein-coupled receptor (GPCR) ligands, N-Formyl-Met-Leu-Phe (fMLF; Item No. 21495), or IL-8 up to a concentration of 10 μM.{34624} It inhibits Ca2+ mobilization in neutrophils in humans, cynomolgus monkeys, and gerbils, but not in mice, rats, guinea pigs, rabbits, or dogs.{34624} At 10 nM, W-54011 also inhibits C5a-mediated migration and vessel formation of human microvascular endothelial cells (HMEC-1).{34625}  

     

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    Cayman
    SKU:21231 -

    Out of stock

  • Calmodulin is a calcium-dependent protein that regulates the activity of a diverse array of enzymes, ion channels, and other proteins and thus has diverse roles in cell function.{23723,23722} W-7 is a cell-permeable antagonist of calmodulin (Ki = 11 μM).{23720,22382} Two molecules of W-7 bind to calcium-binding domains in each calmodulin molecule, blocking its interaction with target proteins.{23720} W-7 also associates, at lower affinities, with calcium-binding domains of other proteins, including troponin C and myosin light chain kinase (Ki = 70 and 300 μM, respectively).{23724,23721,23719}  

     

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  • Calmodulin is a calcium-dependent protein that regulates the activity of a diverse array of enzymes, ion channels, and other proteins and thus has diverse roles in cell function.{23723,23722} W-7 is a cell-permeable antagonist of calmodulin (Ki = 11 μM).{23720,22382} Two molecules of W-7 bind to calcium-binding domains in each calmodulin molecule, blocking its interaction with target proteins.{23720} W-7 also associates, at lower affinities, with calcium-binding domains of other proteins, including troponin C and myosin light chain kinase (Ki = 70 and 300 μM, respectively).{23724,23721,23719}  

     

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  • Calmodulin is a calcium-dependent protein that regulates the activity of a diverse array of enzymes, ion channels, and other proteins and thus has diverse roles in cell function.{23723,23722} W-7 is a cell-permeable antagonist of calmodulin (Ki = 11 μM).{23720,22382} Two molecules of W-7 bind to calcium-binding domains in each calmodulin molecule, blocking its interaction with target proteins.{23720} W-7 also associates, at lower affinities, with calcium-binding domains of other proteins, including troponin C and myosin light chain kinase (Ki = 70 and 300 μM, respectively).{23724,23721,23719}  

     

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    Cayman
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  • Sphingosine-1-phosphate (S1P) modulates skin, vascular endothelial, and immune cells via five distinct G protein-coupled receptors. The S1P type 1 receptor, S1P1, also known as EDG-1, mediates endothelial, lymphoid, and neuronal cell responses to S1P, as well as the synthetic agonist FTY720. W123 is an analog of FTY720 that is a competitive antagonist of S1P1, as measured by GTPγS activation, mitogen-activated protein kinase recruitment, cell migration, and ligand-induced receptor internalization.{16463} It has a Ki value of 0.69 μM when assessed by SEW2871-induced activation of S1P1.{16463} Its specificity for other S1P receptor subtypes remains to be determined.  

     

    Brand:
    Cayman
    SKU:10010992 - 1 mg

    Available on backorder

  • Sphingosine-1-phosphate (S1P) modulates skin, vascular endothelial, and immune cells via five distinct G protein-coupled receptors. The S1P type 1 receptor, S1P1, also known as EDG-1, mediates endothelial, lymphoid, and neuronal cell responses to S1P, as well as the synthetic agonist FTY720. W123 is an analog of FTY720 that is a competitive antagonist of S1P1, as measured by GTPγS activation, mitogen-activated protein kinase recruitment, cell migration, and ligand-induced receptor internalization.{16463} It has a Ki value of 0.69 μM when assessed by SEW2871-induced activation of S1P1.{16463} Its specificity for other S1P receptor subtypes remains to be determined.  

     

    Brand:
    Cayman
    SKU:10010992 - 10 mg

    Available on backorder

  • Sphingosine-1-phosphate (S1P) modulates skin, vascular endothelial, and immune cells via five distinct G protein-coupled receptors. The S1P type 1 receptor, S1P1, also known as EDG-1, mediates endothelial, lymphoid, and neuronal cell responses to S1P, as well as the synthetic agonist FTY720. W123 is an analog of FTY720 that is a competitive antagonist of S1P1, as measured by GTPγS activation, mitogen-activated protein kinase recruitment, cell migration, and ligand-induced receptor internalization.{16463} It has a Ki value of 0.69 μM when assessed by SEW2871-induced activation of S1P1.{16463} Its specificity for other S1P receptor subtypes remains to be determined.  

     

    Brand:
    Cayman
    SKU:10010992 - 5 mg

    Available on backorder

  • Sphingosine-1-phosphate (S1P) is a bioactive lipid that exhibits a broad spectrum of biological activities including cell proliferation, survival, migration, cytoskeletal organization, and morphogenesis.{11895,12477,10628} It exerts its activity by binding to five distinct G protein-coupled receptors, S1P1/EDG-1, S1P2/EDG-5, S1P3/EDG-3, S1P4/EDG-6, and S1P5/EDG-8.{11895,12477} W140 is an inactive enantiomer of W146, a selective S1P1 antagonist (Ki = 77 nM), that binds to the S1P1 receptor with a Ki of 4.6 µM (2a = W146; 2b = W140 in supplemental material).{14254} It exhibits no biological activity in vivo and can therefore serve as an effective control compound for experiments involving W146.  

     

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    Cayman
    SKU:10009110 - 1 mg

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  • Sphingosine-1-phosphate (S1P) is a bioactive lipid that exhibits a broad spectrum of biological activities including cell proliferation, survival, migration, cytoskeletal organization, and morphogenesis.{11895,12477,10628} It exerts its activity by binding to five distinct G protein-coupled receptors, S1P1/EDG-1, S1P2/EDG-5, S1P3/EDG-3, S1P4/EDG-6, and S1P5/EDG-8.{11895,12477} W140 is an inactive enantiomer of W146, a selective S1P1 antagonist (Ki = 77 nM), that binds to the S1P1 receptor with a Ki of 4.6 µM (2a = W146; 2b = W140 in supplemental material).{14254} It exhibits no biological activity in vivo and can therefore serve as an effective control compound for experiments involving W146.  

     

    Brand:
    Cayman
    SKU:10009110 - 10 mg

    Available on backorder

  • Sphingosine-1-phosphate (S1P) is a bioactive lipid that exhibits a broad spectrum of biological activities including cell proliferation, survival, migration, cytoskeletal organization, and morphogenesis.{11895,12477,10628} It exerts its activity by binding to five distinct G protein-coupled receptors, S1P1/EDG-1, S1P2/EDG-5, S1P3/EDG-3, S1P4/EDG-6, and S1P5/EDG-8.{11895,12477} W140 is an inactive enantiomer of W146, a selective S1P1 antagonist (Ki = 77 nM), that binds to the S1P1 receptor with a Ki of 4.6 µM (2a = W146; 2b = W140 in supplemental material).{14254} It exhibits no biological activity in vivo and can therefore serve as an effective control compound for experiments involving W146.  

     

    Brand:
    Cayman
    SKU:10009110 - 5 mg

    Available on backorder

  • Sphingosine-1-phosphate (S1P) is a bioactive lipid that exhibits a broad spectrum of biological activities including cell proliferation, survival, migration, cytoskeletal organization, and morphogenesis.{11895,12477,10628} It exerts its activity by binding to five distinct G protein-coupled receptors, S1P1/EDG-1, S1P2/EDG-5, S1P3/EDG-3, S1P4/EDG-6, and S1P5/EDG-8.{11895,12477} W140 is an inactive enantiomer of W146, a selective S1P1 antagonist (Ki = 77 nM), that binds to the S1P1 receptor with a Ki of 4.6 µM (2a = W146; 2b = W140 in supplemental material).{14254} It exhibits no biological activity in vivo and can therefore serve as an effective control compound for experiments involving W146.  

     

    Brand:
    Cayman
    SKU:10009110 - 500 µg

    Available on backorder

  • Sphingosine-1-phosphate (S1P) is a bioactive lipid that exhibits a broad spectrum of biological activities including cell proliferation, survival, migration, cytoskeletal organization, and morphogenesis.{11895,12477,10628} It exerts its activity by binding to five distinct G protein-coupled receptors, S1P1/EDG-1, S1P2/EDG-5, S1P3/EDG-3, S1P4/EDG-6, and S1P5/EDG-8.{11895,12477} W146 is a S1P1 receptor antagonist that exhibits a Ki value of 77 nM for the human receptor in a GTP-γS binding assay with equipotency at the murine S1P1 receptor (2a = W146; 2b = W140 in supplemental material).{14254} No agonist or antagonist activity was observed at 10 µM W146 at S1P2, S1P3, or S1P5 receptors. W146 is active in vivo causing skin capillary leakage in murine lung and skin as well as inhibition of S1P1 agonist-induced lymphocyte sequestration. The half-life of W146 in rat blood is 73 minutes.  

     

    Brand:
    Cayman
    SKU:10009109 - 1 mg

    Available on backorder

  • Sphingosine-1-phosphate (S1P) is a bioactive lipid that exhibits a broad spectrum of biological activities including cell proliferation, survival, migration, cytoskeletal organization, and morphogenesis.{11895,12477,10628} It exerts its activity by binding to five distinct G protein-coupled receptors, S1P1/EDG-1, S1P2/EDG-5, S1P3/EDG-3, S1P4/EDG-6, and S1P5/EDG-8.{11895,12477} W146 is a S1P1 receptor antagonist that exhibits a Ki value of 77 nM for the human receptor in a GTP-γS binding assay with equipotency at the murine S1P1 receptor (2a = W146; 2b = W140 in supplemental material).{14254} No agonist or antagonist activity was observed at 10 µM W146 at S1P2, S1P3, or S1P5 receptors. W146 is active in vivo causing skin capillary leakage in murine lung and skin as well as inhibition of S1P1 agonist-induced lymphocyte sequestration. The half-life of W146 in rat blood is 73 minutes.  

     

    Brand:
    Cayman
    SKU:10009109 - 10 mg

    Available on backorder

  • Sphingosine-1-phosphate (S1P) is a bioactive lipid that exhibits a broad spectrum of biological activities including cell proliferation, survival, migration, cytoskeletal organization, and morphogenesis.{11895,12477,10628} It exerts its activity by binding to five distinct G protein-coupled receptors, S1P1/EDG-1, S1P2/EDG-5, S1P3/EDG-3, S1P4/EDG-6, and S1P5/EDG-8.{11895,12477} W146 is a S1P1 receptor antagonist that exhibits a Ki value of 77 nM for the human receptor in a GTP-γS binding assay with equipotency at the murine S1P1 receptor (2a = W146; 2b = W140 in supplemental material).{14254} No agonist or antagonist activity was observed at 10 µM W146 at S1P2, S1P3, or S1P5 receptors. W146 is active in vivo causing skin capillary leakage in murine lung and skin as well as inhibition of S1P1 agonist-induced lymphocyte sequestration. The half-life of W146 in rat blood is 73 minutes.  

     

    Brand:
    Cayman
    SKU:10009109 - 5 mg

    Available on backorder

  • Sphingosine-1-phosphate (S1P) is a bioactive lipid that exhibits a broad spectrum of biological activities including cell proliferation, survival, migration, cytoskeletal organization, and morphogenesis.{11895,12477,10628} It exerts its activity by binding to five distinct G protein-coupled receptors, S1P1/EDG-1, S1P2/EDG-5, S1P3/EDG-3, S1P4/EDG-6, and S1P5/EDG-8.{11895,12477} W146 is a S1P1 receptor antagonist that exhibits a Ki value of 77 nM for the human receptor in a GTP-γS binding assay with equipotency at the murine S1P1 receptor (2a = W146; 2b = W140 in supplemental material).{14254} No agonist or antagonist activity was observed at 10 µM W146 at S1P2, S1P3, or S1P5 receptors. W146 is active in vivo causing skin capillary leakage in murine lung and skin as well as inhibition of S1P1 agonist-induced lymphocyte sequestration. The half-life of W146 in rat blood is 73 minutes.  

     

    Brand:
    Cayman
    SKU:10009109 - 500 µg

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  • Walrycin B is an antibiotic that has activity against Gram-positive bacteria (MICs = 0.39 and 3.13 μg/ml for B. subtilis and S. aureus, respectively) via inhibition of WalR, a response regulator that is essential to bacterial viability.{37399} It inhibits WalR-induced repression of EGFP signaling in a reporter assay in a concentration-dependent manner. Walrycin B alters expression of WalR regulon genes, decreasing ydjM, yocH, and ycvE and increasing yoeB and yjeA expression in B. subtilis. It also halts transcription of isaA and ssaA in S. aureus. Overexpression of WalR induces a 4- and 2-fold increase in the MIC against B. subtilis and S. aureus, respectively, indicating cell death is induced specifically through inhibition of WalR by walrycin B.  

     

    Brand:
    Cayman
    SKU:21566 -

    Out of stock

  • Walrycin B is an antibiotic that has activity against Gram-positive bacteria (MICs = 0.39 and 3.13 μg/ml for B. subtilis and S. aureus, respectively) via inhibition of WalR, a response regulator that is essential to bacterial viability.{37399} It inhibits WalR-induced repression of EGFP signaling in a reporter assay in a concentration-dependent manner. Walrycin B alters expression of WalR regulon genes, decreasing ydjM, yocH, and ycvE and increasing yoeB and yjeA expression in B. subtilis. It also halts transcription of isaA and ssaA in S. aureus. Overexpression of WalR induces a 4- and 2-fold increase in the MIC against B. subtilis and S. aureus, respectively, indicating cell death is induced specifically through inhibition of WalR by walrycin B.  

     

    Brand:
    Cayman
    SKU:21566 -

    Out of stock

  • Walrycin B is an antibiotic that has activity against Gram-positive bacteria (MICs = 0.39 and 3.13 μg/ml for B. subtilis and S. aureus, respectively) via inhibition of WalR, a response regulator that is essential to bacterial viability.{37399} It inhibits WalR-induced repression of EGFP signaling in a reporter assay in a concentration-dependent manner. Walrycin B alters expression of WalR regulon genes, decreasing ydjM, yocH, and ycvE and increasing yoeB and yjeA expression in B. subtilis. It also halts transcription of isaA and ssaA in S. aureus. Overexpression of WalR induces a 4- and 2-fold increase in the MIC against B. subtilis and S. aureus, respectively, indicating cell death is induced specifically through inhibition of WalR by walrycin B.  

     

    Brand:
    Cayman
    SKU:21566 -

    Out of stock

  • Walrycin B is an antibiotic that has activity against Gram-positive bacteria (MICs = 0.39 and 3.13 μg/ml for B. subtilis and S. aureus, respectively) via inhibition of WalR, a response regulator that is essential to bacterial viability.{37399} It inhibits WalR-induced repression of EGFP signaling in a reporter assay in a concentration-dependent manner. Walrycin B alters expression of WalR regulon genes, decreasing ydjM, yocH, and ycvE and increasing yoeB and yjeA expression in B. subtilis. It also halts transcription of isaA and ssaA in S. aureus. Overexpression of WalR induces a 4- and 2-fold increase in the MIC against B. subtilis and S. aureus, respectively, indicating cell death is induced specifically through inhibition of WalR by walrycin B.  

     

    Brand:
    Cayman
    SKU:21566 -

    Out of stock

  • WAY-100635 is a potent, silent antagonist of serotonin 5-HT1A receptors with an IC50 value of 2.2 nM (Ki = 0.8 nM) for inhibiting 5-HT1A receptors in rat hippocampal membranes.{23126,23127} Because it displays 100-fold selectivity for 5-HT1A over other 5-HT subtypes, WAY-100635 is classically used to examine the distribution and function of 5-HT1A receptors.{23128} However, WAY-100635 has also been shown to exhibit agonist activity at dopamine D4 receptors (Kd = 2.4 nM).{23125}  

     

    Brand:
    Cayman
    SKU:-
  • WAY-100635 is a potent, silent antagonist of serotonin 5-HT1A receptors with an IC50 value of 2.2 nM (Ki = 0.8 nM) for inhibiting 5-HT1A receptors in rat hippocampal membranes.{23126,23127} Because it displays 100-fold selectivity for 5-HT1A over other 5-HT subtypes, WAY-100635 is classically used to examine the distribution and function of 5-HT1A receptors.{23128} However, WAY-100635 has also been shown to exhibit agonist activity at dopamine D4 receptors (Kd = 2.4 nM).{23125}  

     

    Brand:
    Cayman
    SKU:-
  • WAY-100635 is a potent, silent antagonist of serotonin 5-HT1A receptors with an IC50 value of 2.2 nM (Ki = 0.8 nM) for inhibiting 5-HT1A receptors in rat hippocampal membranes.{23126,23127} Because it displays 100-fold selectivity for 5-HT1A over other 5-HT subtypes, WAY-100635 is classically used to examine the distribution and function of 5-HT1A receptors.{23128} However, WAY-100635 has also been shown to exhibit agonist activity at dopamine D4 receptors (Kd = 2.4 nM).{23125}  

     

    Brand:
    Cayman
    SKU:-
  • WAY-161503 is a full agonist of 5-HT2C receptors (Ki = 3.3 nM for displacement of DOI (Item No. 13885)).{30043} Relative to 5-HT2C receptor binding, WAY-161503 is ~6-fold less potent at 5-HT2A receptors (Ki = 18 nM) and 20-fold less potent at 5-HT2B receptors (Ki = 60 nM).{30043} In functional studies, WAY-161503 can stimulate calcium mobilization coupled to 5-HT2C, 2B, and 2A receptors with EC50 values of 0.8, 1.8, and 7 nM, respectively.{30043} WAY-161503 has been reported to produce dose-dependent decreases in food intake in 24-hour fasted normal Sprague-Dawley rats, diet-induced obese mice, and obese Zucker rats with ED50 values of 1.9, 6.8, and 0.73 mg/kg, respectively.{30043} This compound has been used to examine the role of 5-HT2C receptors in rodent models of depression, locomotion, reinforcement, or motivated behaviors.{30041,30042}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • WAY-161503 is a full agonist of 5-HT2C receptors (Ki = 3.3 nM for displacement of DOI (Item No. 13885)).{30043} Relative to 5-HT2C receptor binding, WAY-161503 is ~6-fold less potent at 5-HT2A receptors (Ki = 18 nM) and 20-fold less potent at 5-HT2B receptors (Ki = 60 nM).{30043} In functional studies, WAY-161503 can stimulate calcium mobilization coupled to 5-HT2C, 2B, and 2A receptors with EC50 values of 0.8, 1.8, and 7 nM, respectively.{30043} WAY-161503 has been reported to produce dose-dependent decreases in food intake in 24-hour fasted normal Sprague-Dawley rats, diet-induced obese mice, and obese Zucker rats with ED50 values of 1.9, 6.8, and 0.73 mg/kg, respectively.{30043} This compound has been used to examine the role of 5-HT2C receptors in rodent models of depression, locomotion, reinforcement, or motivated behaviors.{30041,30042}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • WAY-161503 is a full agonist of 5-HT2C receptors (Ki = 3.3 nM for displacement of DOI (Item No. 13885)).{30043} Relative to 5-HT2C receptor binding, WAY-161503 is ~6-fold less potent at 5-HT2A receptors (Ki = 18 nM) and 20-fold less potent at 5-HT2B receptors (Ki = 60 nM).{30043} In functional studies, WAY-161503 can stimulate calcium mobilization coupled to 5-HT2C, 2B, and 2A receptors with EC50 values of 0.8, 1.8, and 7 nM, respectively.{30043} WAY-161503 has been reported to produce dose-dependent decreases in food intake in 24-hour fasted normal Sprague-Dawley rats, diet-induced obese mice, and obese Zucker rats with ED50 values of 1.9, 6.8, and 0.73 mg/kg, respectively.{30043} This compound has been used to examine the role of 5-HT2C receptors in rodent models of depression, locomotion, reinforcement, or motivated behaviors.{30041,30042}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • WAY-161503 is a full agonist of 5-HT2C receptors (Ki = 3.3 nM for displacement of DOI (Item No. 13885)).{30043} Relative to 5-HT2C receptor binding, WAY-161503 is ~6-fold less potent at 5-HT2A receptors (Ki = 18 nM) and 20-fold less potent at 5-HT2B receptors (Ki = 60 nM).{30043} In functional studies, WAY-161503 can stimulate calcium mobilization coupled to 5-HT2C, 2B, and 2A receptors with EC50 values of 0.8, 1.8, and 7 nM, respectively.{30043} WAY-161503 has been reported to produce dose-dependent decreases in food intake in 24-hour fasted normal Sprague-Dawley rats, diet-induced obese mice, and obese Zucker rats with ED50 values of 1.9, 6.8, and 0.73 mg/kg, respectively.{30043} This compound has been used to examine the role of 5-HT2C receptors in rodent models of depression, locomotion, reinforcement, or motivated behaviors.{30041,30042}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • WAY-200070 is a potent and selective agonist of estrogen receptor β (ERβ; IC50s = 2 and 187 nM for human full-length ERβ and ERα, respectively).{39360} WAY-200070 (30 mg/kg, s.c. in mice) induces nuclear translocation of ERβ and increases c-fos activation and dopamine levels in the striatum four hours after administration.{39359} At the same dose, it decreases depressive-like behavior in the tail suspension test. It has anxiolytic effects in mice using the four-plate and stress-induced hyperthermia tests and in zebrafish larvae using a light-dark choice behavior test.{39359,39358} In addition, WAY-200070 improves glucose and insulin sensitivity in mouse models of diabetes.{39357}  

     

    Brand:
    Cayman
    SKU:23323 - 10 mg

    Available on backorder

  • WAY-200070 is a potent and selective agonist of estrogen receptor β (ERβ; IC50s = 2 and 187 nM for human full-length ERβ and ERα, respectively).{39360} WAY-200070 (30 mg/kg, s.c. in mice) induces nuclear translocation of ERβ and increases c-fos activation and dopamine levels in the striatum four hours after administration.{39359} At the same dose, it decreases depressive-like behavior in the tail suspension test. It has anxiolytic effects in mice using the four-plate and stress-induced hyperthermia tests and in zebrafish larvae using a light-dark choice behavior test.{39359,39358} In addition, WAY-200070 improves glucose and insulin sensitivity in mouse models of diabetes.{39357}  

     

    Brand:
    Cayman
    SKU:23323 - 25 mg

    Available on backorder

  • WAY-200070 is a potent and selective agonist of estrogen receptor β (ERβ; IC50s = 2 and 187 nM for human full-length ERβ and ERα, respectively).{39360} WAY-200070 (30 mg/kg, s.c. in mice) induces nuclear translocation of ERβ and increases c-fos activation and dopamine levels in the striatum four hours after administration.{39359} At the same dose, it decreases depressive-like behavior in the tail suspension test. It has anxiolytic effects in mice using the four-plate and stress-induced hyperthermia tests and in zebrafish larvae using a light-dark choice behavior test.{39359,39358} In addition, WAY-200070 improves glucose and insulin sensitivity in mouse models of diabetes.{39357}  

     

    Brand:
    Cayman
    SKU:23323 - 5 mg

    Available on backorder

  • WAY-200070 is a potent and selective agonist of estrogen receptor β (ERβ; IC50s = 2 and 187 nM for human full-length ERβ and ERα, respectively).{39360} WAY-200070 (30 mg/kg, s.c. in mice) induces nuclear translocation of ERβ and increases c-fos activation and dopamine levels in the striatum four hours after administration.{39359} At the same dose, it decreases depressive-like behavior in the tail suspension test. It has anxiolytic effects in mice using the four-plate and stress-induced hyperthermia tests and in zebrafish larvae using a light-dark choice behavior test.{39359,39358} In addition, WAY-200070 improves glucose and insulin sensitivity in mouse models of diabetes.{39357}  

     

    Brand:
    Cayman
    SKU:23323 - 50 mg

    Available on backorder

  • WAY-208466 is a selective 5-HT6 receptor agonist (EC50 = 7.3 nM at the human 5-HT6 receptor).{32648} It has been shown to increase cortical GABA levels in rat frontal cortex, producing anxiolytic-like effects in vivo. {32648}  

     

    Brand:
    Cayman
    SKU:11938 - 1 mg

    Available on backorder

  • WAY-208466 is a selective 5-HT6 receptor agonist (EC50 = 7.3 nM at the human 5-HT6 receptor).{32648} It has been shown to increase cortical GABA levels in rat frontal cortex, producing anxiolytic-like effects in vivo. {32648}  

     

    Brand:
    Cayman
    SKU:11938 - 10 mg

    Available on backorder

  • WAY-208466 is a selective 5-HT6 receptor agonist (EC50 = 7.3 nM at the human 5-HT6 receptor).{32648} It has been shown to increase cortical GABA levels in rat frontal cortex, producing anxiolytic-like effects in vivo. {32648}  

     

    Brand:
    Cayman
    SKU:11938 - 25 mg

    Available on backorder

  • WAY-208466 is a selective 5-HT6 receptor agonist (EC50 = 7.3 nM at the human 5-HT6 receptor).{32648} It has been shown to increase cortical GABA levels in rat frontal cortex, producing anxiolytic-like effects in vivo. {32648}  

     

    Brand:
    Cayman
    SKU:11938 - 5 mg

    Available on backorder

  • Wnt signaling proteins are small secreted proteins that are active in embryonic development, tissue homeostasis, and tumorigenesis.{14336,13185,17947} Dickkopf-1 (Dkk1) antagonizes Wnt signaling and has important roles in bone formation, cancer, and Alzheimer’s disease.{30956} WAY-262611 is an inhibitor of Dkk1 that activates the Wnt signaling pathway, stimulating β-catenin/TCF-dependent transcription with an EC50 value of 0.63 µM.{30957} It has good pharmacokinetic properties and increases trabecular bone formation in ovariectomized rats following oral administration.{30957} WAY-262611 has been used to elucidate the role of Dkk1 in modulating Wnt signaling, particularly in the context of arthritis.{30955,30954}  

     

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    Cayman
    SKU:-

    Available on backorder

  • Wnt signaling proteins are small secreted proteins that are active in embryonic development, tissue homeostasis, and tumorigenesis.{14336,13185,17947} Dickkopf-1 (Dkk1) antagonizes Wnt signaling and has important roles in bone formation, cancer, and Alzheimer’s disease.{30956} WAY-262611 is an inhibitor of Dkk1 that activates the Wnt signaling pathway, stimulating β-catenin/TCF-dependent transcription with an EC50 value of 0.63 µM.{30957} It has good pharmacokinetic properties and increases trabecular bone formation in ovariectomized rats following oral administration.{30957} WAY-262611 has been used to elucidate the role of Dkk1 in modulating Wnt signaling, particularly in the context of arthritis.{30955,30954}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Wnt signaling proteins are small secreted proteins that are active in embryonic development, tissue homeostasis, and tumorigenesis.{14336,13185,17947} Dickkopf-1 (Dkk1) antagonizes Wnt signaling and has important roles in bone formation, cancer, and Alzheimer’s disease.{30956} WAY-262611 is an inhibitor of Dkk1 that activates the Wnt signaling pathway, stimulating β-catenin/TCF-dependent transcription with an EC50 value of 0.63 µM.{30957} It has good pharmacokinetic properties and increases trabecular bone formation in ovariectomized rats following oral administration.{30957} WAY-262611 has been used to elucidate the role of Dkk1 in modulating Wnt signaling, particularly in the context of arthritis.{30955,30954}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Wnt signaling proteins are small secreted proteins that are active in embryonic development, tissue homeostasis, and tumorigenesis.{14336,13185,17947} Dickkopf-1 (Dkk1) antagonizes Wnt signaling and has important roles in bone formation, cancer, and Alzheimer’s disease.{30956} WAY-262611 is an inhibitor of Dkk1 that activates the Wnt signaling pathway, stimulating β-catenin/TCF-dependent transcription with an EC50 value of 0.63 µM.{30957} It has good pharmacokinetic properties and increases trabecular bone formation in ovariectomized rats following oral administration.{30957} WAY-262611 has been used to elucidate the role of Dkk1 in modulating Wnt signaling, particularly in the context of arthritis.{30955,30954}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • WAY-316606 is an inhibitor of secreted frizzled-related protein 1 (sFRP-1; IC50 = 0.5 μM).{36980} It increases Wnt signaling in U2OS osteosarcoma cells (EC50 = 0.65 μM). WAY-316606 increases total bone area in a murine calvarial organ culture assay when used at concentrations greater than 0.1 nM.{36981}  

     

    Brand:
    Cayman
    SKU:26324 - 1 mg

    Available on backorder

  • WAY-316606 is an inhibitor of secreted frizzled-related protein 1 (sFRP-1; IC50 = 0.5 μM).{36980} It increases Wnt signaling in U2OS osteosarcoma cells (EC50 = 0.65 μM). WAY-316606 increases total bone area in a murine calvarial organ culture assay when used at concentrations greater than 0.1 nM.{36981}  

     

    Brand:
    Cayman
    SKU:26324 - 10 mg

    Available on backorder

  • WAY-316606 is an inhibitor of secreted frizzled-related protein 1 (sFRP-1; IC50 = 0.5 μM).{36980} It increases Wnt signaling in U2OS osteosarcoma cells (EC50 = 0.65 μM). WAY-316606 increases total bone area in a murine calvarial organ culture assay when used at concentrations greater than 0.1 nM.{36981}  

     

    Brand:
    Cayman
    SKU:26324 - 5 mg

    Available on backorder

  • WAY-600 is an inhibitor of mammalian target of rapamycin (mTOR; IC50 = 0.009 µM).{52139} It selectively inhibits mTOR over PI3Kα and PI3Kɣ (IC50s = 1.96 and 8.45 µM, respectively) and 24 additional lipid and protein kinases in a panel (IC50s = >50 µM for all). WAY-600 decreases phosphorylation of the mTORC1 and mTORC2 substrates Akt and S6 kinase (S6K1), respectively, in a cell-free assay when used at concentrations of 0.2, 1, and 5 µM. It decreases proliferation of nine cancer cell lines, including breast, prostate, glioma, kidney, and colorectal cancer cells, with IC50 values ranging from 0.6 to 2.5 µM. WAY-600 reduces tumor growth in a HepG2 mouse xenograft model when administered at a dose of 10 mg/kg for 14 days.{52140}  

     

    Brand:
    Cayman
    SKU:29214 - 1 mg

    Available on backorder

  • WAY-600 is an inhibitor of mammalian target of rapamycin (mTOR; IC50 = 0.009 µM).{52139} It selectively inhibits mTOR over PI3Kα and PI3Kɣ (IC50s = 1.96 and 8.45 µM, respectively) and 24 additional lipid and protein kinases in a panel (IC50s = >50 µM for all). WAY-600 decreases phosphorylation of the mTORC1 and mTORC2 substrates Akt and S6 kinase (S6K1), respectively, in a cell-free assay when used at concentrations of 0.2, 1, and 5 µM. It decreases proliferation of nine cancer cell lines, including breast, prostate, glioma, kidney, and colorectal cancer cells, with IC50 values ranging from 0.6 to 2.5 µM. WAY-600 reduces tumor growth in a HepG2 mouse xenograft model when administered at a dose of 10 mg/kg for 14 days.{52140}  

     

    Brand:
    Cayman
    SKU:29214 - 10 mg

    Available on backorder

  • WAY-600 is an inhibitor of mammalian target of rapamycin (mTOR; IC50 = 0.009 µM).{52139} It selectively inhibits mTOR over PI3Kα and PI3Kɣ (IC50s = 1.96 and 8.45 µM, respectively) and 24 additional lipid and protein kinases in a panel (IC50s = >50 µM for all). WAY-600 decreases phosphorylation of the mTORC1 and mTORC2 substrates Akt and S6 kinase (S6K1), respectively, in a cell-free assay when used at concentrations of 0.2, 1, and 5 µM. It decreases proliferation of nine cancer cell lines, including breast, prostate, glioma, kidney, and colorectal cancer cells, with IC50 values ranging from 0.6 to 2.5 µM. WAY-600 reduces tumor growth in a HepG2 mouse xenograft model when administered at a dose of 10 mg/kg for 14 days.{52140}  

     

    Brand:
    Cayman
    SKU:29214 - 5 mg

    Available on backorder

  • WB 4101 is an antagonist of α-adrenergic receptors (α-ARs).{57351} It inhibits norepinephrine-induced contraction of isolated rat vas deferens (pA2 = 9.8). WB 4101 also inhibits contractions induced by carbachol (carbamoylcholine; Item No. 14486) in isolated guinea pig taenia caeci (pA2 = 8.9).{57352}  

     

    Brand:
    Cayman
    SKU:29528 - 100 mg

    Available on backorder

  • WB 4101 is an antagonist of α-adrenergic receptors (α-ARs).{57351} It inhibits norepinephrine-induced contraction of isolated rat vas deferens (pA2 = 9.8). WB 4101 also inhibits contractions induced by carbachol (carbamoylcholine; Item No. 14486) in isolated guinea pig taenia caeci (pA2 = 8.9).{57352}  

     

    Brand:
    Cayman
    SKU:29528 - 250 mg

    Available on backorder

  • WB 4101 is an antagonist of α-adrenergic receptors (α-ARs).{57351} It inhibits norepinephrine-induced contraction of isolated rat vas deferens (pA2 = 9.8). WB 4101 also inhibits contractions induced by carbachol (carbamoylcholine; Item No. 14486) in isolated guinea pig taenia caeci (pA2 = 8.9).{57352}  

     

    Brand:
    Cayman
    SKU:29528 - 50 mg

    Available on backorder

  • WD-repeat protein 5 (WDR5) is a scaffold protein commonly involved in the formation of nucleosome-modifying protein complexes with histones.{22296} For example, WDR5 is a component of a mixed-lineage leukemia (MLL) methyltransferase complex that targets histone 3.{20287} WDR5 can also be a component of histone acetyltransferase complexes and can directly bind methylated as well as unmodified histones.{24221,22296} WDR5-0103 is a small molecule that binds a peptide-binding pocket on WDR5 (Kd = 450 nM), inhibiting the catalytic activity of the MLL core complex in vitro (IC50 = 39 µM).{24219,24220}  

     

    Brand:
    Cayman
    SKU:-
  • WD-repeat protein 5 (WDR5) is a scaffold protein commonly involved in the formation of nucleosome-modifying protein complexes with histones.{22296} For example, WDR5 is a component of a mixed-lineage leukemia (MLL) methyltransferase complex that targets histone 3.{20287} WDR5 can also be a component of histone acetyltransferase complexes and can directly bind methylated as well as unmodified histones.{24221,22296} WDR5-0103 is a small molecule that binds a peptide-binding pocket on WDR5 (Kd = 450 nM), inhibiting the catalytic activity of the MLL core complex in vitro (IC50 = 39 µM).{24219,24220}  

     

    Brand:
    Cayman
    SKU:-
  • WD-repeat protein 5 (WDR5) is a scaffold protein commonly involved in the formation of nucleosome-modifying protein complexes with histones.{22296} For example, WDR5 is a component of a mixed-lineage leukemia (MLL) methyltransferase complex that targets histone 3.{20287} WDR5 can also be a component of histone acetyltransferase complexes and can directly bind methylated as well as unmodified histones.{24221,22296} WDR5-0103 is a small molecule that binds a peptide-binding pocket on WDR5 (Kd = 450 nM), inhibiting the catalytic activity of the MLL core complex in vitro (IC50 = 39 µM).{24219,24220}  

     

    Brand:
    Cayman
    SKU:-
  • WD-repeat protein 5 (WDR5) is a scaffold protein commonly involved in the formation of nucleosome-modifying protein complexes with histones.{22296} For example, WDR5 is a component of a mixed-lineage leukemia (MLL) methyltransferase complex that targets histone 3.{20287} WDR5 can also be a component of histone acetyltransferase complexes and can directly bind methylated as well as unmodified histones.{24221,22296} WDR5-0103 is a small molecule that binds a peptide-binding pocket on WDR5 (Kd = 450 nM), inhibiting the catalytic activity of the MLL core complex in vitro (IC50 = 39 µM).{24219,24220}  

     

    Brand:
    Cayman
    SKU:-
  • Wedelolactone is a natural coumestan originally isolated from plants used in herbal therapies. It inhibits NF-κB signaling at the level of IKK action, resulting in suppression of NF-κB-mediated gene expression at concentrations of 1-100 µM.{30948,30949,30944} Wedelolactone can also inhibit hepatitis C virus NS5B RNA-dependent RNA polymerase in vitro (IC50 = 36 µM), STAT1 dephosphorylation (50 µM), and EZH2-EED interactions (Kd = 2.8 µM).{30947,30945,30946} Prolonged incubation of HepG2 liver cells with wedelolactone alters lipid metabolism through increased expression of AMPK, PPARα, lipoprotein lipase, and low-density lipoprotein receptor.{30950}  

     

    Brand:
    Cayman
    SKU:11796 - 1 mg

    Available on backorder

  • Wedelolactone is a natural coumestan originally isolated from plants used in herbal therapies. It inhibits NF-κB signaling at the level of IKK action, resulting in suppression of NF-κB-mediated gene expression at concentrations of 1-100 µM.{30948,30949,30944} Wedelolactone can also inhibit hepatitis C virus NS5B RNA-dependent RNA polymerase in vitro (IC50 = 36 µM), STAT1 dephosphorylation (50 µM), and EZH2-EED interactions (Kd = 2.8 µM).{30947,30945,30946} Prolonged incubation of HepG2 liver cells with wedelolactone alters lipid metabolism through increased expression of AMPK, PPARα, lipoprotein lipase, and low-density lipoprotein receptor.{30950}  

     

    Brand:
    Cayman
    SKU:11796 - 5 mg

    Available on backorder

  • Wedelolactone is a natural coumestan originally isolated from plants used in herbal therapies. It inhibits NF-κB signaling at the level of IKK action, resulting in suppression of NF-κB-mediated gene expression at concentrations of 1-100 µM.{30948,30949,30944} Wedelolactone can also inhibit hepatitis C virus NS5B RNA-dependent RNA polymerase in vitro (IC50 = 36 µM), STAT1 dephosphorylation (50 µM), and EZH2-EED interactions (Kd = 2.8 µM).{30947,30945,30946} Prolonged incubation of HepG2 liver cells with wedelolactone alters lipid metabolism through increased expression of AMPK, PPARα, lipoprotein lipase, and low-density lipoprotein receptor.{30950}  

     

    Brand:
    Cayman
    SKU:11796 - 500 µg

    Available on backorder

  • WEHI-345 is an inhibitor of receptor-interacting protein kinase 2 (RIPK2; IC50 = 130 nM in a kinase assay using human recombinant RIPK2).{41305} It is selective for RIPK2 over RIPK1, 4, and 5 (Kds = 46, >10,000, >10,000, and >10,000 nM, respectively) and a panel of 95 kinases at a concentration of 1 μM. WEHI-345 reduces levels of RIPK2 phosphorylation at Ser176 in bone marrow-derived macrophages (BMDMs) stimulated by muramyl dipeptide (MDP). It decreases MDP-induced transcription of TNF and IL-6 in BMDMs and reduces mRNA levels of the NF-κB target genes TNF, IL-8, IL-1β, and A20 in MDP-stimulated THP-1 cells in a concentration-dependent manner. WEHI-345 (3-10 mg/kg) reduces plasma levels of TNF and delays disease onset in a mouse model of experimental autoimmune encephalomyelitis (EAE).  

     

    Brand:
    Cayman
    SKU:23023 - 1 mg

    Available on backorder

  • WEHI-345 is an inhibitor of receptor-interacting protein kinase 2 (RIPK2; IC50 = 130 nM in a kinase assay using human recombinant RIPK2).{41305} It is selective for RIPK2 over RIPK1, 4, and 5 (Kds = 46, >10,000, >10,000, and >10,000 nM, respectively) and a panel of 95 kinases at a concentration of 1 μM. WEHI-345 reduces levels of RIPK2 phosphorylation at Ser176 in bone marrow-derived macrophages (BMDMs) stimulated by muramyl dipeptide (MDP). It decreases MDP-induced transcription of TNF and IL-6 in BMDMs and reduces mRNA levels of the NF-κB target genes TNF, IL-8, IL-1β, and A20 in MDP-stimulated THP-1 cells in a concentration-dependent manner. WEHI-345 (3-10 mg/kg) reduces plasma levels of TNF and delays disease onset in a mouse model of experimental autoimmune encephalomyelitis (EAE).  

     

    Brand:
    Cayman
    SKU:23023 - 10 mg

    Available on backorder

  • WEHI-345 is an inhibitor of receptor-interacting protein kinase 2 (RIPK2; IC50 = 130 nM in a kinase assay using human recombinant RIPK2).{41305} It is selective for RIPK2 over RIPK1, 4, and 5 (Kds = 46, >10,000, >10,000, and >10,000 nM, respectively) and a panel of 95 kinases at a concentration of 1 μM. WEHI-345 reduces levels of RIPK2 phosphorylation at Ser176 in bone marrow-derived macrophages (BMDMs) stimulated by muramyl dipeptide (MDP). It decreases MDP-induced transcription of TNF and IL-6 in BMDMs and reduces mRNA levels of the NF-κB target genes TNF, IL-8, IL-1β, and A20 in MDP-stimulated THP-1 cells in a concentration-dependent manner. WEHI-345 (3-10 mg/kg) reduces plasma levels of TNF and delays disease onset in a mouse model of experimental autoimmune encephalomyelitis (EAE).  

     

    Brand:
    Cayman
    SKU:23023 - 25 mg

    Available on backorder

  • WEHI-345 is an inhibitor of receptor-interacting protein kinase 2 (RIPK2; IC50 = 130 nM in a kinase assay using human recombinant RIPK2).{41305} It is selective for RIPK2 over RIPK1, 4, and 5 (Kds = 46, >10,000, >10,000, and >10,000 nM, respectively) and a panel of 95 kinases at a concentration of 1 μM. WEHI-345 reduces levels of RIPK2 phosphorylation at Ser176 in bone marrow-derived macrophages (BMDMs) stimulated by muramyl dipeptide (MDP). It decreases MDP-induced transcription of TNF and IL-6 in BMDMs and reduces mRNA levels of the NF-κB target genes TNF, IL-8, IL-1β, and A20 in MDP-stimulated THP-1 cells in a concentration-dependent manner. WEHI-345 (3-10 mg/kg) reduces plasma levels of TNF and delays disease onset in a mouse model of experimental autoimmune encephalomyelitis (EAE).  

     

    Brand:
    Cayman
    SKU:23023 - 5 mg

    Available on backorder

  • WEHI-539 is an inhibitor of Bcl-xL (IC50 = 1.1 nM) that demonstrates more than 400-fold selectivity for Bcl-xL over Bcl-2, Mcl-1, Bcl-W, or A1.{33606} It has been shown to induce apoptosis specifically in Mcl-1 deficient cells and does not affect Bcl-2 overexpressing cells.{33606} WEHI-539 can be used as a tool for distinguishing the roles of Bcl-xL in both normal and cancer cells from those of the related prosurvival proteins such as Bcl-2 and Mcl-1.{33606}  

     

    Brand:
    Cayman
    SKU:21478 -

    Out of stock

  • WEHI-539 is an inhibitor of Bcl-xL (IC50 = 1.1 nM) that demonstrates more than 400-fold selectivity for Bcl-xL over Bcl-2, Mcl-1, Bcl-W, or A1.{33606} It has been shown to induce apoptosis specifically in Mcl-1 deficient cells and does not affect Bcl-2 overexpressing cells.{33606} WEHI-539 can be used as a tool for distinguishing the roles of Bcl-xL in both normal and cancer cells from those of the related prosurvival proteins such as Bcl-2 and Mcl-1.{33606}  

     

    Brand:
    Cayman
    SKU:21478 -

    Out of stock

  • WEHI-539 is an inhibitor of Bcl-xL (IC50 = 1.1 nM) that demonstrates more than 400-fold selectivity for Bcl-xL over Bcl-2, Mcl-1, Bcl-W, or A1.{33606} It has been shown to induce apoptosis specifically in Mcl-1 deficient cells and does not affect Bcl-2 overexpressing cells.{33606} WEHI-539 can be used as a tool for distinguishing the roles of Bcl-xL in both normal and cancer cells from those of the related prosurvival proteins such as Bcl-2 and Mcl-1.{33606}  

     

    Brand:
    Cayman
    SKU:21478 -

    Out of stock

  • WH-4-023 is a selective inhibitor of the Src family of non-receptor tyrosine kinases (IC50s = 2 and 6 nM for Lck and Src, respectively).{32088,32089} It inhibits the related kinases p38α and KDR at >300-fold higher concentrations (IC50s = 1.3 and 0.65 µM, respectively).{32088} At 1 µM, it has been used in combination with PD 0325901 (Item No. 13034), CHIR99021 (Item No. 13122), and SB-590885 (Item No. 16643) to support self-renewal of naïve human embryonic stem cells.{32090}  

     

    Brand:
    Cayman
    SKU:9002067 - 1 mg

    Available on backorder

  • WH-4-023 is a selective inhibitor of the Src family of non-receptor tyrosine kinases (IC50s = 2 and 6 nM for Lck and Src, respectively).{32088,32089} It inhibits the related kinases p38α and KDR at >300-fold higher concentrations (IC50s = 1.3 and 0.65 µM, respectively).{32088} At 1 µM, it has been used in combination with PD 0325901 (Item No. 13034), CHIR99021 (Item No. 13122), and SB-590885 (Item No. 16643) to support self-renewal of naïve human embryonic stem cells.{32090}  

     

    Brand:
    Cayman
    SKU:9002067 - 10 mg

    Available on backorder

  • WH-4-023 is a selective inhibitor of the Src family of non-receptor tyrosine kinases (IC50s = 2 and 6 nM for Lck and Src, respectively).{32088,32089} It inhibits the related kinases p38α and KDR at >300-fold higher concentrations (IC50s = 1.3 and 0.65 µM, respectively).{32088} At 1 µM, it has been used in combination with PD 0325901 (Item No. 13034), CHIR99021 (Item No. 13122), and SB-590885 (Item No. 16643) to support self-renewal of naïve human embryonic stem cells.{32090}  

     

    Brand:
    Cayman
    SKU:9002067 - 25 mg

    Available on backorder

  • WH-4-023 is a selective inhibitor of the Src family of non-receptor tyrosine kinases (IC50s = 2 and 6 nM for Lck and Src, respectively).{32088,32089} It inhibits the related kinases p38α and KDR at >300-fold higher concentrations (IC50s = 1.3 and 0.65 µM, respectively).{32088} At 1 µM, it has been used in combination with PD 0325901 (Item No. 13034), CHIR99021 (Item No. 13122), and SB-590885 (Item No. 16643) to support self-renewal of naïve human embryonic stem cells.{32090}  

     

    Brand:
    Cayman
    SKU:9002067 - 5 mg

    Available on backorder

  • Janus kinase 3 (JAK3) is a cytoplasmic protein tyrosine kinase that functions in the initiation of cytokine-triggered signal transduction by catalyzing the phosphorylation of signal transduction and activators of transcription (STATs). JAK3 is abundantly expressed in normal lymphoid cells as well as human lymphoblastic and myeloblastic leukemia cells. WHI-P131 selectively inhibits the tyrosine kinase activity of JAK3 with an IC50 value of 78 µM without affecting the enzymatic activity of JAK1, JAK2, or other protein tyrosine kinases (IC50 ≥350 µM).{16507} WHI-P131 induces apoptosis in JAK3-expressing human leukemia cell lines NALM-6 and LC1;19, but not in melanoma or squamous carcinoma cell lines.{16507}  

     

    Brand:
    Cayman
    SKU:10011246 - 1 mg

    Available on backorder

  • Janus kinase 3 (JAK3) is a cytoplasmic protein tyrosine kinase that functions in the initiation of cytokine-triggered signal transduction by catalyzing the phosphorylation of signal transduction and activators of transcription (STATs). JAK3 is abundantly expressed in normal lymphoid cells as well as human lymphoblastic and myeloblastic leukemia cells. WHI-P131 selectively inhibits the tyrosine kinase activity of JAK3 with an IC50 value of 78 µM without affecting the enzymatic activity of JAK1, JAK2, or other protein tyrosine kinases (IC50 ≥350 µM).{16507} WHI-P131 induces apoptosis in JAK3-expressing human leukemia cell lines NALM-6 and LC1;19, but not in melanoma or squamous carcinoma cell lines.{16507}  

     

    Brand:
    Cayman
    SKU:10011246 - 10 mg

    Available on backorder

  • Janus kinase 3 (JAK3) is a cytoplasmic protein tyrosine kinase that functions in the initiation of cytokine-triggered signal transduction by catalyzing the phosphorylation of signal transduction and activators of transcription (STATs). JAK3 is abundantly expressed in normal lymphoid cells as well as human lymphoblastic and myeloblastic leukemia cells. WHI-P131 selectively inhibits the tyrosine kinase activity of JAK3 with an IC50 value of 78 µM without affecting the enzymatic activity of JAK1, JAK2, or other protein tyrosine kinases (IC50 ≥350 µM).{16507} WHI-P131 induces apoptosis in JAK3-expressing human leukemia cell lines NALM-6 and LC1;19, but not in melanoma or squamous carcinoma cell lines.{16507}  

     

    Brand:
    Cayman
    SKU:10011246 - 25 mg

    Available on backorder

  • Janus kinase 3 (JAK3) is a cytoplasmic protein tyrosine kinase that functions in the initiation of cytokine-triggered signal transduction by catalyzing the phosphorylation of signal transduction and activators of transcription (STATs). JAK3 is abundantly expressed in normal lymphoid cells as well as human lymphoblastic and myeloblastic leukemia cells. WHI-P131 selectively inhibits the tyrosine kinase activity of JAK3 with an IC50 value of 78 µM without affecting the enzymatic activity of JAK1, JAK2, or other protein tyrosine kinases (IC50 ≥350 µM).{16507} WHI-P131 induces apoptosis in JAK3-expressing human leukemia cell lines NALM-6 and LC1;19, but not in melanoma or squamous carcinoma cell lines.{16507}  

     

    Brand:
    Cayman
    SKU:10011246 - 5 mg

    Available on backorder

  • WHI-P154 is a quinazoline derivative that exhibits immunosuppressive effects by selectively inhibiting JAK3 (IC50 = 1.8 μM versus IC50s > 10 μM for JAK1 and JAK2).{26468} It has been reported to inhibit additional kinases including EGFR (IC50 = 4 nM) and VEGFR as well as the non-receptor tyrosine kinases, Abl, Lck, and Src.{26468} WHI-P154 is cytotoxic to human glioblastoma cells (IC50 = 813 nM) and has been used to induce the differentiation of neuronal precursor cells.{26470,26471,26469}  

     

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    Cayman
    SKU:-
  • WHI-P154 is a quinazoline derivative that exhibits immunosuppressive effects by selectively inhibiting JAK3 (IC50 = 1.8 μM versus IC50s > 10 μM for JAK1 and JAK2).{26468} It has been reported to inhibit additional kinases including EGFR (IC50 = 4 nM) and VEGFR as well as the non-receptor tyrosine kinases, Abl, Lck, and Src.{26468} WHI-P154 is cytotoxic to human glioblastoma cells (IC50 = 813 nM) and has been used to induce the differentiation of neuronal precursor cells.{26470,26471,26469}  

     

    Brand:
    Cayman
    SKU:-
  • WHI-P154 is a quinazoline derivative that exhibits immunosuppressive effects by selectively inhibiting JAK3 (IC50 = 1.8 μM versus IC50s > 10 μM for JAK1 and JAK2).{26468} It has been reported to inhibit additional kinases including EGFR (IC50 = 4 nM) and VEGFR as well as the non-receptor tyrosine kinases, Abl, Lck, and Src.{26468} WHI-P154 is cytotoxic to human glioblastoma cells (IC50 = 813 nM) and has been used to induce the differentiation of neuronal precursor cells.{26470,26471,26469}  

     

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    Cayman
    SKU:-
  • WHI-P180 is a multi-kinase inhibitor with IC50 values of 4.5 and 66 nM for the human proto-oncogene RET and kinase insert domain receptor (KDR), respectively.{40380} It also inhibits EGFR (IC50 = 4 μM) and binds to tau-tubulin kinase 1 (TTBK1; Kds = 0.46 and 0.24 μM for phosphorylated and non-phosphorylated TTBK1, respectively).{40381,40382} WHI-P180 inhibits JAK3 and JAK3-driven graft versus host disease responses in mice receiving allogenic bone marrow and splenocyte grafts.{40381,40383} WHI-P180 (25 mg/kg, i.p) inhibits IgE-induced vascular hyperpermeability in a mouse model of passive anaphylaxis.{40384}  

     

    Brand:
    Cayman
    SKU:23452 - 1 mg

    Available on backorder

  • WHI-P180 is a multi-kinase inhibitor with IC50 values of 4.5 and 66 nM for the human proto-oncogene RET and kinase insert domain receptor (KDR), respectively.{40380} It also inhibits EGFR (IC50 = 4 μM) and binds to tau-tubulin kinase 1 (TTBK1; Kds = 0.46 and 0.24 μM for phosphorylated and non-phosphorylated TTBK1, respectively).{40381,40382} WHI-P180 inhibits JAK3 and JAK3-driven graft versus host disease responses in mice receiving allogenic bone marrow and splenocyte grafts.{40381,40383} WHI-P180 (25 mg/kg, i.p) inhibits IgE-induced vascular hyperpermeability in a mouse model of passive anaphylaxis.{40384}  

     

    Brand:
    Cayman
    SKU:23452 - 5 mg

    Available on backorder

  • WHI-P180 is a multi-kinase inhibitor with IC50 values of 4.5 and 66 nM for the human proto-oncogene RET and kinase insert domain receptor (KDR), respectively.{40380} It also inhibits EGFR (IC50 = 4 μM) and binds to tau-tubulin kinase 1 (TTBK1; Kds = 0.46 and 0.24 μM for phosphorylated and non-phosphorylated TTBK1, respectively).{40381,40382} WHI-P180 inhibits JAK3 and JAK3-driven graft versus host disease responses in mice receiving allogenic bone marrow and splenocyte grafts.{40381,40383} WHI-P180 (25 mg/kg, i.p) inhibits IgE-induced vascular hyperpermeability in a mouse model of passive anaphylaxis.{40384}  

     

    Brand:
    Cayman
    SKU:23452 - 500 µg

    Available on backorder

  • WHI-P258 is a quinazoline compound that modeling studies suggested would bind to the active site of JAK3 with an estimated Ki value of 72 µM.{16507} However, it is inactive at JAK3 (IC50 = >300 µM) and has been used as a negative control for structurally similar compounds that inhibit platelet aggregation and herpes simplex virus 1 (HSV-1) replication.{40398,40397}  

     

    Brand:
    Cayman
    SKU:23453 - 1 mg

    Available on backorder

  • WHI-P258 is a quinazoline compound that modeling studies suggested would bind to the active site of JAK3 with an estimated Ki value of 72 µM.{16507} However, it is inactive at JAK3 (IC50 = >300 µM) and has been used as a negative control for structurally similar compounds that inhibit platelet aggregation and herpes simplex virus 1 (HSV-1) replication.{40398,40397}  

     

    Brand:
    Cayman
    SKU:23453 - 5 mg

    Available on backorder

  • WHI-P258 is a quinazoline compound that modeling studies suggested would bind to the active site of JAK3 with an estimated Ki value of 72 µM.{16507} However, it is inactive at JAK3 (IC50 = >300 µM) and has been used as a negative control for structurally similar compounds that inhibit platelet aggregation and herpes simplex virus 1 (HSV-1) replication.{40398,40397}  

     

    Brand:
    Cayman
    SKU:23453 - 500 µg

    Available on backorder

  • Tankyrases (TNKS) cleave NAD+ to produce nicotinamide and ADP-ribose, which is then covalently attached to an acceptor protein in the process known as poly(ADP-ribosyl)ation. WIKI4 is a potent and selective inhibitor of TNKS1 and TNKS2 (IC50s = 26 and 15 nM, respectively).{27316,27317} It has little or no effect on related polymerases or transferases at 10 µM.{27317} Through its effects on TNKS2, WIKI4 prevents AXIN ubiquitinylation and degradation, blocking signaling through the Wnt/β-catenin pathway.{27316} WIKI4 inhibits the expression of β-catenin target genes and cellular responses to Wnt/β-catenin signaling in both cancer cell lines and embryonic stem cells.{27316}  

     

    Brand:
    Cayman
    SKU:-
  • Tankyrases (TNKS) cleave NAD+ to produce nicotinamide and ADP-ribose, which is then covalently attached to an acceptor protein in the process known as poly(ADP-ribosyl)ation. WIKI4 is a potent and selective inhibitor of TNKS1 and TNKS2 (IC50s = 26 and 15 nM, respectively).{27316,27317} It has little or no effect on related polymerases or transferases at 10 µM.{27317} Through its effects on TNKS2, WIKI4 prevents AXIN ubiquitinylation and degradation, blocking signaling through the Wnt/β-catenin pathway.{27316} WIKI4 inhibits the expression of β-catenin target genes and cellular responses to Wnt/β-catenin signaling in both cancer cell lines and embryonic stem cells.{27316}  

     

    Brand:
    Cayman
    SKU:-
  • Tankyrases (TNKS) cleave NAD+ to produce nicotinamide and ADP-ribose, which is then covalently attached to an acceptor protein in the process known as poly(ADP-ribosyl)ation. WIKI4 is a potent and selective inhibitor of TNKS1 and TNKS2 (IC50s = 26 and 15 nM, respectively).{27316,27317} It has little or no effect on related polymerases or transferases at 10 µM.{27317} Through its effects on TNKS2, WIKI4 prevents AXIN ubiquitinylation and degradation, blocking signaling through the Wnt/β-catenin pathway.{27316} WIKI4 inhibits the expression of β-catenin target genes and cellular responses to Wnt/β-catenin signaling in both cancer cell lines and embryonic stem cells.{27316}  

     

    Brand:
    Cayman
    SKU:-
  • Tankyrases (TNKS) cleave NAD+ to produce nicotinamide and ADP-ribose, which is then covalently attached to an acceptor protein in the process known as poly(ADP-ribosyl)ation. WIKI4 is a potent and selective inhibitor of TNKS1 and TNKS2 (IC50s = 26 and 15 nM, respectively).{27316,27317} It has little or no effect on related polymerases or transferases at 10 µM.{27317} Through its effects on TNKS2, WIKI4 prevents AXIN ubiquitinylation and degradation, blocking signaling through the Wnt/β-catenin pathway.{27316} WIKI4 inhibits the expression of β-catenin target genes and cellular responses to Wnt/β-catenin signaling in both cancer cell lines and embryonic stem cells.{27316}  

     

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    Cayman
    SKU:-
  • WIN 18,446 is a bis-(dichloroacetyl)-diamine which inhibits aldehyde dehydrogenase 1a2, (IC50 = 300 nM), a testes-specific isoform of the enzyme involved in vitamin A metabolism.{23122} In this way, WIN 18,446 suppresses the expression of several genes that are regulated by retinoic acid and are necessary for spermatogenesis.{23123,23122} As a result, WIN 18,446 may cause infertility in males.{23123,23122}  

     

    Brand:
    Cayman
    SKU:-
  • WIN 18,446 is a bis-(dichloroacetyl)-diamine which inhibits aldehyde dehydrogenase 1a2, (IC50 = 300 nM), a testes-specific isoform of the enzyme involved in vitamin A metabolism.{23122} In this way, WIN 18,446 suppresses the expression of several genes that are regulated by retinoic acid and are necessary for spermatogenesis.{23123,23122} As a result, WIN 18,446 may cause infertility in males.{23123,23122}  

     

    Brand:
    Cayman
    SKU:-
  • WIN 18,446 is a bis-(dichloroacetyl)-diamine which inhibits aldehyde dehydrogenase 1a2, (IC50 = 300 nM), a testes-specific isoform of the enzyme involved in vitamin A metabolism.{23122} In this way, WIN 18,446 suppresses the expression of several genes that are regulated by retinoic acid and are necessary for spermatogenesis.{23123,23122} As a result, WIN 18,446 may cause infertility in males.{23123,23122}  

     

    Brand:
    Cayman
    SKU:-
  • WIN 54,461 is an aminoalikylindole which acts as a cannabinoid (CB) mimetic, displacing WIN 55212-2 from CB receptors on rat cerebellum membranes (IC50 = 515 nM).{16961} As it antagonizes the inhibition of electrically-induced contractions in isolated mouse vas deferens preparations by tetrahydrocannabinol or pravadoline, it may act as a receptor antagonist.{16961} The physiological effects of WIN 54,461 in vivo have not been examined. This product is intended for research and forensic applications.  

     

    Brand:
    Cayman
    SKU:9001204 - 1 mg

    Available on backorder

  • WIN 54,461 is an aminoalikylindole which acts as a cannabinoid (CB) mimetic, displacing WIN 55212-2 from CB receptors on rat cerebellum membranes (IC50 = 515 nM).{16961} As it antagonizes the inhibition of electrically-induced contractions in isolated mouse vas deferens preparations by tetrahydrocannabinol or pravadoline, it may act as a receptor antagonist.{16961} The physiological effects of WIN 54,461 in vivo have not been examined. This product is intended for research and forensic applications.  

     

    Brand:
    Cayman
    SKU:9001204 - 10 mg

    Available on backorder

  • WIN 54,461 is an aminoalikylindole which acts as a cannabinoid (CB) mimetic, displacing WIN 55212-2 from CB receptors on rat cerebellum membranes (IC50 = 515 nM).{16961} As it antagonizes the inhibition of electrically-induced contractions in isolated mouse vas deferens preparations by tetrahydrocannabinol or pravadoline, it may act as a receptor antagonist.{16961} The physiological effects of WIN 54,461 in vivo have not been examined. This product is intended for research and forensic applications.  

     

    Brand:
    Cayman
    SKU:9001204 - 5 mg

    Available on backorder

  • Wiskott-Aldrich syndrome proteins (WASPs) regulate the actin cytoskeleton by directly interacting with actin in the Arp2/3 complex.{23890} As a result, they have essential functions in diverse cellular processes, including phagocytosis, cell motility, and membrane trafficking.{23889} Wiskostatin is a cell-permeable, selective inhibitor of neural WASP (N-WASP, IC50 = ~10 μM).{23889} It directly associates with the GTPase-binding domain of N-WASP, preventing its activation by Cdc42 and phosphatidylinositol 4,5-bisphosphate.{23889} By inhibiting N-WASP, wiskostatin interferes with membrane transport, endocytosis, and neurological development.{23891,23887,23888}  

     

    Brand:
    Cayman
    SKU:-
  • Wiskott-Aldrich syndrome proteins (WASPs) regulate the actin cytoskeleton by directly interacting with actin in the Arp2/3 complex.{23890} As a result, they have essential functions in diverse cellular processes, including phagocytosis, cell motility, and membrane trafficking.{23889} Wiskostatin is a cell-permeable, selective inhibitor of neural WASP (N-WASP, IC50 = ~10 μM).{23889} It directly associates with the GTPase-binding domain of N-WASP, preventing its activation by Cdc42 and phosphatidylinositol 4,5-bisphosphate.{23889} By inhibiting N-WASP, wiskostatin interferes with membrane transport, endocytosis, and neurological development.{23891,23887,23888}  

     

    Brand:
    Cayman
    SKU:-
  • Wiskott-Aldrich syndrome proteins (WASPs) regulate the actin cytoskeleton by directly interacting with actin in the Arp2/3 complex.{23890} As a result, they have essential functions in diverse cellular processes, including phagocytosis, cell motility, and membrane trafficking.{23889} Wiskostatin is a cell-permeable, selective inhibitor of neural WASP (N-WASP, IC50 = ~10 μM).{23889} It directly associates with the GTPase-binding domain of N-WASP, preventing its activation by Cdc42 and phosphatidylinositol 4,5-bisphosphate.{23889} By inhibiting N-WASP, wiskostatin interferes with membrane transport, endocytosis, and neurological development.{23891,23887,23888}  

     

    Brand:
    Cayman
    SKU:-
  • Wiskott-Aldrich syndrome proteins (WASPs) regulate the actin cytoskeleton by directly interacting with actin in the Arp2/3 complex.{23890} As a result, they have essential functions in diverse cellular processes, including phagocytosis, cell motility, and membrane trafficking.{23889} Wiskostatin is a cell-permeable, selective inhibitor of neural WASP (N-WASP, IC50 = ~10 μM).{23889} It directly associates with the GTPase-binding domain of N-WASP, preventing its activation by Cdc42 and phosphatidylinositol 4,5-bisphosphate.{23889} By inhibiting N-WASP, wiskostatin interferes with membrane transport, endocytosis, and neurological development.{23891,23887,23888}  

     

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    Cayman
    SKU:-
  • Withaferin A is a steroidal lactone that has been found in W. somnifera with diverse biological activities.{21343,21342} It binds to and induces aggregation of vimentin intermediate filaments in cultured endothelial cells and fibroblasts, inducing apoptosis when used at concentrations ranging from 2 to 25 μM. It also induces formation of perinuclear aggregates in other intermediate filament networks including peripherin, neurofilament-triplet protein, and keratin as well as disrupts the organization of microtubules and actin/microfilaments.{21342} Withaferin A induces noncanonical ferroptosis via induction of lipid peroxidation through interaction with Kelch-like ECH-associated protein 1 (KEAP1) in IMR-32 neuroblastoma cells, an effect that is blocked by the ferroptosis inhibitors ciclopirox olamine and ferrostatin-1 (Item No. 17729).{35972} It also binds to and inhibits glutathione peroxidase 4 (GPX4) in IMR-32 cells. In vivo, withaferin A (4 mg/kg) reduces intratumor GPX4 expression and induces tumor regression in an IMR-32 mouse xenograft model. Withaferin A (2 mg/kg) also inhibits angiogenesis in a mouse model of injury-induced corneal neovascularization.{21343}  

     

    Brand:
    Cayman
    SKU:11352 - 1 mg

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  • Withaferin A is a steroidal lactone that has been found in W. somnifera with diverse biological activities.{21343,21342} It binds to and induces aggregation of vimentin intermediate filaments in cultured endothelial cells and fibroblasts, inducing apoptosis when used at concentrations ranging from 2 to 25 μM. It also induces formation of perinuclear aggregates in other intermediate filament networks including peripherin, neurofilament-triplet protein, and keratin as well as disrupts the organization of microtubules and actin/microfilaments.{21342} Withaferin A induces noncanonical ferroptosis via induction of lipid peroxidation through interaction with Kelch-like ECH-associated protein 1 (KEAP1) in IMR-32 neuroblastoma cells, an effect that is blocked by the ferroptosis inhibitors ciclopirox olamine and ferrostatin-1 (Item No. 17729).{35972} It also binds to and inhibits glutathione peroxidase 4 (GPX4) in IMR-32 cells. In vivo, withaferin A (4 mg/kg) reduces intratumor GPX4 expression and induces tumor regression in an IMR-32 mouse xenograft model. Withaferin A (2 mg/kg) also inhibits angiogenesis in a mouse model of injury-induced corneal neovascularization.{21343}  

     

    Brand:
    Cayman
    SKU:11352 - 10 mg

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  • Withaferin A is a steroidal lactone that has been found in W. somnifera with diverse biological activities.{21343,21342} It binds to and induces aggregation of vimentin intermediate filaments in cultured endothelial cells and fibroblasts, inducing apoptosis when used at concentrations ranging from 2 to 25 μM. It also induces formation of perinuclear aggregates in other intermediate filament networks including peripherin, neurofilament-triplet protein, and keratin as well as disrupts the organization of microtubules and actin/microfilaments.{21342} Withaferin A induces noncanonical ferroptosis via induction of lipid peroxidation through interaction with Kelch-like ECH-associated protein 1 (KEAP1) in IMR-32 neuroblastoma cells, an effect that is blocked by the ferroptosis inhibitors ciclopirox olamine and ferrostatin-1 (Item No. 17729).{35972} It also binds to and inhibits glutathione peroxidase 4 (GPX4) in IMR-32 cells. In vivo, withaferin A (4 mg/kg) reduces intratumor GPX4 expression and induces tumor regression in an IMR-32 mouse xenograft model. Withaferin A (2 mg/kg) also inhibits angiogenesis in a mouse model of injury-induced corneal neovascularization.{21343}  

     

    Brand:
    Cayman
    SKU:11352 - 25 mg

    Available on backorder

  • Withaferin A is a steroidal lactone that has been found in W. somnifera with diverse biological activities.{21343,21342} It binds to and induces aggregation of vimentin intermediate filaments in cultured endothelial cells and fibroblasts, inducing apoptosis when used at concentrations ranging from 2 to 25 μM. It also induces formation of perinuclear aggregates in other intermediate filament networks including peripherin, neurofilament-triplet protein, and keratin as well as disrupts the organization of microtubules and actin/microfilaments.{21342} Withaferin A induces noncanonical ferroptosis via induction of lipid peroxidation through interaction with Kelch-like ECH-associated protein 1 (KEAP1) in IMR-32 neuroblastoma cells, an effect that is blocked by the ferroptosis inhibitors ciclopirox olamine and ferrostatin-1 (Item No. 17729).{35972} It also binds to and inhibits glutathione peroxidase 4 (GPX4) in IMR-32 cells. In vivo, withaferin A (4 mg/kg) reduces intratumor GPX4 expression and induces tumor regression in an IMR-32 mouse xenograft model. Withaferin A (2 mg/kg) also inhibits angiogenesis in a mouse model of injury-induced corneal neovascularization.{21343}  

     

    Brand:
    Cayman
    SKU:11352 - 5 mg

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  • Withanolide A is a natural product isolated from the medicinal plant W. somnifera that has antioxidant and neuroprotective activity.{28425} It helps to promote neurite outgrowth at 1 µM in cultured neurons and in rodents injected with Aβ(25-35), and also recovers Aβ(25-35)-induced memory deficit in mice (10 µmol/kg/day).{28426,28427} Withanolide A reverses hypoxia-mediated neurodegeneration by restoring hypoxia-induced glutathione depletion in the hippocampus of mice.{28428}  

     

    Brand:
    Cayman
    SKU:11797 - 1 mg

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  • Withanolide A is a natural product isolated from the medicinal plant W. somnifera that has antioxidant and neuroprotective activity.{28425} It helps to promote neurite outgrowth at 1 µM in cultured neurons and in rodents injected with Aβ(25-35), and also recovers Aβ(25-35)-induced memory deficit in mice (10 µmol/kg/day).{28426,28427} Withanolide A reverses hypoxia-mediated neurodegeneration by restoring hypoxia-induced glutathione depletion in the hippocampus of mice.{28428}  

     

    Brand:
    Cayman
    SKU:11797 - 10 mg

    Available on backorder

  • Withanolide A is a natural product isolated from the medicinal plant W. somnifera that has antioxidant and neuroprotective activity.{28425} It helps to promote neurite outgrowth at 1 µM in cultured neurons and in rodents injected with Aβ(25-35), and also recovers Aβ(25-35)-induced memory deficit in mice (10 µmol/kg/day).{28426,28427} Withanolide A reverses hypoxia-mediated neurodegeneration by restoring hypoxia-induced glutathione depletion in the hippocampus of mice.{28428}  

     

    Brand:
    Cayman
    SKU:11797 - 5 mg

    Available on backorder

  • Withanolide A is a natural product isolated from the medicinal plant W. somnifera that has antioxidant and neuroprotective activity.{28425} It helps to promote neurite outgrowth at 1 µM in cultured neurons and in rodents injected with Aβ(25-35), and also recovers Aβ(25-35)-induced memory deficit in mice (10 µmol/kg/day).{28426,28427} Withanolide A reverses hypoxia-mediated neurodegeneration by restoring hypoxia-induced glutathione depletion in the hippocampus of mice.{28428}  

     

    Brand:
    Cayman
    SKU:11797 - 500 µg

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  • Withanolide B is a withanolide that has been found in W. somnifera.{48147} Unlike withanolide A, it does not increase glucose uptake in L6 myotubes.{48148} In in silico docking studies, withanolide B was identified as a neuronal nitric oxide synthase (nNOS) inhibitor (Ki = 5.15 nM), that also inhibited inducible NOS (iNOS) and endothelial NOS (eNOS; Kis = 15.48 and 66.59 nM, respectively), and as a ligand for the PARP1 catalytic domain with an estimated Ki value of 7.54 nM.{48150,48149}  

     

    Brand:
    Cayman
    SKU:11798 - 1 mg

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  • Withanolide B is a withanolide that has been found in W. somnifera.{48147} Unlike withanolide A, it does not increase glucose uptake in L6 myotubes.{48148} In in silico docking studies, withanolide B was identified as a neuronal nitric oxide synthase (nNOS) inhibitor (Ki = 5.15 nM), that also inhibited inducible NOS (iNOS) and endothelial NOS (eNOS; Kis = 15.48 and 66.59 nM, respectively), and as a ligand for the PARP1 catalytic domain with an estimated Ki value of 7.54 nM.{48150,48149}  

     

    Brand:
    Cayman
    SKU:11798 - 10 mg

    Available on backorder

  • Withanolide B is a withanolide that has been found in W. somnifera.{48147} Unlike withanolide A, it does not increase glucose uptake in L6 myotubes.{48148} In in silico docking studies, withanolide B was identified as a neuronal nitric oxide synthase (nNOS) inhibitor (Ki = 5.15 nM), that also inhibited inducible NOS (iNOS) and endothelial NOS (eNOS; Kis = 15.48 and 66.59 nM, respectively), and as a ligand for the PARP1 catalytic domain with an estimated Ki value of 7.54 nM.{48150,48149}  

     

    Brand:
    Cayman
    SKU:11798 - 5 mg

    Available on backorder

  • WM-1119 is an orally bioavailable inhibitor of lysine acetyltransferase 6A (KAT6A/MOZ; IC50 = 6.3 nM).{54159} It binds to KAT6A with a Kd value of 2 nM and is selective for KAT6A over KAT5 and KAT7 (Kds = 2,200 and 500 nM, respectively), as well as over a panel of 159 additional targets at 1 and 10 μM.{51034} WM-1119 inhibits proliferation of EMRK1184 B cell lymphoma cells (IC50 = 0.25 μM). It reduces tumor growth and spleen weight in a murine EMRK1184 model when administered at a dose of 50 mg/kg four times per day.  

     

    Brand:
    Cayman
    SKU:30509 - 10 mg

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  • WM-1119 is an orally bioavailable inhibitor of lysine acetyltransferase 6A (KAT6A/MOZ; IC50 = 6.3 nM).{54159} It binds to KAT6A with a Kd value of 2 nM and is selective for KAT6A over KAT5 and KAT7 (Kds = 2,200 and 500 nM, respectively), as well as over a panel of 159 additional targets at 1 and 10 μM.{51034} WM-1119 inhibits proliferation of EMRK1184 B cell lymphoma cells (IC50 = 0.25 μM). It reduces tumor growth and spleen weight in a murine EMRK1184 model when administered at a dose of 50 mg/kg four times per day.  

     

    Brand:
    Cayman
    SKU:30509 - 25 mg

    Available on backorder

  • WM-1119 is an orally bioavailable inhibitor of lysine acetyltransferase 6A (KAT6A/MOZ; IC50 = 6.3 nM).{54159} It binds to KAT6A with a Kd value of 2 nM and is selective for KAT6A over KAT5 and KAT7 (Kds = 2,200 and 500 nM, respectively), as well as over a panel of 159 additional targets at 1 and 10 μM.{51034} WM-1119 inhibits proliferation of EMRK1184 B cell lymphoma cells (IC50 = 0.25 μM). It reduces tumor growth and spleen weight in a murine EMRK1184 model when administered at a dose of 50 mg/kg four times per day.  

     

    Brand:
    Cayman
    SKU:30509 - 5 mg

    Available on backorder

  • WM-1119 is an orally bioavailable inhibitor of lysine acetyltransferase 6A (KAT6A/MOZ; IC50 = 6.3 nM).{54159} It binds to KAT6A with a Kd value of 2 nM and is selective for KAT6A over KAT5 and KAT7 (Kds = 2,200 and 500 nM, respectively), as well as over a panel of 159 additional targets at 1 and 10 μM.{51034} WM-1119 inhibits proliferation of EMRK1184 B cell lymphoma cells (IC50 = 0.25 μM). It reduces tumor growth and spleen weight in a murine EMRK1184 model when administered at a dose of 50 mg/kg four times per day.  

     

    Brand:
    Cayman
    SKU:30509 - 50 mg

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  • WNK-IN-11 is an allosteric inhibitor of lysine-deficient protein kinase 1 (WNK1; IC50 = 4 nM).{52277} It is 57- and 1000-fold selective for WNK1 over WNK2 and WNK4, respectively, as well as a panel of 400 kinases at 10 µM. It inhibits WNK1-mediated phosphorylation of the transcription factor OSR1 in HEK293 cells (EC50 = 0.352 µM).  

     

    Brand:
    Cayman
    SKU:29676 - 10 mg

    Available on backorder

  • WNK-IN-11 is an allosteric inhibitor of lysine-deficient protein kinase 1 (WNK1; IC50 = 4 nM).{52277} It is 57- and 1000-fold selective for WNK1 over WNK2 and WNK4, respectively, as well as a panel of 400 kinases at 10 µM. It inhibits WNK1-mediated phosphorylation of the transcription factor OSR1 in HEK293 cells (EC50 = 0.352 µM).  

     

    Brand:
    Cayman
    SKU:29676 - 25 mg

    Available on backorder

  • WNK-IN-11 is an allosteric inhibitor of lysine-deficient protein kinase 1 (WNK1; IC50 = 4 nM).{52277} It is 57- and 1000-fold selective for WNK1 over WNK2 and WNK4, respectively, as well as a panel of 400 kinases at 10 µM. It inhibits WNK1-mediated phosphorylation of the transcription factor OSR1 in HEK293 cells (EC50 = 0.352 µM).  

     

    Brand:
    Cayman
    SKU:29676 - 5 mg

    Available on backorder

  • WNK-IN-11 is an allosteric inhibitor of lysine-deficient protein kinase 1 (WNK1; IC50 = 4 nM).{52277} It is 57- and 1000-fold selective for WNK1 over WNK2 and WNK4, respectively, as well as a panel of 400 kinases at 10 µM. It inhibits WNK1-mediated phosphorylation of the transcription factor OSR1 in HEK293 cells (EC50 = 0.352 µM).  

     

    Brand:
    Cayman
    SKU:29676 - 50 mg

    Available on backorder

  • Wnt Agonist I is a cell-permeable activator of Wnt signaling that does not inhibit GSK-3β (IC50 > 60 µM).{32213} It induces nuclear accumulation of β-catenin, increasing transcriptional activity driven by TCF (EC50 = 700 nM) and altering embryonic development.{32213,32212} Wnt Agonist I is effective in vivo, decreasing tissue damage and improving renal function after ischemia-reperfusion in rats.{32211}  

     

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    Cayman
    SKU:19903 -

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  • Wnt Agonist I is a cell-permeable activator of Wnt signaling that does not inhibit GSK-3β (IC50 > 60 µM).{32213} It induces nuclear accumulation of β-catenin, increasing transcriptional activity driven by TCF (EC50 = 700 nM) and altering embryonic development.{32213,32212} Wnt Agonist I is effective in vivo, decreasing tissue damage and improving renal function after ischemia-reperfusion in rats.{32211}  

     

    Brand:
    Cayman
    SKU:19903 -

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  • Wnt Agonist I is a cell-permeable activator of Wnt signaling that does not inhibit GSK-3β (IC50 > 60 µM).{32213} It induces nuclear accumulation of β-catenin, increasing transcriptional activity driven by TCF (EC50 = 700 nM) and altering embryonic development.{32213,32212} Wnt Agonist I is effective in vivo, decreasing tissue damage and improving renal function after ischemia-reperfusion in rats.{32211}  

     

    Brand:
    Cayman
    SKU:19903 -

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  • Wnt Agonist I is a cell-permeable activator of Wnt signaling that does not inhibit GSK-3β (IC50 > 60 µM).{32213} It induces nuclear accumulation of β-catenin, increasing transcriptional activity driven by TCF (EC50 = 700 nM) and altering embryonic development.{32213,32212} Wnt Agonist I is effective in vivo, decreasing tissue damage and improving renal function after ischemia-reperfusion in rats.{32211}  

     

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    Cayman
    SKU:19903 -

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  • Porcupine (PORCN) is a membrane bound O-acyltransferase that mediates palmitoylation of Wnt family proteins.{27064} This step is required for secretion and biologic activity of Wnt proteins, which have roles in embryonic development and cancer.{27064,27062} Wnt-C59 is a potent inhibitor of PORCN, as measured by prevention of Wnt3A activation (IC50 = 74 pM).{27062} As palmitoylation of Wnt is required for its secretion, Wnt-C59 completely blocks Wnt3A secretion into culture media.{27062} Wnt-C59 prevents activation of all evaluated Wnt family members.{27062} This compound is effective in vivo as well as in vitro. Whether given by intravenous (2.5 mg/kg) or oral administration (5 mg/kg), Wnt-C59 displays a half-life in blood of approximately 1.94 hours, and remains greater than 10-fold above the in vitro IC50 concentration for at least 16 hours after a single oral dose.{27062} It blocks the progression of both basal-like and triple-negative breast cancers while downregulating Wnt/β-catenin pathway target genes in mice.{27062,27063}  

     

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    Cayman
    SKU:-

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