Chemicals

Showing 21001–21150 of 41137 results

  • Golvatinib is an orally bioavailable dual inhibitor of the receptor tyrosine kinases c-Met and VEGF receptor 2 (VEGFR2), which are involved in tumor progression.{41051} Golvatinib inhibits autophosphorylation of c-Met in MKN45 cells and phosphorylation of VEGFR2 in human umbilical vein endothelial cells (HUVECs; IC50s = 14 and 16 nM, respectively). It also inhibits proliferation of a variety of cancer cell lines and of HUVECs stimulated with hepatocyte growth factor (HGF) and VEGF but not bFGF (IC50s = 17, 84, and >1,000 nM for HGF-, VEGF-, and bFGF-stimulated HUVECs, respectively). In nude mouse xenograft models using MKN45, Hs746T, SNU-5, or EBC-1 cancer cells, golvatinib (25-200 mg/kg, daily) dose-dependently reduces tumor volume, and it increases survival in the model using MKN45 cells.  

     

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    Cayman
    SKU:22143 -

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  • Gomisin C, a lignan first isolated from the fruits of S. chinensis, scavenges oxygen radicals and reduces the production of reactive oxygen species by inhibiting neutrophil activity.{30125} It has been shown to attenuate respiratory burst in rat peripheral neutrophils via suppression of NADPH oxidase (39% inhibition at 30 µg/ml) and inhibition of cytosolic calcium release from intracellular stores (36% inhibition at 50 µg/ml).{30126} Gomisin C can induce liver microsomal cytochrome P450, thus facilitating the clearance of xenobiotics and protecting against hepatotoxicity in rodent models of liver injury.{30124}  

     

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  • Gomisin C, a lignan first isolated from the fruits of S. chinensis, scavenges oxygen radicals and reduces the production of reactive oxygen species by inhibiting neutrophil activity.{30125} It has been shown to attenuate respiratory burst in rat peripheral neutrophils via suppression of NADPH oxidase (39% inhibition at 30 µg/ml) and inhibition of cytosolic calcium release from intracellular stores (36% inhibition at 50 µg/ml).{30126} Gomisin C can induce liver microsomal cytochrome P450, thus facilitating the clearance of xenobiotics and protecting against hepatotoxicity in rodent models of liver injury.{30124}  

     

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    Cayman
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  • Gomisin C, a lignan first isolated from the fruits of S. chinensis, scavenges oxygen radicals and reduces the production of reactive oxygen species by inhibiting neutrophil activity.{30125} It has been shown to attenuate respiratory burst in rat peripheral neutrophils via suppression of NADPH oxidase (39% inhibition at 30 µg/ml) and inhibition of cytosolic calcium release from intracellular stores (36% inhibition at 50 µg/ml).{30126} Gomisin C can induce liver microsomal cytochrome P450, thus facilitating the clearance of xenobiotics and protecting against hepatotoxicity in rodent models of liver injury.{30124}  

     

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    Cayman
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  • Gomisin C, a lignan first isolated from the fruits of S. chinensis, scavenges oxygen radicals and reduces the production of reactive oxygen species by inhibiting neutrophil activity.{30125} It has been shown to attenuate respiratory burst in rat peripheral neutrophils via suppression of NADPH oxidase (39% inhibition at 30 µg/ml) and inhibition of cytosolic calcium release from intracellular stores (36% inhibition at 50 µg/ml).{30126} Gomisin C can induce liver microsomal cytochrome P450, thus facilitating the clearance of xenobiotics and protecting against hepatotoxicity in rodent models of liver injury.{30124}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Gomisin D is a lignan that has been found in S. chinensis and has diverse biological activities, including enzyme inhibitory and antioxidant properties.{52842,52843,47352} It inhibits acetylcholinesterase (AChE) with an IC50 value of 7.84 µM.{52842} Gomisin D scavenges ABTS (Item No. 27317) and 2,2-diphenyl-1-picrylhydrazyl (DPPH; Item No. 14805) radicals (IC50s = 24.5 and 203 µM, respectively).{47352} It inhibits the UDP-glucuronosyltransferase (UGT) isoforms UGT1A1 and UGT1A3 by 89.9 and 83.1%, respectively, when used at a concentration of 100 µM.{52843} It is selective for UGT1A1 and UGT1A3 over other UGT isoforms at 100 µM.  

     

    Brand:
    Cayman
    SKU:30697 - 1 mg

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  • Gomisin D is a lignan that has been found in S. chinensis and has diverse biological activities, including enzyme inhibitory and antioxidant properties.{52842,52843,47352} It inhibits acetylcholinesterase (AChE) with an IC50 value of 7.84 µM.{52842} Gomisin D scavenges ABTS (Item No. 27317) and 2,2-diphenyl-1-picrylhydrazyl (DPPH; Item No. 14805) radicals (IC50s = 24.5 and 203 µM, respectively).{47352} It inhibits the UDP-glucuronosyltransferase (UGT) isoforms UGT1A1 and UGT1A3 by 89.9 and 83.1%, respectively, when used at a concentration of 100 µM.{52843} It is selective for UGT1A1 and UGT1A3 over other UGT isoforms at 100 µM.  

     

    Brand:
    Cayman
    SKU:30697 - 10 mg

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  • Gomisin D is a lignan that has been found in S. chinensis and has diverse biological activities, including enzyme inhibitory and antioxidant properties.{52842,52843,47352} It inhibits acetylcholinesterase (AChE) with an IC50 value of 7.84 µM.{52842} Gomisin D scavenges ABTS (Item No. 27317) and 2,2-diphenyl-1-picrylhydrazyl (DPPH; Item No. 14805) radicals (IC50s = 24.5 and 203 µM, respectively).{47352} It inhibits the UDP-glucuronosyltransferase (UGT) isoforms UGT1A1 and UGT1A3 by 89.9 and 83.1%, respectively, when used at a concentration of 100 µM.{52843} It is selective for UGT1A1 and UGT1A3 over other UGT isoforms at 100 µM.  

     

    Brand:
    Cayman
    SKU:30697 - 5 mg

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  • Gomisin J is a lignan that has been found in Schisandra chinensis and has diverse biological activities.{52505,52506} It inhibits HIV-1 IIIB replication in H9 T cells (EC50 = 1.5 µg/ml).{52505} Gomisin J (20 µM) decreases LPS-induced increases in nitric oxide (NO) production and p38, ERK, and JNK phosphorylation in RAW 264.7 cells.{52506} It induces relaxation of isolated, precontracted endothelium-intact rat aortic rings when used at concentrations of 3, 10, and 30 µg/ml.{52508} Gomisin J is cytotoxic to 13 cancer cell lines, including breast, colon, and cervical cancer cells, when used at a concentration of 30 µg/ml.{52507}  

     

    Brand:
    Cayman
    SKU:30213 - 1 mg

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  • Gomisin J is a lignan that has been found in Schisandra chinensis and has diverse biological activities.{52505,52506} It inhibits HIV-1 IIIB replication in H9 T cells (EC50 = 1.5 µg/ml).{52505} Gomisin J (20 µM) decreases LPS-induced increases in nitric oxide (NO) production and p38, ERK, and JNK phosphorylation in RAW 264.7 cells.{52506} It induces relaxation of isolated, precontracted endothelium-intact rat aortic rings when used at concentrations of 3, 10, and 30 µg/ml.{52508} Gomisin J is cytotoxic to 13 cancer cell lines, including breast, colon, and cervical cancer cells, when used at a concentration of 30 µg/ml.{52507}  

     

    Brand:
    Cayman
    SKU:30213 - 10 mg

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  • Gomisin J is a lignan that has been found in Schisandra chinensis and has diverse biological activities.{52505,52506} It inhibits HIV-1 IIIB replication in H9 T cells (EC50 = 1.5 µg/ml).{52505} Gomisin J (20 µM) decreases LPS-induced increases in nitric oxide (NO) production and p38, ERK, and JNK phosphorylation in RAW 264.7 cells.{52506} It induces relaxation of isolated, precontracted endothelium-intact rat aortic rings when used at concentrations of 3, 10, and 30 µg/ml.{52508} Gomisin J is cytotoxic to 13 cancer cell lines, including breast, colon, and cervical cancer cells, when used at a concentration of 30 µg/ml.{52507}  

     

    Brand:
    Cayman
    SKU:30213 - 5 mg

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  • Gonadorelin is a tropic hormone and agonist of the gonadotropin-releasing hormone receptor (GNRHR; Ki = 13 nM in CHO cells expressing the human receptor).{36464} It stimulates luteinizing hormone (LH) and follicle-stimulating hormone (FSH) release from rat anterior pituitary cultures when administered at a dose of 0.1 μg.{40777} It also stimulates LH release from bovine anterior pituitary cultures at a concentration of 1 μM.{40778} In vivo, gonadorelin induces ovulation in rats pretreated with fluphenazine (Item No. 23555; ED50 = 610.3 ng/kg).{40779} Formulations containing gonadorelin have been used as diagnostic agents to assess pituitary gland function.  

     

    Brand:
    Cayman
    SKU:24240 - 10 mg

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  • Gonadorelin is a tropic hormone and agonist of the gonadotropin-releasing hormone receptor (GNRHR; Ki = 13 nM in CHO cells expressing the human receptor).{36464} It stimulates luteinizing hormone (LH) and follicle-stimulating hormone (FSH) release from rat anterior pituitary cultures when administered at a dose of 0.1 μg.{40777} It also stimulates LH release from bovine anterior pituitary cultures at a concentration of 1 μM.{40778} In vivo, gonadorelin induces ovulation in rats pretreated with fluphenazine (Item No. 23555; ED50 = 610.3 ng/kg).{40779} Formulations containing gonadorelin have been used as diagnostic agents to assess pituitary gland function.  

     

    Brand:
    Cayman
    SKU:24240 - 25 mg

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  • Gonadorelin is a tropic hormone and agonist of the gonadotropin-releasing hormone receptor (GNRHR; Ki = 13 nM in CHO cells expressing the human receptor).{36464} It stimulates luteinizing hormone (LH) and follicle-stimulating hormone (FSH) release from rat anterior pituitary cultures when administered at a dose of 0.1 μg.{40777} It also stimulates LH release from bovine anterior pituitary cultures at a concentration of 1 μM.{40778} In vivo, gonadorelin induces ovulation in rats pretreated with fluphenazine (Item No. 23555; ED50 = 610.3 ng/kg).{40779} Formulations containing gonadorelin have been used as diagnostic agents to assess pituitary gland function.  

     

    Brand:
    Cayman
    SKU:24240 - 5 mg

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  • Goserelin is a synthetic gonadotropin-releasing hormone (GNRH) agonist that binds to the GNRH receptor (GNRHR; Ki = 1.6 nM, in CHO cells expressing the human receptor).{36464} It binds to mouse pituitary αT3-1 cells and human placenta (Kds = 2 and 580 nM, respectively) and increases intracellular calcium in αT3-1 cells.{36465} Goserelin induces testosterone production in vitro within 4 h in rat Leydig cells (ED50 = 83 nM) but decreases testosterone plasma level in vivo in rats over a period of 2 to 24 weeks.{36466,36467} It inhibits tumor growth in a DU145 human prostate carcinoma mouse xenograft model when administered at a dose of 100 μg per day.{36468} Formulations containing goserelin have been used in the treatment of hormone-dependent breast and prostate cancers, as well as endometriosis and uterine fibroids.  

     

    Brand:
    Cayman
    SKU:24071 - 1 mg

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  • Goserelin is a synthetic gonadotropin-releasing hormone (GNRH) agonist that binds to the GNRH receptor (GNRHR; Ki = 1.6 nM, in CHO cells expressing the human receptor).{36464} It binds to mouse pituitary αT3-1 cells and human placenta (Kds = 2 and 580 nM, respectively) and increases intracellular calcium in αT3-1 cells.{36465} Goserelin induces testosterone production in vitro within 4 h in rat Leydig cells (ED50 = 83 nM) but decreases testosterone plasma level in vivo in rats over a period of 2 to 24 weeks.{36466,36467} It inhibits tumor growth in a DU145 human prostate carcinoma mouse xenograft model when administered at a dose of 100 μg per day.{36468} Formulations containing goserelin have been used in the treatment of hormone-dependent breast and prostate cancers, as well as endometriosis and uterine fibroids.  

     

    Brand:
    Cayman
    SKU:24071 - 10 mg

    Available on backorder

  • Goserelin is a synthetic gonadotropin-releasing hormone (GNRH) agonist that binds to the GNRH receptor (GNRHR; Ki = 1.6 nM, in CHO cells expressing the human receptor).{36464} It binds to mouse pituitary αT3-1 cells and human placenta (Kds = 2 and 580 nM, respectively) and increases intracellular calcium in αT3-1 cells.{36465} Goserelin induces testosterone production in vitro within 4 h in rat Leydig cells (ED50 = 83 nM) but decreases testosterone plasma level in vivo in rats over a period of 2 to 24 weeks.{36466,36467} It inhibits tumor growth in a DU145 human prostate carcinoma mouse xenograft model when administered at a dose of 100 μg per day.{36468} Formulations containing goserelin have been used in the treatment of hormone-dependent breast and prostate cancers, as well as endometriosis and uterine fibroids.  

     

    Brand:
    Cayman
    SKU:24071 - 5 mg

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  • Gossypol is a racemic mixture of natural polyphenols isolated from parts of the cotton plant (genus Gossypium). It causes infertility in a variety of cotton pests and spermatogenesis arrest in humans.{23003} Gossypol also has antimalarial properties, preventing the growth of P. falciparum at low micromolar concentrations.{23001} It inhibits aldose reductase (Ki = 0.5 µM).{23002} Gossypol also acts as an anticancer agent, inhibiting cell growth in various cancer cell lines, in part by blocking the anti-apoptotic functions of Bcl-2 and Bcl-xL, again at low micromolar concentrations.{23000}  

     

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  • Gossypol is a racemic mixture of natural polyphenols isolated from parts of the cotton plant (genus Gossypium). It causes infertility in a variety of cotton pests and spermatogenesis arrest in humans.{23003} Gossypol also has antimalarial properties, preventing the growth of P. falciparum at low micromolar concentrations.{23001} It inhibits aldose reductase (Ki = 0.5 µM).{23002} Gossypol also acts as an anticancer agent, inhibiting cell growth in various cancer cell lines, in part by blocking the anti-apoptotic functions of Bcl-2 and Bcl-xL, again at low micromolar concentrations.{23000}  

     

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    Cayman
    SKU:-
  • Gossypol is a racemic mixture of natural polyphenols isolated from parts of the cotton plant (genus Gossypium). It causes infertility in a variety of cotton pests and spermatogenesis arrest in humans.{23003} Gossypol also has antimalarial properties, preventing the growth of P. falciparum at low micromolar concentrations.{23001} It inhibits aldose reductase (Ki = 0.5 µM).{23002} Gossypol also acts as an anticancer agent, inhibiting cell growth in various cancer cell lines, in part by blocking the anti-apoptotic functions of Bcl-2 and Bcl-xL, again at low micromolar concentrations.{23000}  

     

    Brand:
    Cayman
    SKU:-
  • Gossypol is a racemic mixture of natural polyphenols isolated from parts of the cotton plant (genus Gossypium). It causes infertility in a variety of cotton pests and spermatogenesis arrest in humans.{23003} Gossypol also has antimalarial properties, preventing the growth of P. falciparum at low micromolar concentrations.{23001} It inhibits aldose reductase (Ki = 0.5 µM).{23002} Gossypol also acts as an anticancer agent, inhibiting cell growth in various cancer cell lines, in part by blocking the anti-apoptotic functions of Bcl-2 and Bcl-xL, again at low micromolar concentrations.{23000}  

     

    Brand:
    Cayman
    SKU:-
  • Nicotinamide phosphoribosyltransferase (Nampt) converts nicotinamide into nicotinamide mononucleotide (NMN), which is subsequently converted to NAD+ by NMN adenyltransferase. Cancer cells commonly have an unusually high rate of NAD+ turnover, suggesting that inhibition of Nampt might selectively target cancer cells. GPP 78 is a potent inhibitor of Nampt (IC50 = 3 nM).{17893} It induces cell death in the neuroblastoma cell line SH-SY5Y with an IC50 value of 3.8 nM through a process that appears to involve autophagy.{13670}  

     

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    Cayman
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  • Nicotinamide phosphoribosyltransferase (Nampt) converts nicotinamide into nicotinamide mononucleotide (NMN), which is subsequently converted to NAD+ by NMN adenyltransferase. Cancer cells commonly have an unusually high rate of NAD+ turnover, suggesting that inhibition of Nampt might selectively target cancer cells. GPP 78 is a potent inhibitor of Nampt (IC50 = 3 nM).{17893} It induces cell death in the neuroblastoma cell line SH-SY5Y with an IC50 value of 3.8 nM through a process that appears to involve autophagy.{13670}  

     

    Brand:
    Cayman
    SKU:-
  • Nicotinamide phosphoribosyltransferase (Nampt) converts nicotinamide into nicotinamide mononucleotide (NMN), which is subsequently converted to NAD+ by NMN adenyltransferase. Cancer cells commonly have an unusually high rate of NAD+ turnover, suggesting that inhibition of Nampt might selectively target cancer cells. GPP 78 is a potent inhibitor of Nampt (IC50 = 3 nM).{17893} It induces cell death in the neuroblastoma cell line SH-SY5Y with an IC50 value of 3.8 nM through a process that appears to involve autophagy.{13670}  

     

    Brand:
    Cayman
    SKU:-
  • Nicotinamide phosphoribosyltransferase (Nampt) converts nicotinamide into nicotinamide mononucleotide (NMN), which is subsequently converted to NAD+ by NMN adenyltransferase. Cancer cells commonly have an unusually high rate of NAD+ turnover, suggesting that inhibition of Nampt might selectively target cancer cells. GPP 78 is a potent inhibitor of Nampt (IC50 = 3 nM).{17893} It induces cell death in the neuroblastoma cell line SH-SY5Y with an IC50 value of 3.8 nM through a process that appears to involve autophagy.{13670}  

     

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    Cayman
    SKU:-
  • GPR120 (free fatty acid receptor 4/FFAR4) is a G protein-coupled receptor expressed in intestine, adipocytes, and pro-inflammatory macrophages that is activated by long chain free fatty acids. It has been linked to the ability of fatty acids to produce anti-inflammatory effects and to acutely potentiate insulin secretion. GPR120 compound A is an orally available, high-affinity agonist of GPR120 (EC50 = ~0.35 µM) that demonstrates potent selectivity over another lipid-sensing G-protein, GPR40 (FFAR1).{26948} This compound exerts anti-inflammatory effects on macrophages in vitro and improves glucose tolerance, decreases hyperinsulinemia, increases insulin sensitivity, and decreases hepatic steatosis when included at 30 mg/kg body weight in a high-fat diet fed to obese mice.{26948}  

     

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    Cayman
    SKU:-

    Out of stock

  • GPR120 (free fatty acid receptor 4/FFAR4) is a G protein-coupled receptor expressed in intestine, adipocytes, and pro-inflammatory macrophages that is activated by long chain free fatty acids. It has been linked to the ability of fatty acids to produce anti-inflammatory effects and to acutely potentiate insulin secretion. GPR120 compound A is an orally available, high-affinity agonist of GPR120 (EC50 = ~0.35 µM) that demonstrates potent selectivity over another lipid-sensing G-protein, GPR40 (FFAR1).{26948} This compound exerts anti-inflammatory effects on macrophages in vitro and improves glucose tolerance, decreases hyperinsulinemia, increases insulin sensitivity, and decreases hepatic steatosis when included at 30 mg/kg body weight in a high-fat diet fed to obese mice.{26948}  

     

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    Cayman
    SKU:-

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  • GPR120 (free fatty acid receptor 4/FFAR4) is a G protein-coupled receptor expressed in intestine, adipocytes, and pro-inflammatory macrophages that is activated by long chain free fatty acids. It has been linked to the ability of fatty acids to produce anti-inflammatory effects and to acutely potentiate insulin secretion. GPR120 compound A is an orally available, high-affinity agonist of GPR120 (EC50 = ~0.35 µM) that demonstrates potent selectivity over another lipid-sensing G-protein, GPR40 (FFAR1).{26948} This compound exerts anti-inflammatory effects on macrophages in vitro and improves glucose tolerance, decreases hyperinsulinemia, increases insulin sensitivity, and decreases hepatic steatosis when included at 30 mg/kg body weight in a high-fat diet fed to obese mice.{26948}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • GPR120 (free fatty acid receptor 4/FFAR4) is a G protein-coupled receptor expressed in intestine, adipocytes, and pro-inflammatory macrophages that is activated by long chain free fatty acids. It has been linked to the ability of fatty acids to produce anti-inflammatory effects and to acutely potentiate insulin secretion. GPR120 compound A is an orally available, high-affinity agonist of GPR120 (EC50 = ~0.35 µM) that demonstrates potent selectivity over another lipid-sensing G-protein, GPR40 (FFAR1).{26948} This compound exerts anti-inflammatory effects on macrophages in vitro and improves glucose tolerance, decreases hyperinsulinemia, increases insulin sensitivity, and decreases hepatic steatosis when included at 30 mg/kg body weight in a high-fat diet fed to obese mice.{26948}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • GPR39-C3 is a potent agonist of the orphan G protein-coupled receptor GPR39 with EC50 values of 0.8 and 0.4 nM for cAMP production in HEK293 cells expressing human and rat receptors, respectively.{42282} It is selective for GPR39 over a panel of kinases (IC50s = >10 μM), ghrelin and neurotensin-1 receptors (IC50s = >30 μM), and a variety of enzymes, transporters, or G protein-coupled receptors. GPR39-C3 increases secretion of glucagon-like peptide 1 (GLP-1; Item No. 24460) in STC-1 mouse enteroendocrine cells (EC50 = 0.06 μM) and is protective against cytokine-induced cell death in INS-1E rat insulinoma cells (EC50 = 0.02 μM). In vivo, GPR39-C3 (30 mg/kg) increases the amount of active GLP-1 in sera by 6-fold in glucose-challenged mice when administered concurrently with a dipeptidyl peptidase 4 (DPP-4) inhibitor.  

     

    Brand:
    Cayman
    SKU:25445 - 1 mg

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  • GPR39-C3 is a potent agonist of the orphan G protein-coupled receptor GPR39 with EC50 values of 0.8 and 0.4 nM for cAMP production in HEK293 cells expressing human and rat receptors, respectively.{42282} It is selective for GPR39 over a panel of kinases (IC50s = >10 μM), ghrelin and neurotensin-1 receptors (IC50s = >30 μM), and a variety of enzymes, transporters, or G protein-coupled receptors. GPR39-C3 increases secretion of glucagon-like peptide 1 (GLP-1; Item No. 24460) in STC-1 mouse enteroendocrine cells (EC50 = 0.06 μM) and is protective against cytokine-induced cell death in INS-1E rat insulinoma cells (EC50 = 0.02 μM). In vivo, GPR39-C3 (30 mg/kg) increases the amount of active GLP-1 in sera by 6-fold in glucose-challenged mice when administered concurrently with a dipeptidyl peptidase 4 (DPP-4) inhibitor.  

     

    Brand:
    Cayman
    SKU:25445 - 10 mg

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  • GPR39-C3 is a potent agonist of the orphan G protein-coupled receptor GPR39 with EC50 values of 0.8 and 0.4 nM for cAMP production in HEK293 cells expressing human and rat receptors, respectively.{42282} It is selective for GPR39 over a panel of kinases (IC50s = >10 μM), ghrelin and neurotensin-1 receptors (IC50s = >30 μM), and a variety of enzymes, transporters, or G protein-coupled receptors. GPR39-C3 increases secretion of glucagon-like peptide 1 (GLP-1; Item No. 24460) in STC-1 mouse enteroendocrine cells (EC50 = 0.06 μM) and is protective against cytokine-induced cell death in INS-1E rat insulinoma cells (EC50 = 0.02 μM). In vivo, GPR39-C3 (30 mg/kg) increases the amount of active GLP-1 in sera by 6-fold in glucose-challenged mice when administered concurrently with a dipeptidyl peptidase 4 (DPP-4) inhibitor.  

     

    Brand:
    Cayman
    SKU:25445 - 25 mg

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  • GPR39-C3 is a potent agonist of the orphan G protein-coupled receptor GPR39 with EC50 values of 0.8 and 0.4 nM for cAMP production in HEK293 cells expressing human and rat receptors, respectively.{42282} It is selective for GPR39 over a panel of kinases (IC50s = >10 μM), ghrelin and neurotensin-1 receptors (IC50s = >30 μM), and a variety of enzymes, transporters, or G protein-coupled receptors. GPR39-C3 increases secretion of glucagon-like peptide 1 (GLP-1; Item No. 24460) in STC-1 mouse enteroendocrine cells (EC50 = 0.06 μM) and is protective against cytokine-induced cell death in INS-1E rat insulinoma cells (EC50 = 0.02 μM). In vivo, GPR39-C3 (30 mg/kg) increases the amount of active GLP-1 in sera by 6-fold in glucose-challenged mice when administered concurrently with a dipeptidyl peptidase 4 (DPP-4) inhibitor.  

     

    Brand:
    Cayman
    SKU:25445 - 5 mg

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  • Full activation of peroxisome proliferator-activated receptor γ (PPARγ), e.g., using thiazolidinediones, effectively treats insulin resistance and type 2 diabetes but also commonly promotes weight gain, hyperphagia, and edema.{21030} GQ-16 is a partial agonist for PPARγ (Ki = 160 nM) which induces adipogenesis significantly less than the full activator rosiglitazone.{21030} Like rosiglitazone, GQ-16 reverses high fat diet-mediated impairments in insulin signaling.{21030} However, GQ-16 does not induce weight gain, hyperphagia, or edema. GQ-16 does not activate PPARα, PPARβ/δ, or RXRα.{21030}  

     

    Brand:
    Cayman
    SKU:11908 - 10 mg

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  • Full activation of peroxisome proliferator-activated receptor γ (PPARγ), e.g., using thiazolidinediones, effectively treats insulin resistance and type 2 diabetes but also commonly promotes weight gain, hyperphagia, and edema.{21030} GQ-16 is a partial agonist for PPARγ (Ki = 160 nM) which induces adipogenesis significantly less than the full activator rosiglitazone.{21030} Like rosiglitazone, GQ-16 reverses high fat diet-mediated impairments in insulin signaling.{21030} However, GQ-16 does not induce weight gain, hyperphagia, or edema. GQ-16 does not activate PPARα, PPARβ/δ, or RXRα.{21030}  

     

    Brand:
    Cayman
    SKU:11908 - 100 mg

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  • Full activation of peroxisome proliferator-activated receptor γ (PPARγ), e.g., using thiazolidinediones, effectively treats insulin resistance and type 2 diabetes but also commonly promotes weight gain, hyperphagia, and edema.{21030} GQ-16 is a partial agonist for PPARγ (Ki = 160 nM) which induces adipogenesis significantly less than the full activator rosiglitazone.{21030} Like rosiglitazone, GQ-16 reverses high fat diet-mediated impairments in insulin signaling.{21030} However, GQ-16 does not induce weight gain, hyperphagia, or edema. GQ-16 does not activate PPARα, PPARβ/δ, or RXRα.{21030}  

     

    Brand:
    Cayman
    SKU:11908 - 5 mg

    Available on backorder

  • Full activation of peroxisome proliferator-activated receptor γ (PPARγ), e.g., using thiazolidinediones, effectively treats insulin resistance and type 2 diabetes but also commonly promotes weight gain, hyperphagia, and edema.{21030} GQ-16 is a partial agonist for PPARγ (Ki = 160 nM) which induces adipogenesis significantly less than the full activator rosiglitazone.{21030} Like rosiglitazone, GQ-16 reverses high fat diet-mediated impairments in insulin signaling.{21030} However, GQ-16 does not induce weight gain, hyperphagia, or edema. GQ-16 does not activate PPARα, PPARβ/δ, or RXRα.{21030}  

     

    Brand:
    Cayman
    SKU:11908 - 50 mg

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  • GR113808 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT4.{42967} It binds to 5-HT4 receptors with an IC50 value of 0.4 nM in COS-7 cells expressing the human recombinant receptor and in guinea pig striatal membranes (IC50 = 0.5 nM).{42968} GR113808 is selective for 5-HT4 receptors over 5-HT1 receptors (Kis = >10 µM in dog saphenous vein and porcine vena cava), as well as 5-HT2 and 5-HT3 receptors (Kis = >10 and 1 μM in rabbit thoracic aorta and rat cerebral cortex, respectively).{42967} It is also selective for 5-HT4 over adenosine, adrenergic, dopamine, GABA, muscarinic, nicotinic, histamine, and NMDA receptors (Kis = >10 μM for all). GR113808 inhibits relaxation induced by 5-HT (Item No. 14332) in rat thoracic esophagus precontracted by carbachol (carbamoylcholine; Item No. 14486; pA2 = 9.3). In vivo, GR113808 inhibits 5-methoxytryptamine-induced tachycardia in anaesthetized piglets.  

     

    Brand:
    Cayman
    SKU:28733 - 10 mg

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  • GR113808 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT4.{42967} It binds to 5-HT4 receptors with an IC50 value of 0.4 nM in COS-7 cells expressing the human recombinant receptor and in guinea pig striatal membranes (IC50 = 0.5 nM).{42968} GR113808 is selective for 5-HT4 receptors over 5-HT1 receptors (Kis = >10 µM in dog saphenous vein and porcine vena cava), as well as 5-HT2 and 5-HT3 receptors (Kis = >10 and 1 μM in rabbit thoracic aorta and rat cerebral cortex, respectively).{42967} It is also selective for 5-HT4 over adenosine, adrenergic, dopamine, GABA, muscarinic, nicotinic, histamine, and NMDA receptors (Kis = >10 μM for all). GR113808 inhibits relaxation induced by 5-HT (Item No. 14332) in rat thoracic esophagus precontracted by carbachol (carbamoylcholine; Item No. 14486; pA2 = 9.3). In vivo, GR113808 inhibits 5-methoxytryptamine-induced tachycardia in anaesthetized piglets.  

     

    Brand:
    Cayman
    SKU:28733 - 25 mg

    Available on backorder

  • GR113808 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT4.{42967} It binds to 5-HT4 receptors with an IC50 value of 0.4 nM in COS-7 cells expressing the human recombinant receptor and in guinea pig striatal membranes (IC50 = 0.5 nM).{42968} GR113808 is selective for 5-HT4 receptors over 5-HT1 receptors (Kis = >10 µM in dog saphenous vein and porcine vena cava), as well as 5-HT2 and 5-HT3 receptors (Kis = >10 and 1 μM in rabbit thoracic aorta and rat cerebral cortex, respectively).{42967} It is also selective for 5-HT4 over adenosine, adrenergic, dopamine, GABA, muscarinic, nicotinic, histamine, and NMDA receptors (Kis = >10 μM for all). GR113808 inhibits relaxation induced by 5-HT (Item No. 14332) in rat thoracic esophagus precontracted by carbachol (carbamoylcholine; Item No. 14486; pA2 = 9.3). In vivo, GR113808 inhibits 5-methoxytryptamine-induced tachycardia in anaesthetized piglets.  

     

    Brand:
    Cayman
    SKU:28733 - 5 mg

    Available on backorder

  • GR113808 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT4.{42967} It binds to 5-HT4 receptors with an IC50 value of 0.4 nM in COS-7 cells expressing the human recombinant receptor and in guinea pig striatal membranes (IC50 = 0.5 nM).{42968} GR113808 is selective for 5-HT4 receptors over 5-HT1 receptors (Kis = >10 µM in dog saphenous vein and porcine vena cava), as well as 5-HT2 and 5-HT3 receptors (Kis = >10 and 1 μM in rabbit thoracic aorta and rat cerebral cortex, respectively).{42967} It is also selective for 5-HT4 over adenosine, adrenergic, dopamine, GABA, muscarinic, nicotinic, histamine, and NMDA receptors (Kis = >10 μM for all). GR113808 inhibits relaxation induced by 5-HT (Item No. 14332) in rat thoracic esophagus precontracted by carbachol (carbamoylcholine; Item No. 14486; pA2 = 9.3). In vivo, GR113808 inhibits 5-methoxytryptamine-induced tachycardia in anaesthetized piglets.  

     

    Brand:
    Cayman
    SKU:28733 - 50 mg

    Available on backorder

  • GR127935 is an antagonist of the serotonin (5-HT) receptor subtypes 5-HT1B, 5-HT1Dα, and 5-HT1Dβ (IC50s = 3.16, 1.26, and 0.13 nM, respectively).{53337} It is selective for the 5-HT1B and 5-HT1D receptors over other 5-HT receptors (IC50s = 39.81->10,000 nM in radioligand binding assays). GR127935 increases extracellular 5-HT levels in the guinea pig frontal cortex and prevents increases in 5-HT in rat frontal cortex induced by the selective serotonin reuptake inhibitor paroxetine (Item No. 14998).{53338} It enhances memory consolidation in an autoshaping learning task in rats when administered post-training at a dose of 10 mg/kg.{53339} It has been used to elucidate the 5-HT receptor subtypes involved in the anti-inflammatory activity of sumatriptan (Item No. 14600) following myocardial ischemia-reperfusion injury and testicular torsion/detorsion.{53340,53341}  

     

    Brand:
    Cayman
    SKU:29651 - 10 mg

    Available on backorder

  • GR127935 is an antagonist of the serotonin (5-HT) receptor subtypes 5-HT1B, 5-HT1Dα, and 5-HT1Dβ (IC50s = 3.16, 1.26, and 0.13 nM, respectively).{53337} It is selective for the 5-HT1B and 5-HT1D receptors over other 5-HT receptors (IC50s = 39.81->10,000 nM in radioligand binding assays). GR127935 increases extracellular 5-HT levels in the guinea pig frontal cortex and prevents increases in 5-HT in rat frontal cortex induced by the selective serotonin reuptake inhibitor paroxetine (Item No. 14998).{53338} It enhances memory consolidation in an autoshaping learning task in rats when administered post-training at a dose of 10 mg/kg.{53339} It has been used to elucidate the 5-HT receptor subtypes involved in the anti-inflammatory activity of sumatriptan (Item No. 14600) following myocardial ischemia-reperfusion injury and testicular torsion/detorsion.{53340,53341}  

     

    Brand:
    Cayman
    SKU:29651 - 25 mg

    Available on backorder

  • GR127935 is an antagonist of the serotonin (5-HT) receptor subtypes 5-HT1B, 5-HT1Dα, and 5-HT1Dβ (IC50s = 3.16, 1.26, and 0.13 nM, respectively).{53337} It is selective for the 5-HT1B and 5-HT1D receptors over other 5-HT receptors (IC50s = 39.81->10,000 nM in radioligand binding assays). GR127935 increases extracellular 5-HT levels in the guinea pig frontal cortex and prevents increases in 5-HT in rat frontal cortex induced by the selective serotonin reuptake inhibitor paroxetine (Item No. 14998).{53338} It enhances memory consolidation in an autoshaping learning task in rats when administered post-training at a dose of 10 mg/kg.{53339} It has been used to elucidate the 5-HT receptor subtypes involved in the anti-inflammatory activity of sumatriptan (Item No. 14600) following myocardial ischemia-reperfusion injury and testicular torsion/detorsion.{53340,53341}  

     

    Brand:
    Cayman
    SKU:29651 - 5 mg

    Available on backorder

  • GR127935 is an antagonist of the serotonin (5-HT) receptor subtypes 5-HT1B, 5-HT1Dα, and 5-HT1Dβ (IC50s = 3.16, 1.26, and 0.13 nM, respectively).{53337} It is selective for the 5-HT1B and 5-HT1D receptors over other 5-HT receptors (IC50s = 39.81->10,000 nM in radioligand binding assays). GR127935 increases extracellular 5-HT levels in the guinea pig frontal cortex and prevents increases in 5-HT in rat frontal cortex induced by the selective serotonin reuptake inhibitor paroxetine (Item No. 14998).{53338} It enhances memory consolidation in an autoshaping learning task in rats when administered post-training at a dose of 10 mg/kg.{53339} It has been used to elucidate the 5-HT receptor subtypes involved in the anti-inflammatory activity of sumatriptan (Item No. 14600) following myocardial ischemia-reperfusion injury and testicular torsion/detorsion.{53340,53341}  

     

    Brand:
    Cayman
    SKU:29651 - 50 mg

    Available on backorder

  • GR148672X is an inhibitor of triacylglycerol hydrolase/carboxylesterase 1 (TGH/CES1; IC50 = 4 nM for the human hepatic enzyme).{45656,45657} It is selective for TGH/CES1 over lipoprotein lipase (LPL) at 5 μM.{45656} GR148672X (25 mg/kg twice per day) decreases plasma levels of triglycerides, total, VLDL, and LDL cholesterol, and apolipoprotein B-100 (ApoB-100) in hamsters.  

     

    Brand:
    Cayman
    SKU:28756 - 1 mg

    Available on backorder

  • GR148672X is an inhibitor of triacylglycerol hydrolase/carboxylesterase 1 (TGH/CES1; IC50 = 4 nM for the human hepatic enzyme).{45656,45657} It is selective for TGH/CES1 over lipoprotein lipase (LPL) at 5 μM.{45656} GR148672X (25 mg/kg twice per day) decreases plasma levels of triglycerides, total, VLDL, and LDL cholesterol, and apolipoprotein B-100 (ApoB-100) in hamsters.  

     

    Brand:
    Cayman
    SKU:28756 - 10 mg

    Available on backorder

  • GR148672X is an inhibitor of triacylglycerol hydrolase/carboxylesterase 1 (TGH/CES1; IC50 = 4 nM for the human hepatic enzyme).{45656,45657} It is selective for TGH/CES1 over lipoprotein lipase (LPL) at 5 μM.{45656} GR148672X (25 mg/kg twice per day) decreases plasma levels of triglycerides, total, VLDL, and LDL cholesterol, and apolipoprotein B-100 (ApoB-100) in hamsters.  

     

    Brand:
    Cayman
    SKU:28756 - 5 mg

    Available on backorder

  • GR159897 is a nonpeptide antagonist of the neurokinin-2 (NK2) receptor.{60141} It binds to NK2 receptors (Ki = 0.32 nM) and is selective for NK2 over NK1 and NK3 receptors in radioligand binding assays (Kis = 5,010 and >1,000 nM, respectively). GR159897 inhibits contractions induced by the NK2 receptor agonist GR64349 in isolated guinea pig trachea (pA2 = 8.7). In vivo GR159897 (0.12 mg/kg) inhibits GR64349-induced bronchoconstriction in anesthetized guinea pigs. GR159897 (0.2-50 µg/kg) increases the amount of time spent in the front of the cage during confrontation with a human observer, a marker of anxiolytic-like activity, in marmosets.{60142}  

     

    Brand:
    Cayman
    SKU:32774 - 1 mg

    Available on backorder

  • GR159897 is a nonpeptide antagonist of the neurokinin-2 (NK2) receptor.{60141} It binds to NK2 receptors (Ki = 0.32 nM) and is selective for NK2 over NK1 and NK3 receptors in radioligand binding assays (Kis = 5,010 and >1,000 nM, respectively). GR159897 inhibits contractions induced by the NK2 receptor agonist GR64349 in isolated guinea pig trachea (pA2 = 8.7). In vivo GR159897 (0.12 mg/kg) inhibits GR64349-induced bronchoconstriction in anesthetized guinea pigs. GR159897 (0.2-50 µg/kg) increases the amount of time spent in the front of the cage during confrontation with a human observer, a marker of anxiolytic-like activity, in marmosets.{60142}  

     

    Brand:
    Cayman
    SKU:32774 - 10 mg

    Available on backorder

  • GR159897 is a nonpeptide antagonist of the neurokinin-2 (NK2) receptor.{60141} It binds to NK2 receptors (Ki = 0.32 nM) and is selective for NK2 over NK1 and NK3 receptors in radioligand binding assays (Kis = 5,010 and >1,000 nM, respectively). GR159897 inhibits contractions induced by the NK2 receptor agonist GR64349 in isolated guinea pig trachea (pA2 = 8.7). In vivo GR159897 (0.12 mg/kg) inhibits GR64349-induced bronchoconstriction in anesthetized guinea pigs. GR159897 (0.2-50 µg/kg) increases the amount of time spent in the front of the cage during confrontation with a human observer, a marker of anxiolytic-like activity, in marmosets.{60142}  

     

    Brand:
    Cayman
    SKU:32774 - 5 mg

    Available on backorder

  • GR24 is a synthetic strigalactone and plant growth regulator.{53559,53560} It stimulates the germination of Striga and Orobanche parasitic weed seeds (EC50s = 5-50 nM).{53559} GR24 increases root-hair length and decreases the number of lateral roots in Arabidopsis.{53560}  

     

    Brand:
    Cayman
    SKU:-
  • GR79236 is a selective agonist of adenosine A1 receptors (Kis = 3.1 and 1,300 nM for adenosine A1 and A2 receptors, respectively, in rat brain).{47666} GR79236 inhibits cAMP accumulation induced by isoprenaline (isoproterenol; Item No. 15592) in DDT1MF-2 hamster smooth muscle cells (IC50 = 2.6 nM) but only decreases contractility in isolated guinea pig atria with an EC50 value of 1,500 nM. It also inhibits lipolysis induced by norepinephrine (Item No. 16673) in rat adipocytes (EC50 = 0.83 nM).{47667} GR79236 decreases locomotor activity and inhibits DMCM-induced seizures in mice (ED50s = 0.13 and 0.3 mg/kg, respectively).{47666} It also decreases mean blood pressure by 74% in anesthetized rats when administered at a dose of 0.1 mg/kg.  

     

    Brand:
    Cayman
    SKU:28430 - 1 mg

    Available on backorder

  • GR79236 is a selective agonist of adenosine A1 receptors (Kis = 3.1 and 1,300 nM for adenosine A1 and A2 receptors, respectively, in rat brain).{47666} GR79236 inhibits cAMP accumulation induced by isoprenaline (isoproterenol; Item No. 15592) in DDT1MF-2 hamster smooth muscle cells (IC50 = 2.6 nM) but only decreases contractility in isolated guinea pig atria with an EC50 value of 1,500 nM. It also inhibits lipolysis induced by norepinephrine (Item No. 16673) in rat adipocytes (EC50 = 0.83 nM).{47667} GR79236 decreases locomotor activity and inhibits DMCM-induced seizures in mice (ED50s = 0.13 and 0.3 mg/kg, respectively).{47666} It also decreases mean blood pressure by 74% in anesthetized rats when administered at a dose of 0.1 mg/kg.  

     

    Brand:
    Cayman
    SKU:28430 - 10 mg

    Available on backorder

  • GR79236 is a selective agonist of adenosine A1 receptors (Kis = 3.1 and 1,300 nM for adenosine A1 and A2 receptors, respectively, in rat brain).{47666} GR79236 inhibits cAMP accumulation induced by isoprenaline (isoproterenol; Item No. 15592) in DDT1MF-2 hamster smooth muscle cells (IC50 = 2.6 nM) but only decreases contractility in isolated guinea pig atria with an EC50 value of 1,500 nM. It also inhibits lipolysis induced by norepinephrine (Item No. 16673) in rat adipocytes (EC50 = 0.83 nM).{47667} GR79236 decreases locomotor activity and inhibits DMCM-induced seizures in mice (ED50s = 0.13 and 0.3 mg/kg, respectively).{47666} It also decreases mean blood pressure by 74% in anesthetized rats when administered at a dose of 0.1 mg/kg.  

     

    Brand:
    Cayman
    SKU:28430 - 25 mg

    Available on backorder

  • GR79236 is a selective agonist of adenosine A1 receptors (Kis = 3.1 and 1,300 nM for adenosine A1 and A2 receptors, respectively, in rat brain).{47666} GR79236 inhibits cAMP accumulation induced by isoprenaline (isoproterenol; Item No. 15592) in DDT1MF-2 hamster smooth muscle cells (IC50 = 2.6 nM) but only decreases contractility in isolated guinea pig atria with an EC50 value of 1,500 nM. It also inhibits lipolysis induced by norepinephrine (Item No. 16673) in rat adipocytes (EC50 = 0.83 nM).{47667} GR79236 decreases locomotor activity and inhibits DMCM-induced seizures in mice (ED50s = 0.13 and 0.3 mg/kg, respectively).{47666} It also decreases mean blood pressure by 74% in anesthetized rats when administered at a dose of 0.1 mg/kg.  

     

    Brand:
    Cayman
    SKU:28430 - 5 mg

    Available on backorder

  • GRA Ex-25 is a glucagon receptor (GCGR) antagonist (IC50s = 55 and 56 nM for the human and rat receptors, respectively).{49499} It inhibits adenylate cyclase activity induced by glucagon (Item No. 24204) with a Ki value of 254 nM.{49500} GRA Ex-25 (3 mg/kg, i.v.) reduces glucagon-induced increases in blood glucose levels in rats.{49499}  

     

    Brand:
    Cayman
    SKU:29727 - 1 mg

    Available on backorder

  • GRA Ex-25 is a glucagon receptor (GCGR) antagonist (IC50s = 55 and 56 nM for the human and rat receptors, respectively).{49499} It inhibits adenylate cyclase activity induced by glucagon (Item No. 24204) with a Ki value of 254 nM.{49500} GRA Ex-25 (3 mg/kg, i.v.) reduces glucagon-induced increases in blood glucose levels in rats.{49499}  

     

    Brand:
    Cayman
    SKU:29727 - 10 mg

    Available on backorder

  • GRA Ex-25 is a glucagon receptor (GCGR) antagonist (IC50s = 55 and 56 nM for the human and rat receptors, respectively).{49499} It inhibits adenylate cyclase activity induced by glucagon (Item No. 24204) with a Ki value of 254 nM.{49500} GRA Ex-25 (3 mg/kg, i.v.) reduces glucagon-induced increases in blood glucose levels in rats.{49499}  

     

    Brand:
    Cayman
    SKU:29727 - 25 mg

    Available on backorder

  • GRA Ex-25 is a glucagon receptor (GCGR) antagonist (IC50s = 55 and 56 nM for the human and rat receptors, respectively).{49499} It inhibits adenylate cyclase activity induced by glucagon (Item No. 24204) with a Ki value of 254 nM.{49500} GRA Ex-25 (3 mg/kg, i.v.) reduces glucagon-induced increases in blood glucose levels in rats.{49499}  

     

    Brand:
    Cayman
    SKU:29727 - 5 mg

    Available on backorder

  • Gracillin is a steroidal saponin that has been found in C. speciosus and has diverse biological activities.{43305,43306,43307} It reduces cell growth in a panel of 58 leukemia, non-small cell lung, colon, CNS, prostate, melanoma, ovarian, renal, and breast cancer cell lines (GI50s = 0.58-2.44 μM).{43305} Gracillin reduces growth of fish Ich parasite (I. multifiliis) theronts (EC50 = 0.53 mg/L) and induces 100 and 92.5% mortality of I. multifiliis protomonts and encysted tomonts, respectively, when used at a concentration of 0.8 mg/L.{43306} It decreases the number of I. multifiliis-infected goldfish by approximately 75% when used at a concentration of 1 mg/L in tank water. Gracillin (100 mg/kg) reduces ear edema induced by arachidonic acid (Item No. 90010) in mice.{43307}  

     

    Brand:
    Cayman
    SKU:11848 - 1 mg

    Available on backorder

  • Gracillin is a steroidal saponin that has been found in C. speciosus and has diverse biological activities.{43305,43306,43307} It reduces cell growth in a panel of 58 leukemia, non-small cell lung, colon, CNS, prostate, melanoma, ovarian, renal, and breast cancer cell lines (GI50s = 0.58-2.44 μM).{43305} Gracillin reduces growth of fish Ich parasite (I. multifiliis) theronts (EC50 = 0.53 mg/L) and induces 100 and 92.5% mortality of I. multifiliis protomonts and encysted tomonts, respectively, when used at a concentration of 0.8 mg/L.{43306} It decreases the number of I. multifiliis-infected goldfish by approximately 75% when used at a concentration of 1 mg/L in tank water. Gracillin (100 mg/kg) reduces ear edema induced by arachidonic acid (Item No. 90010) in mice.{43307}  

     

    Brand:
    Cayman
    SKU:11848 - 10 mg

    Available on backorder

  • Gracillin is a steroidal saponin that has been found in C. speciosus and has diverse biological activities.{43305,43306,43307} It reduces cell growth in a panel of 58 leukemia, non-small cell lung, colon, CNS, prostate, melanoma, ovarian, renal, and breast cancer cell lines (GI50s = 0.58-2.44 μM).{43305} Gracillin reduces growth of fish Ich parasite (I. multifiliis) theronts (EC50 = 0.53 mg/L) and induces 100 and 92.5% mortality of I. multifiliis protomonts and encysted tomonts, respectively, when used at a concentration of 0.8 mg/L.{43306} It decreases the number of I. multifiliis-infected goldfish by approximately 75% when used at a concentration of 1 mg/L in tank water. Gracillin (100 mg/kg) reduces ear edema induced by arachidonic acid (Item No. 90010) in mice.{43307}  

     

    Brand:
    Cayman
    SKU:11848 - 25 mg

    Available on backorder

  • Gracillin is a steroidal saponin that has been found in C. speciosus and has diverse biological activities.{43305,43306,43307} It reduces cell growth in a panel of 58 leukemia, non-small cell lung, colon, CNS, prostate, melanoma, ovarian, renal, and breast cancer cell lines (GI50s = 0.58-2.44 μM).{43305} Gracillin reduces growth of fish Ich parasite (I. multifiliis) theronts (EC50 = 0.53 mg/L) and induces 100 and 92.5% mortality of I. multifiliis protomonts and encysted tomonts, respectively, when used at a concentration of 0.8 mg/L.{43306} It decreases the number of I. multifiliis-infected goldfish by approximately 75% when used at a concentration of 1 mg/L in tank water. Gracillin (100 mg/kg) reduces ear edema induced by arachidonic acid (Item No. 90010) in mice.{43307}  

     

    Brand:
    Cayman
    SKU:11848 - 5 mg

    Available on backorder

  • Gramicidin is a polypeptide antibiotic mixture of gramicidin A (Item No. 26384), gramicidin B, and gramicidin C originally isolated from B. brevis.{47490} It is also a component of the antibiotic tyrothricin (Item No. 22177).{47491} Gramicidin is active against the Gram-positive bacterium S. aureus but not Gram-negative E. coli.{38058} It also protects mice from Pneumococcus infection in vivo when administered at a dose of 0.002 mg/animal. Gramicidin inhibits growth of bacteria by forming pores and channels in the cell wall, which increases its permeability to monovalent cations.{47490} Formulations containing gramicidin have been used as topical agents in the treatment of bacterial skin infections.  

     

    Brand:
    Cayman
    SKU:28251 - 250 mg

    Available on backorder

  • Gramicidin A is a peptide component of gramicidin, an antibiotic mixture originally isolated from B. brevis.{47164} Gramicidin A is a highly hydrophobic channel-forming ionophore that forms channels in model membranes that are permeable to monovalent cations. It induces degradation of hypoxia inducible factor 1 α (HIF-1α) in HEK293 cells and reduces growth in a human renal cell carcinoma mouse xenograft model when administered at a dose of 0.22 mg/kg three times per week.{47165} Gramicidin A has commonly been used to study channel structure and function.{47164}  

     

    Brand:
    Cayman
    SKU:26384 - 1 mg

    Available on backorder

  • Gramicidin A is a peptide component of gramicidin, an antibiotic mixture originally isolated from B. brevis.{47164} Gramicidin A is a highly hydrophobic channel-forming ionophore that forms channels in model membranes that are permeable to monovalent cations. It induces degradation of hypoxia inducible factor 1 α (HIF-1α) in HEK293 cells and reduces growth in a human renal cell carcinoma mouse xenograft model when administered at a dose of 0.22 mg/kg three times per week.{47165} Gramicidin A has commonly been used to study channel structure and function.{47164}  

     

    Brand:
    Cayman
    SKU:26384 - 5 mg

    Available on backorder

  • Gramine (Item No. 23401) is an analytical reference standard that is categorized as an alkaloid.{38364} It is used as an intermediate in the synthesis of tryptophans and tryptamines. This product is intended for research and forensic applications.  

     

    Brand:
    Cayman
    SKU:23401 - 5 mg

    Available on backorder

  • Gramine (Item No. 23401) is an analytical reference standard that is categorized as an alkaloid.{38364} It is used as an intermediate in the synthesis of tryptophans and tryptamines. This product is intended for research and forensic applications.  

     

    Brand:
    Cayman
    SKU:23401 - 50 mg

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  • Granisetron is an antagonist of the serotonin (5-HT) receptor subtype 5-HT3 (Ki = 3.9 nM) with antiemetic activity.{23960,47619} It is selective for 5-HT3 over 5-HT4 receptors (Ki = >1,000 nM).{23960} Granisetron (0.3, 1, and 3 mg/kg, p.o.) increases the latency to first vomiting episode and reduces the number of vomiting episodes in a canine model of emesis induced by cisplatin (Item No. 13119).{47619} It also increases the latency to first vomiting episode and reduces the number of vomiting and retching episodes in a ferret model of emesis induced by doxorubicin (Item No. 15007) and cyclophosphamide (Item No. 13849) when administered at doses of 0.1, 0.3, and 1 mg/kg. Formulations containing granisetron have been used in the prevention of nausea and vomiting associated with chemotherapy.  

     

    Brand:
    Cayman
    SKU:21239 -

    Out of stock

  • Granisetron is an antagonist of the serotonin (5-HT) receptor subtype 5-HT3 (Ki = 3.9 nM) with antiemetic activity.{23960,47619} It is selective for 5-HT3 over 5-HT4 receptors (Ki = >1,000 nM).{23960} Granisetron (0.3, 1, and 3 mg/kg, p.o.) increases the latency to first vomiting episode and reduces the number of vomiting episodes in a canine model of emesis induced by cisplatin (Item No. 13119).{47619} It also increases the latency to first vomiting episode and reduces the number of vomiting and retching episodes in a ferret model of emesis induced by doxorubicin (Item No. 15007) and cyclophosphamide (Item No. 13849) when administered at doses of 0.1, 0.3, and 1 mg/kg. Formulations containing granisetron have been used in the prevention of nausea and vomiting associated with chemotherapy.  

     

    Brand:
    Cayman
    SKU:21239 -

    Out of stock

  • Granisetron-d3 is intended for use as an internal standard for the quantification of granisetron (Item No. 21239) by GC- or LC-MS. Granisetron is an antagonist of the serotonin (5-HT) receptor subtype 5-HT3 (Ki = 3.9 nM) with antiemetic activity.{23960,47619} It is selective for 5-HT3 over 5-HT4 receptors (Ki = >1,000 nM).{23960} Granisetron (0.3, 1, and 3 mg/kg, p.o.) increases the latency to a first vomiting episode and reduces the number of vomiting episodes in a canine model of emesis induced by cisplatin (Item No. 13119).{47619} It also increases the latency to a first vomiting episode and reduces the number of vomiting and retching episodes in a ferret model of emesis induced by doxorubicin (Item No. 15007) and cyclophosphamide (Item No. 13849) when administered at doses of 0.1, 0.3, and 1 mg/kg. Formulations containing granisetron have been used in the prevention of nausea and vomiting associated with chemotherapy.  

     

    Brand:
    Cayman
    SKU:31786 - 1 mg

    Available on backorder

  • Graphislactone A is an antioxidant produced by Cephalosporium IFB-E001 and M. olivacea.{38444,38445} It exhibits dose-dependent scavenging activity against DPPH radicals and metal ion-dependent hydroxyl radicals in vitro.{38444} Graphislactone A reduces peroxidation of human LDL and slows peroxidation of linoleic acid (Item Nos. 90150 | 21909) by 4.4-fold. It also inhibits acetylcholinesterase (AChE) with an IC50 value of 27 μM.{38445}  

     

    Brand:
    Cayman
    SKU:23643 - 1 mg

    Available on backorder

  • Graphislactone A is an antioxidant produced by Cephalosporium IFB-E001 and M. olivacea.{38444,38445} It exhibits dose-dependent scavenging activity against DPPH radicals and metal ion-dependent hydroxyl radicals in vitro.{38444} Graphislactone A reduces peroxidation of human LDL and slows peroxidation of linoleic acid (Item Nos. 90150 | 21909) by 4.4-fold. It also inhibits acetylcholinesterase (AChE) with an IC50 value of 27 μM.{38445}  

     

    Brand:
    Cayman
    SKU:23643 - 5 mg

    Available on backorder

  • Grassofermata is an inhibitor of fatty acid transport.{43557} It inhibits C1-BODIPY-C12 uptake in HepG2, Caco-2, C2C12, and INS-1E cells (IC50s = 8.1-10.6 μM).{43557} Grassofermata prevents palmitate-mediated lipid accumulation and cell death in HepG2 cells and primary hepatocytes. In vivo, grassofermata (300 mg/kg) decreases absorption of 13C-oleate in mice.  

     

    Brand:
    Cayman
    SKU:26202 - 1 mg

    Available on backorder

  • Grassofermata is an inhibitor of fatty acid transport.{43557} It inhibits C1-BODIPY-C12 uptake in HepG2, Caco-2, C2C12, and INS-1E cells (IC50s = 8.1-10.6 μM).{43557} Grassofermata prevents palmitate-mediated lipid accumulation and cell death in HepG2 cells and primary hepatocytes. In vivo, grassofermata (300 mg/kg) decreases absorption of 13C-oleate in mice.  

     

    Brand:
    Cayman
    SKU:26202 - 10 mg

    Available on backorder

  • Grassofermata is an inhibitor of fatty acid transport.{43557} It inhibits C1-BODIPY-C12 uptake in HepG2, Caco-2, C2C12, and INS-1E cells (IC50s = 8.1-10.6 μM).{43557} Grassofermata prevents palmitate-mediated lipid accumulation and cell death in HepG2 cells and primary hepatocytes. In vivo, grassofermata (300 mg/kg) decreases absorption of 13C-oleate in mice.  

     

    Brand:
    Cayman
    SKU:26202 - 25 mg

    Available on backorder

  • Grassofermata is an inhibitor of fatty acid transport.{43557} It inhibits C1-BODIPY-C12 uptake in HepG2, Caco-2, C2C12, and INS-1E cells (IC50s = 8.1-10.6 μM).{43557} Grassofermata prevents palmitate-mediated lipid accumulation and cell death in HepG2 cells and primary hepatocytes. In vivo, grassofermata (300 mg/kg) decreases absorption of 13C-oleate in mice.  

     

    Brand:
    Cayman
    SKU:26202 - 5 mg

    Available on backorder

  • Grazoprevir is a pan-genotypic protease inhibitor that binds to hepatitis C virus (HCV) non-structural protein 3/4A (NS3/4A), a serine protease essential for viral replication.{36012} Grazoprevir has potent in vitro activity against major HCV genotypes (Kis = 0.1, 0.1, 0.08, 0.15, and 0.9 nM for genotypes 1a, 1b, 2a, 2b, and 3a, respectively) and common resistance genotypes (Kis = 0.07, 0.14, and 0.30 nM for genotypes 1b R155K, D165V, and D168Y, respectively).  Grazoprevir inhibits the NS3/4A protease in an in vitro replicon system with EC50 values of 2 and 8 nM for genotypes 1a and 2a, respectively. Formulations containing grazoprevir are used in combination therapies to treat HCV.{36013}    

     

    Brand:
    Cayman
    SKU:21816 -

    Out of stock

  • Grazoprevir is a pan-genotypic protease inhibitor that binds to hepatitis C virus (HCV) non-structural protein 3/4A (NS3/4A), a serine protease essential for viral replication.{36012} Grazoprevir has potent in vitro activity against major HCV genotypes (Kis = 0.1, 0.1, 0.08, 0.15, and 0.9 nM for genotypes 1a, 1b, 2a, 2b, and 3a, respectively) and common resistance genotypes (Kis = 0.07, 0.14, and 0.30 nM for genotypes 1b R155K, D165V, and D168Y, respectively).  Grazoprevir inhibits the NS3/4A protease in an in vitro replicon system with EC50 values of 2 and 8 nM for genotypes 1a and 2a, respectively. Formulations containing grazoprevir are used in combination therapies to treat HCV.{36013}    

     

    Brand:
    Cayman
    SKU:21816 -

    Out of stock

  • Grazoprevir is a pan-genotypic protease inhibitor that binds to hepatitis C virus (HCV) non-structural protein 3/4A (NS3/4A), a serine protease essential for viral replication.{36012} Grazoprevir has potent in vitro activity against major HCV genotypes (Kis = 0.1, 0.1, 0.08, 0.15, and 0.9 nM for genotypes 1a, 1b, 2a, 2b, and 3a, respectively) and common resistance genotypes (Kis = 0.07, 0.14, and 0.30 nM for genotypes 1b R155K, D165V, and D168Y, respectively).  Grazoprevir inhibits the NS3/4A protease in an in vitro replicon system with EC50 values of 2 and 8 nM for genotypes 1a and 2a, respectively. Formulations containing grazoprevir are used in combination therapies to treat HCV.{36013}    

     

    Brand:
    Cayman
    SKU:21816 -

    Out of stock

  • Grazoprevir is a pan-genotypic protease inhibitor that binds to hepatitis C virus (HCV) non-structural protein 3/4A (NS3/4A), a serine protease essential for viral replication.{36012} Grazoprevir has potent in vitro activity against major HCV genotypes (Kis = 0.1, 0.1, 0.08, 0.15, and 0.9 nM for genotypes 1a, 1b, 2a, 2b, and 3a, respectively) and common resistance genotypes (Kis = 0.07, 0.14, and 0.30 nM for genotypes 1b R155K, D165V, and D168Y, respectively).  Grazoprevir inhibits the NS3/4A protease in an in vitro replicon system with EC50 values of 2 and 8 nM for genotypes 1a and 2a, respectively. Formulations containing grazoprevir are used in combination therapies to treat HCV.{36013}    

     

    Brand:
    Cayman
    SKU:21816 -

    Out of stock

  • Green CMFDA is a cell-permeable fluorescent probe that freely enters living cells, where it is transformed into a cell-impermeable, soluble, fluorescent compound. The resulting molecule does not affect cell viability or proliferation and stably fluoresces for at least 72 hours, allowing for its use in cell tracking.{31943} It is also transferred to daughter cells. Green CMFDA is brightly fluorescent with standard filters (ex/em max = 492/517 nm) and is often used with additional fluorescent dyes and proteins.{31944,26644}  

     

    Brand:
    Cayman
    SKU:19583 -

    Available on backorder

  • Green CMFDA is a cell-permeable fluorescent probe that freely enters living cells, where it is transformed into a cell-impermeable, soluble, fluorescent compound. The resulting molecule does not affect cell viability or proliferation and stably fluoresces for at least 72 hours, allowing for its use in cell tracking.{31943} It is also transferred to daughter cells. Green CMFDA is brightly fluorescent with standard filters (ex/em max = 492/517 nm) and is often used with additional fluorescent dyes and proteins.{31944,26644}  

     

    Brand:
    Cayman
    SKU:19583 -

    Available on backorder

  • Green CMFDA is a cell-permeable fluorescent probe that freely enters living cells, where it is transformed into a cell-impermeable, soluble, fluorescent compound. The resulting molecule does not affect cell viability or proliferation and stably fluoresces for at least 72 hours, allowing for its use in cell tracking.{31943} It is also transferred to daughter cells. Green CMFDA is brightly fluorescent with standard filters (ex/em max = 492/517 nm) and is often used with additional fluorescent dyes and proteins.{31944,26644}  

     

    Brand:
    Cayman
    SKU:19583 -

    Available on backorder

  • GRI-977143 is an agonist of G protein-coupled lysophosphatidic acid receptor 2 (LPA2) with an EC50 value of 3.3 μM in LPA2-transfected RH7777 cells.{40202} It is selective for LPA2, having no activity at LPA1, LPA3, LPA4, and LPA5 at concentrations up to 10 μM. GRI-977143 increases growth and reduces caspase-3 and -7 activation in LPA2-transduced MEF fibroblasts. It increases MM1 rat hepatoma cell invasion and inhibits apoptosis of IEC-6 cells induced by TNF-α, doxorubicin (Item No. 15007), or serum withdrawal. GRI-977143 also rescues apoptotic cells from γ-irradiation-induced injury in vitro and in vivo.{40203}  

     

    Brand:
    Cayman
    SKU:21900 -

    Out of stock

  • GRI-977143 is an agonist of G protein-coupled lysophosphatidic acid receptor 2 (LPA2) with an EC50 value of 3.3 μM in LPA2-transfected RH7777 cells.{40202} It is selective for LPA2, having no activity at LPA1, LPA3, LPA4, and LPA5 at concentrations up to 10 μM. GRI-977143 increases growth and reduces caspase-3 and -7 activation in LPA2-transduced MEF fibroblasts. It increases MM1 rat hepatoma cell invasion and inhibits apoptosis of IEC-6 cells induced by TNF-α, doxorubicin (Item No. 15007), or serum withdrawal. GRI-977143 also rescues apoptotic cells from γ-irradiation-induced injury in vitro and in vivo.{40203}  

     

    Brand:
    Cayman
    SKU:21900 -

    Out of stock

  • GRI-977143 is an agonist of G protein-coupled lysophosphatidic acid receptor 2 (LPA2) with an EC50 value of 3.3 μM in LPA2-transfected RH7777 cells.{40202} It is selective for LPA2, having no activity at LPA1, LPA3, LPA4, and LPA5 at concentrations up to 10 μM. GRI-977143 increases growth and reduces caspase-3 and -7 activation in LPA2-transduced MEF fibroblasts. It increases MM1 rat hepatoma cell invasion and inhibits apoptosis of IEC-6 cells induced by TNF-α, doxorubicin (Item No. 15007), or serum withdrawal. GRI-977143 also rescues apoptotic cells from γ-irradiation-induced injury in vitro and in vivo.{40203}  

     

    Brand:
    Cayman
    SKU:21900 -

    Out of stock

  • GRI-977143 is an agonist of G protein-coupled lysophosphatidic acid receptor 2 (LPA2) with an EC50 value of 3.3 μM in LPA2-transfected RH7777 cells.{40202} It is selective for LPA2, having no activity at LPA1, LPA3, LPA4, and LPA5 at concentrations up to 10 μM. GRI-977143 increases growth and reduces caspase-3 and -7 activation in LPA2-transduced MEF fibroblasts. It increases MM1 rat hepatoma cell invasion and inhibits apoptosis of IEC-6 cells induced by TNF-α, doxorubicin (Item No. 15007), or serum withdrawal. GRI-977143 also rescues apoptotic cells from γ-irradiation-induced injury in vitro and in vivo.{40203}  

     

    Brand:
    Cayman
    SKU:21900 -

    Out of stock

  • GPR120 (free fatty acid receptor 4/FFAR4) is a G protein-coupled receptor expressed in intestine, adipocytes, and pro-inflammatory macrophages that is activated by long-chain free fatty acids. It has been linked to the ability of fatty acids to produce anti-inflammatory effects and to acutely potentiate insulin secretion. Grifolic acid is a selective partial agonist of GPR120 that induces ERK activation and intracellular calcium responses in mouse enteroendocrine STC-1 cells that express GPR120 endogenously, but not those expressing GPR40.{31125}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • GPR120 (free fatty acid receptor 4/FFAR4) is a G protein-coupled receptor expressed in intestine, adipocytes, and pro-inflammatory macrophages that is activated by long-chain free fatty acids. It has been linked to the ability of fatty acids to produce anti-inflammatory effects and to acutely potentiate insulin secretion. Grifolic acid is a selective partial agonist of GPR120 that induces ERK activation and intracellular calcium responses in mouse enteroendocrine STC-1 cells that express GPR120 endogenously, but not those expressing GPR40.{31125}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Griseofulvin is a natural bacterial product used, in certain formulations, as an oral antibiotic for fungal infections of the skin.{31420} It alters microtubule dynamics, resulting in metaphase arrest.{31421} Antimicrotubule agents, including griseofulvin, have potential applications in cancer therapy, particularly when combined with other chemotherapeutic compounds.{31422,31419}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Griseofulvin is a natural bacterial product used, in certain formulations, as an oral antibiotic for fungal infections of the skin.{31420} It alters microtubule dynamics, resulting in metaphase arrest.{31421} Antimicrotubule agents, including griseofulvin, have potential applications in cancer therapy, particularly when combined with other chemotherapeutic compounds.{31422,31419}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Griseofulvin is a natural bacterial product used, in certain formulations, as an oral antibiotic for fungal infections of the skin.{31420} It alters microtubule dynamics, resulting in metaphase arrest.{31421} Antimicrotubule agents, including griseofulvin, have potential applications in cancer therapy, particularly when combined with other chemotherapeutic compounds.{31422,31419}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • GS-143 is an inhibitor of IκBα ubiquitylation.{45272} It inhibits ubiquitylation of phosphorylated IκBα mediated by the SCFβTrCP1 E3 ubiquitin ligase complex in vitro (IC50 = 5.2 μM) and reduces TNF-α-induced degradation of phosphorylated IκBα, but not β-catenin, another SCFβTrCP1 substrate, in HeLa S3 cells. GS-143 inhibits LPS-induced expression of TNF-α, IL-6, IL-12, ICAM-1, and NF-κB in THP-1 cells in a concentration-dependent manner. Intranasal administration of GS-143 (32 μg/animal) reduces the number of eosinophils, lymphocytes, and total cells in bronchoalveolar lavage fluid (BALF) in an ovalbumin-sensitized mouse model of allergic asthma.{45273}  

     

    Brand:
    Cayman
    SKU:26138 - 10 mg

    Available on backorder

  • GS-143 is an inhibitor of IκBα ubiquitylation.{45272} It inhibits ubiquitylation of phosphorylated IκBα mediated by the SCFβTrCP1 E3 ubiquitin ligase complex in vitro (IC50 = 5.2 μM) and reduces TNF-α-induced degradation of phosphorylated IκBα, but not β-catenin, another SCFβTrCP1 substrate, in HeLa S3 cells. GS-143 inhibits LPS-induced expression of TNF-α, IL-6, IL-12, ICAM-1, and NF-κB in THP-1 cells in a concentration-dependent manner. Intranasal administration of GS-143 (32 μg/animal) reduces the number of eosinophils, lymphocytes, and total cells in bronchoalveolar lavage fluid (BALF) in an ovalbumin-sensitized mouse model of allergic asthma.{45273}  

     

    Brand:
    Cayman
    SKU:26138 - 25 mg

    Available on backorder

  • GS-143 is an inhibitor of IκBα ubiquitylation.{45272} It inhibits ubiquitylation of phosphorylated IκBα mediated by the SCFβTrCP1 E3 ubiquitin ligase complex in vitro (IC50 = 5.2 μM) and reduces TNF-α-induced degradation of phosphorylated IκBα, but not β-catenin, another SCFβTrCP1 substrate, in HeLa S3 cells. GS-143 inhibits LPS-induced expression of TNF-α, IL-6, IL-12, ICAM-1, and NF-κB in THP-1 cells in a concentration-dependent manner. Intranasal administration of GS-143 (32 μg/animal) reduces the number of eosinophils, lymphocytes, and total cells in bronchoalveolar lavage fluid (BALF) in an ovalbumin-sensitized mouse model of allergic asthma.{45273}  

     

    Brand:
    Cayman
    SKU:26138 - 5 mg

    Available on backorder

  • GS-143 is an inhibitor of IκBα ubiquitylation.{45272} It inhibits ubiquitylation of phosphorylated IκBα mediated by the SCFβTrCP1 E3 ubiquitin ligase complex in vitro (IC50 = 5.2 μM) and reduces TNF-α-induced degradation of phosphorylated IκBα, but not β-catenin, another SCFβTrCP1 substrate, in HeLa S3 cells. GS-143 inhibits LPS-induced expression of TNF-α, IL-6, IL-12, ICAM-1, and NF-κB in THP-1 cells in a concentration-dependent manner. Intranasal administration of GS-143 (32 μg/animal) reduces the number of eosinophils, lymphocytes, and total cells in bronchoalveolar lavage fluid (BALF) in an ovalbumin-sensitized mouse model of allergic asthma.{45273}  

     

    Brand:
    Cayman
    SKU:26138 - 50 mg

    Available on backorder

  • GS-39783 is a positive allosteric modulator of GABAB receptors that potentiates GABA-stimulated [35S]GTPγS binding to recombinant human GABAB receptors and rat cortical membranes (EC50s = 2.1 and 3.1 μM, respectively).{53122} It amplifies GABAB receptor-mediated transient calcium signaling in HEK293 cells expressing human receptors (EC50 = 2.4 μM). GS-39783 (25-100 mg/kg) suppresses alcohol self-administration, but has no effect on lever-responding for food, in Indiana alcohol-preferring, Sardinian alcohol-preferring, and Alko Alcohol rats.{53123} It reduces amphetamine- or MK-801-induced hyperactivity in rats and the number of DOI-induced head twitches in mice, indicating antipsychotic-like activity.{53124} GS-39783 also reduces the incidence of sound-induced tonic convulsions in juvenile mice (ED50 = 55.38 mg/kg).{53125}  

     

    Brand:
    Cayman
    SKU:29482 - 10 mg

    Available on backorder

  • GS-39783 is a positive allosteric modulator of GABAB receptors that potentiates GABA-stimulated [35S]GTPγS binding to recombinant human GABAB receptors and rat cortical membranes (EC50s = 2.1 and 3.1 μM, respectively).{53122} It amplifies GABAB receptor-mediated transient calcium signaling in HEK293 cells expressing human receptors (EC50 = 2.4 μM). GS-39783 (25-100 mg/kg) suppresses alcohol self-administration, but has no effect on lever-responding for food, in Indiana alcohol-preferring, Sardinian alcohol-preferring, and Alko Alcohol rats.{53123} It reduces amphetamine- or MK-801-induced hyperactivity in rats and the number of DOI-induced head twitches in mice, indicating antipsychotic-like activity.{53124} GS-39783 also reduces the incidence of sound-induced tonic convulsions in juvenile mice (ED50 = 55.38 mg/kg).{53125}  

     

    Brand:
    Cayman
    SKU:29482 - 25 mg

    Available on backorder

  • GS-39783 is a positive allosteric modulator of GABAB receptors that potentiates GABA-stimulated [35S]GTPγS binding to recombinant human GABAB receptors and rat cortical membranes (EC50s = 2.1 and 3.1 μM, respectively).{53122} It amplifies GABAB receptor-mediated transient calcium signaling in HEK293 cells expressing human receptors (EC50 = 2.4 μM). GS-39783 (25-100 mg/kg) suppresses alcohol self-administration, but has no effect on lever-responding for food, in Indiana alcohol-preferring, Sardinian alcohol-preferring, and Alko Alcohol rats.{53123} It reduces amphetamine- or MK-801-induced hyperactivity in rats and the number of DOI-induced head twitches in mice, indicating antipsychotic-like activity.{53124} GS-39783 also reduces the incidence of sound-induced tonic convulsions in juvenile mice (ED50 = 55.38 mg/kg).{53125}  

     

    Brand:
    Cayman
    SKU:29482 - 5 mg

    Available on backorder

  • GS-39783 is a positive allosteric modulator of GABAB receptors that potentiates GABA-stimulated [35S]GTPγS binding to recombinant human GABAB receptors and rat cortical membranes (EC50s = 2.1 and 3.1 μM, respectively).{53122} It amplifies GABAB receptor-mediated transient calcium signaling in HEK293 cells expressing human receptors (EC50 = 2.4 μM). GS-39783 (25-100 mg/kg) suppresses alcohol self-administration, but has no effect on lever-responding for food, in Indiana alcohol-preferring, Sardinian alcohol-preferring, and Alko Alcohol rats.{53123} It reduces amphetamine- or MK-801-induced hyperactivity in rats and the number of DOI-induced head twitches in mice, indicating antipsychotic-like activity.{53124} GS-39783 also reduces the incidence of sound-induced tonic convulsions in juvenile mice (ED50 = 55.38 mg/kg).{53125}  

     

    Brand:
    Cayman
    SKU:29482 - 50 mg

    Available on backorder

  • GS-441524 is an antiviral nucleoside analog and a metabolite of remdesivir (Item No. 30354).{45842} Upon entry into cells, GS-441524 is metabolized to an active triphosphate form that induces RNA chain termination and inhibits viral polymerases. It is active against Middle East respiratory syndrome coronavirus (MERS-CoV) and severe acute respiratory syndrome CoV (SARS-CoV) in infected primary human airway epithelial (HAE) cells (EC50s = 0.86 and 0.18 µM, respectively). GS-441524 reduces viral plaque formation in SARS-CoV-2-infected Vero E6 and Calu-3 2B4 cells (EC50s = 0.42 and 0.62 mM, respectively).{61140} It is cytoprotective against hepatitis C virus (HCV), yellow fever virus (YFV), dengue virus type 2 (DENV-2), influenza A, and parainfluenza 3 in cell-based assays (EC50s = 4.1, 11, 9.46, 27.9, and 1.71 µM, respectively).{53439}  

     

    Brand:
    Cayman
    SKU:30469 - 1 mg

    Available on backorder

  • GS-441524 is an antiviral nucleoside analog and a metabolite of remdesivir (Item No. 30354).{45842} Upon entry into cells, GS-441524 is metabolized to an active triphosphate form that induces RNA chain termination and inhibits viral polymerases. It is active against Middle East respiratory syndrome coronavirus (MERS-CoV) and severe acute respiratory syndrome CoV (SARS-CoV) in infected primary human airway epithelial (HAE) cells (EC50s = 0.86 and 0.18 µM, respectively). GS-441524 reduces viral plaque formation in SARS-CoV-2-infected Vero E6 and Calu-3 2B4 cells (EC50s = 0.42 and 0.62 mM, respectively).{61140} It is cytoprotective against hepatitis C virus (HCV), yellow fever virus (YFV), dengue virus type 2 (DENV-2), influenza A, and parainfluenza 3 in cell-based assays (EC50s = 4.1, 11, 9.46, 27.9, and 1.71 µM, respectively).{53439}  

     

    Brand:
    Cayman
    SKU:30469 - 10 mg

    Available on backorder

  • GS-441524 is an antiviral nucleoside analog and a metabolite of remdesivir (Item No. 30354).{45842} Upon entry into cells, GS-441524 is metabolized to an active triphosphate form that induces RNA chain termination and inhibits viral polymerases. It is active against Middle East respiratory syndrome coronavirus (MERS-CoV) and severe acute respiratory syndrome CoV (SARS-CoV) in infected primary human airway epithelial (HAE) cells (EC50s = 0.86 and 0.18 µM, respectively). GS-441524 reduces viral plaque formation in SARS-CoV-2-infected Vero E6 and Calu-3 2B4 cells (EC50s = 0.42 and 0.62 mM, respectively).{61140} It is cytoprotective against hepatitis C virus (HCV), yellow fever virus (YFV), dengue virus type 2 (DENV-2), influenza A, and parainfluenza 3 in cell-based assays (EC50s = 4.1, 11, 9.46, 27.9, and 1.71 µM, respectively).{53439}  

     

    Brand:
    Cayman
    SKU:30469 - 25 mg

    Available on backorder

  • GS-441524 is an antiviral nucleoside analog and a metabolite of remdesivir (Item No. 30354).{45842} Upon entry into cells, GS-441524 is metabolized to an active triphosphate form that induces RNA chain termination and inhibits viral polymerases. It is active against Middle East respiratory syndrome coronavirus (MERS-CoV) and severe acute respiratory syndrome CoV (SARS-CoV) in infected primary human airway epithelial (HAE) cells (EC50s = 0.86 and 0.18 µM, respectively). GS-441524 reduces viral plaque formation in SARS-CoV-2-infected Vero E6 and Calu-3 2B4 cells (EC50s = 0.42 and 0.62 mM, respectively).{61140} It is cytoprotective against hepatitis C virus (HCV), yellow fever virus (YFV), dengue virus type 2 (DENV-2), influenza A, and parainfluenza 3 in cell-based assays (EC50s = 4.1, 11, 9.46, 27.9, and 1.71 µM, respectively).{53439}  

     

    Brand:
    Cayman
    SKU:30469 - 5 mg

    Available on backorder

  • GS-441524 isopropyl ester is a derivative of the antiviral prodrug remdesivir (Item No. 30354).  

     

    Brand:
    Cayman
    SKU:9003635 - 1 mg

    Available on backorder

  • GS-441524 isopropyl ester is a derivative of the antiviral prodrug remdesivir (Item No. 30354).  

     

    Brand:
    Cayman
    SKU:9003635 - 5 mg

    Available on backorder

  • GS-704277 is an intermediate alanine metabolite of the antiviral prodrug remdesivir (Item No. 30354).{52858,52859} It is formed from remdesivir via intracellular hydrolysis. GS-704277 is further metabolized to the nucleoside monophosphate form and then to the nucleoside analog GS-441524 (Item No. 30469) or active nucleoside triphosphate GS-443902.  

     

    Brand:
    Cayman
    SKU:9003569 - 1 mg

    Available on backorder

  • GS-704277 is an intermediate alanine metabolite of the antiviral prodrug remdesivir (Item No. 30354).{52858,52859} It is formed from remdesivir via intracellular hydrolysis. GS-704277 is further metabolized to the nucleoside monophosphate form and then to the nucleoside analog GS-441524 (Item No. 30469) or active nucleoside triphosphate GS-443902.  

     

    Brand:
    Cayman
    SKU:9003569 - 500 µg

    Available on backorder

  • GS-7340 is a prodrug form of the antiviral adenosine analog tenofovir (Item No. 13874).{42639} It reduces HIV-1 viral replication in MT-2 cells with an EC50 value of 5 nM.  

     

    Brand:
    Cayman
    SKU:26214 - 10 mg

    Available on backorder

  • GS-7340 is a prodrug form of the antiviral adenosine analog tenofovir (Item No. 13874).{42639} It reduces HIV-1 viral replication in MT-2 cells with an EC50 value of 5 nM.  

     

    Brand:
    Cayman
    SKU:26214 - 100 mg

    Available on backorder

  • GS-7340 is a prodrug form of the antiviral adenosine analog tenofovir (Item No. 13874).{42639} It reduces HIV-1 viral replication in MT-2 cells with an EC50 value of 5 nM.  

     

    Brand:
    Cayman
    SKU:26214 - 5 mg

    Available on backorder

  • GS-7340 is a prodrug form of the antiviral adenosine analog tenofovir (Item No. 13874).{42639} It reduces HIV-1 viral replication in MT-2 cells with an EC50 value of 5 nM.  

     

    Brand:
    Cayman
    SKU:26214 - 50 mg

    Available on backorder

  • GS-9620 is an orally available agonist of toll-like receptor 7 (TLR7; EC50 = 291 nM) with 30-fold selectivity over TLR8 (EC50 = 9 µM).{32637} It has been shown to stimulate a TLR7 immune response in two different animal models of chronic hepatitis B infection and to inhibit HIV-1 infection in human peripheral blood mononuclear cells.{32636,32635,32634}  

     

    Brand:
    Cayman
    SKU:19628 -

    Available on backorder

  • GS-9620 is an orally available agonist of toll-like receptor 7 (TLR7; EC50 = 291 nM) with 30-fold selectivity over TLR8 (EC50 = 9 µM).{32637} It has been shown to stimulate a TLR7 immune response in two different animal models of chronic hepatitis B infection and to inhibit HIV-1 infection in human peripheral blood mononuclear cells.{32636,32635,32634}  

     

    Brand:
    Cayman
    SKU:19628 -

    Available on backorder

  • GS-9620 is an orally available agonist of toll-like receptor 7 (TLR7; EC50 = 291 nM) with 30-fold selectivity over TLR8 (EC50 = 9 µM).{32637} It has been shown to stimulate a TLR7 immune response in two different animal models of chronic hepatitis B infection and to inhibit HIV-1 infection in human peripheral blood mononuclear cells.{32636,32635,32634}  

     

    Brand:
    Cayman
    SKU:19628 -

    Available on backorder

  • GS-9620 is an orally available agonist of toll-like receptor 7 (TLR7; EC50 = 291 nM) with 30-fold selectivity over TLR8 (EC50 = 9 µM).{32637} It has been shown to stimulate a TLR7 immune response in two different animal models of chronic hepatitis B infection and to inhibit HIV-1 infection in human peripheral blood mononuclear cells.{32636,32635,32634}  

     

    Brand:
    Cayman
    SKU:19628 -

    Available on backorder

  • Spleen tyrosine kinase (Syk) is a non-receptor tyrosine kinase that upon phosphorylation binds to immunoreceptor tyrosine-based activation motifs of FcRγ chains and mediates downstream signaling related to platelet function and inflammation.{24052} GS-9973 is a potent Syk inhibitor (IC50 = 7.7 nM) that demonstrates 10-35-fold selectivity for Syk over a panel of 359 nonmutant kinases.{28699} In conjunction with the PI3Kδ inhibitor CAL-101 (Item No. 15279), it has been used to reduce chronic lymphocytic leukemia cell survival and to disrupt chemokine signaling at nanomolar concentrations.{28700}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Spleen tyrosine kinase (Syk) is a non-receptor tyrosine kinase that upon phosphorylation binds to immunoreceptor tyrosine-based activation motifs of FcRγ chains and mediates downstream signaling related to platelet function and inflammation.{24052} GS-9973 is a potent Syk inhibitor (IC50 = 7.7 nM) that demonstrates 10-35-fold selectivity for Syk over a panel of 359 nonmutant kinases.{28699} In conjunction with the PI3Kδ inhibitor CAL-101 (Item No. 15279), it has been used to reduce chronic lymphocytic leukemia cell survival and to disrupt chemokine signaling at nanomolar concentrations.{28700}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Spleen tyrosine kinase (Syk) is a non-receptor tyrosine kinase that upon phosphorylation binds to immunoreceptor tyrosine-based activation motifs of FcRγ chains and mediates downstream signaling related to platelet function and inflammation.{24052} GS-9973 is a potent Syk inhibitor (IC50 = 7.7 nM) that demonstrates 10-35-fold selectivity for Syk over a panel of 359 nonmutant kinases.{28699} In conjunction with the PI3Kδ inhibitor CAL-101 (Item No. 15279), it has been used to reduce chronic lymphocytic leukemia cell survival and to disrupt chemokine signaling at nanomolar concentrations.{28700}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Spleen tyrosine kinase (Syk) is a non-receptor tyrosine kinase that upon phosphorylation binds to immunoreceptor tyrosine-based activation motifs of FcRγ chains and mediates downstream signaling related to platelet function and inflammation.{24052} GS-9973 is a potent Syk inhibitor (IC50 = 7.7 nM) that demonstrates 10-35-fold selectivity for Syk over a panel of 359 nonmutant kinases.{28699} In conjunction with the PI3Kδ inhibitor CAL-101 (Item No. 15279), it has been used to reduce chronic lymphocytic leukemia cell survival and to disrupt chemokine signaling at nanomolar concentrations.{28700}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Inhibition of cardiac late sodium current (late INa) is a strategy to suppress arrhythmias and sodium-dependent calcium overload associated with myocardial ischemia and heart failure. GS967 is a selective inhibitor of late INa that has been shown to suppress experimentally induced arrhythmias in rabbit myocytes and hearts.{30900} It can inhibit A. sulcata toxin II–induced late INa in ventricular myocytes and isolated hearts with IC50 values of 0.13 and 0.21 µM, respectively.{30900} GS967 causes minimal inhibition of the delayed-rectifier potassium current nor does it affect L- or T-type calcium channel currents, sodium-calcium exchanger currents, or a panel of 162 receptors, ion channels, transporters, and enzymes.{30900}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Inhibition of cardiac late sodium current (late INa) is a strategy to suppress arrhythmias and sodium-dependent calcium overload associated with myocardial ischemia and heart failure. GS967 is a selective inhibitor of late INa that has been shown to suppress experimentally induced arrhythmias in rabbit myocytes and hearts.{30900} It can inhibit A. sulcata toxin II–induced late INa in ventricular myocytes and isolated hearts with IC50 values of 0.13 and 0.21 µM, respectively.{30900} GS967 causes minimal inhibition of the delayed-rectifier potassium current nor does it affect L- or T-type calcium channel currents, sodium-calcium exchanger currents, or a panel of 162 receptors, ion channels, transporters, and enzymes.{30900}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Inhibition of cardiac late sodium current (late INa) is a strategy to suppress arrhythmias and sodium-dependent calcium overload associated with myocardial ischemia and heart failure. GS967 is a selective inhibitor of late INa that has been shown to suppress experimentally induced arrhythmias in rabbit myocytes and hearts.{30900} It can inhibit A. sulcata toxin II–induced late INa in ventricular myocytes and isolated hearts with IC50 values of 0.13 and 0.21 µM, respectively.{30900} GS967 causes minimal inhibition of the delayed-rectifier potassium current nor does it affect L- or T-type calcium channel currents, sodium-calcium exchanger currents, or a panel of 162 receptors, ion channels, transporters, and enzymes.{30900}  

     

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    Cayman
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  • Smoothened (SMO) is a cell surface receptor that, with Patched, mediates hedgehog signaling to regulate gene expression through the Gli transcription factors.{21774} GSA 10 is a quinolinecarboxamide derivative that acts as an agonist of SMO.{26551} By acting at SMO, GSA 10 has been shown to promote the differentiation of multipotent mesenchymal progenitor cells into osteoblasts (EC50 = 1.2 µM).{26551} Most notably, GSA 10 does not recognize the classic cyclopamine binding site as do other SMO agonists and as such has been used to characterize a novel SMO active site.{26551}  

     

    Brand:
    Cayman
    SKU:-
  • Smoothened (SMO) is a cell surface receptor that, with Patched, mediates hedgehog signaling to regulate gene expression through the Gli transcription factors.{21774} GSA 10 is a quinolinecarboxamide derivative that acts as an agonist of SMO.{26551} By acting at SMO, GSA 10 has been shown to promote the differentiation of multipotent mesenchymal progenitor cells into osteoblasts (EC50 = 1.2 µM).{26551} Most notably, GSA 10 does not recognize the classic cyclopamine binding site as do other SMO agonists and as such has been used to characterize a novel SMO active site.{26551}  

     

    Brand:
    Cayman
    SKU:-
  • Smoothened (SMO) is a cell surface receptor that, with Patched, mediates hedgehog signaling to regulate gene expression through the Gli transcription factors.{21774} GSA 10 is a quinolinecarboxamide derivative that acts as an agonist of SMO.{26551} By acting at SMO, GSA 10 has been shown to promote the differentiation of multipotent mesenchymal progenitor cells into osteoblasts (EC50 = 1.2 µM).{26551} Most notably, GSA 10 does not recognize the classic cyclopamine binding site as do other SMO agonists and as such has been used to characterize a novel SMO active site.{26551}  

     

    Brand:
    Cayman
    SKU:-
  • Smoothened (SMO) is a cell surface receptor that, with Patched, mediates hedgehog signaling to regulate gene expression through the Gli transcription factors.{21774} GSA 10 is a quinolinecarboxamide derivative that acts as an agonist of SMO.{26551} By acting at SMO, GSA 10 has been shown to promote the differentiation of multipotent mesenchymal progenitor cells into osteoblasts (EC50 = 1.2 µM).{26551} Most notably, GSA 10 does not recognize the classic cyclopamine binding site as do other SMO agonists and as such has been used to characterize a novel SMO active site.{26551}  

     

    Brand:
    Cayman
    SKU:-
  • The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer.{19496,19494} GSK-J1 is a potent inhibitor of the H3K27 histone demethylases JMJD3 and UTX (IC50s = 18 and 56 µM, respectively as measured by mass spectrometry; IC50 = 60 nM in JMJD3 antibody-based assays).{21388} It is inactive against a panel of additional JMJ family demethylases, including several variants of JMJD2 and JMJD1 and, at concentrations up to 30 μM, has no effect on more than 100 different kinases or other unrelated proteins, including other chromatin-modifying enzymes such as histone deacetylases.{21388} Since the highly polar carboxylate group of GSK-J1 restricts its cellular permeability, a prodrug ethyl ester, GSK-J4 (Item No. 12073) has also been developed. See the Structural Genomics Consortium (SGC) website for more information.  

     

    Brand:
    Cayman
    SKU:12054 - 1 mg

    Available on backorder

  • The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer.{19496,19494} GSK-J1 is a potent inhibitor of the H3K27 histone demethylases JMJD3 and UTX (IC50s = 18 and 56 µM, respectively as measured by mass spectrometry; IC50 = 60 nM in JMJD3 antibody-based assays).{21388} It is inactive against a panel of additional JMJ family demethylases, including several variants of JMJD2 and JMJD1 and, at concentrations up to 30 μM, has no effect on more than 100 different kinases or other unrelated proteins, including other chromatin-modifying enzymes such as histone deacetylases.{21388} Since the highly polar carboxylate group of GSK-J1 restricts its cellular permeability, a prodrug ethyl ester, GSK-J4 (Item No. 12073) has also been developed. See the Structural Genomics Consortium (SGC) website for more information.  

     

    Brand:
    Cayman
    SKU:12054 - 10 mg

    Available on backorder

  • The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer.{19496,19494} GSK-J1 is a potent inhibitor of the H3K27 histone demethylases JMJD3 and UTX (IC50s = 18 and 56 µM, respectively as measured by mass spectrometry; IC50 = 60 nM in JMJD3 antibody-based assays).{21388} It is inactive against a panel of additional JMJ family demethylases, including several variants of JMJD2 and JMJD1 and, at concentrations up to 30 μM, has no effect on more than 100 different kinases or other unrelated proteins, including other chromatin-modifying enzymes such as histone deacetylases.{21388} Since the highly polar carboxylate group of GSK-J1 restricts its cellular permeability, a prodrug ethyl ester, GSK-J4 (Item No. 12073) has also been developed. See the Structural Genomics Consortium (SGC) website for more information.  

     

    Brand:
    Cayman
    SKU:12054 - 5 mg

    Available on backorder

  • The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer.{19496,19494} GSK-J1 is a potent inhibitor of the H3K27 histone demethylases JMJD3 and UTX (IC50s = 18 and 56 µM, respectively as measured by mass spectrometry; IC50 = 60 nM in JMJD3 antibody-based assays).{21388} It is inactive against a panel of additional JMJ family demethylases, including several variants of JMJD2 and JMJD1 and, at concentrations up to 30 μM, has no effect on more than 100 different kinases or other unrelated proteins, including other chromatin-modifying enzymes such as histone deacetylases.{21388} Since the highly polar carboxylate group of GSK-J1 restricts its cellular permeability, a prodrug ethyl ester, GSK-J4 (Item No. 12073) has also been developed. See the Structural Genomics Consortium (SGC) website for more information.  

     

    Brand:
    Cayman
    SKU:12054 - 50 mg

    Available on backorder

  • The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer.{19496,19494} GSK-J2 is a pyridine regio-isomer of GSK-J1 which poorly inhibits JMJD3 (IC50 > 100 μM), making it an appropriate negative control for in vitro studies involving GSK-J1.{21388} For in vivo research, cell-permeable prodrug forms of GSK-J1 and GSK-J2 are available as GSK-J4 (Item No. 12073) and GSK-J5 (Item No. 12074), respectively. See the Structural Genomics Consortium (SGC) website for more information.  

     

    Brand:
    Cayman
    SKU:12056 - 1 mg

    Available on backorder

  • The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer.{19496,19494} GSK-J2 is a pyridine regio-isomer of GSK-J1 which poorly inhibits JMJD3 (IC50 > 100 μM), making it an appropriate negative control for in vitro studies involving GSK-J1.{21388} For in vivo research, cell-permeable prodrug forms of GSK-J1 and GSK-J2 are available as GSK-J4 (Item No. 12073) and GSK-J5 (Item No. 12074), respectively. See the Structural Genomics Consortium (SGC) website for more information.  

     

    Brand:
    Cayman
    SKU:12056 - 10 mg

    Available on backorder

  • The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer.{19496,19494} GSK-J2 is a pyridine regio-isomer of GSK-J1 which poorly inhibits JMJD3 (IC50 > 100 μM), making it an appropriate negative control for in vitro studies involving GSK-J1.{21388} For in vivo research, cell-permeable prodrug forms of GSK-J1 and GSK-J2 are available as GSK-J4 (Item No. 12073) and GSK-J5 (Item No. 12074), respectively. See the Structural Genomics Consortium (SGC) website for more information.  

     

    Brand:
    Cayman
    SKU:12056 - 5 mg

    Available on backorder

  • The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer.{19496,19494} GSK-J2 is a pyridine regio-isomer of GSK-J1 which poorly inhibits JMJD3 (IC50 > 100 μM), making it an appropriate negative control for in vitro studies involving GSK-J1.{21388} For in vivo research, cell-permeable prodrug forms of GSK-J1 and GSK-J2 are available as GSK-J4 (Item No. 12073) and GSK-J5 (Item No. 12074), respectively. See the Structural Genomics Consortium (SGC) website for more information.  

     

    Brand:
    Cayman
    SKU:12056 - 50 mg

    Available on backorder

  • The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer.{19496,19494} GSK-J4 (hydrochloride) is an ethyl ester derivative of the JMJD3 selective histone demethylase inhibitor GSK-J1 (Item No. 12054) with an IC50 value greater than 50 μM in vitro.{21388} Acting as a prodrug, GSK-J4 is rapidly hydrolyzed in cells to the otherwise cell impermeable GSK-J1, which exhibits an IC50 value of 60 nM for the purified enzyme. When administered to human primary macrophages, GSK-J4 can reduce LPS-induced proinflammatory cytokine production, most notably including that of TNFα (IC50 = 9 µM).{21388}  

     

    Brand:
    Cayman
    SKU:12073 - 1 mg

    Available on backorder

  • The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer.{19496,19494} GSK-J4 (hydrochloride) is an ethyl ester derivative of the JMJD3 selective histone demethylase inhibitor GSK-J1 (Item No. 12054) with an IC50 value greater than 50 μM in vitro.{21388} Acting as a prodrug, GSK-J4 is rapidly hydrolyzed in cells to the otherwise cell impermeable GSK-J1, which exhibits an IC50 value of 60 nM for the purified enzyme. When administered to human primary macrophages, GSK-J4 can reduce LPS-induced proinflammatory cytokine production, most notably including that of TNFα (IC50 = 9 µM).{21388}  

     

    Brand:
    Cayman
    SKU:12073 - 10 mg

    Available on backorder

  • The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer.{19496,19494} GSK-J4 (hydrochloride) is an ethyl ester derivative of the JMJD3 selective histone demethylase inhibitor GSK-J1 (Item No. 12054) with an IC50 value greater than 50 μM in vitro.{21388} Acting as a prodrug, GSK-J4 is rapidly hydrolyzed in cells to the otherwise cell impermeable GSK-J1, which exhibits an IC50 value of 60 nM for the purified enzyme. When administered to human primary macrophages, GSK-J4 can reduce LPS-induced proinflammatory cytokine production, most notably including that of TNFα (IC50 = 9 µM).{21388}  

     

    Brand:
    Cayman
    SKU:12073 - 5 mg

    Available on backorder

  • The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer.{19496,19494} GSK-J4 (hydrochloride) is an ethyl ester derivative of the JMJD3 selective histone demethylase inhibitor GSK-J1 (Item No. 12054) with an IC50 value greater than 50 μM in vitro.{21388} Acting as a prodrug, GSK-J4 is rapidly hydrolyzed in cells to the otherwise cell impermeable GSK-J1, which exhibits an IC50 value of 60 nM for the purified enzyme. When administered to human primary macrophages, GSK-J4 can reduce LPS-induced proinflammatory cytokine production, most notably including that of TNFα (IC50 = 9 µM).{21388}  

     

    Brand:
    Cayman
    SKU:12073 - 50 mg

    Available on backorder

  • The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer.{19496,19494} GSK-J4 (Item No. 12073) is a cell-permeable prodrug which is modified by intracellular esterases to give GSK-J1 (Item No. 12054), an inhibitor of JMJD3. GSK-J5 is a pyridine regio-isomer of GSK-J4. Like GSK-J4, this isomer is cell-permeable and hydrolyzed to a free base.{21388} However, the free base is a weak inhibitor of JMJD3 (IC50 > 100 μM), making it an ideal inactive control molecule for elucidating the functional role of JMJD3 inhibition.{21388}  

     

    Brand:
    Cayman
    SKU:12074 - 1 mg

    Available on backorder

  • The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer.{19496,19494} GSK-J4 (Item No. 12073) is a cell-permeable prodrug which is modified by intracellular esterases to give GSK-J1 (Item No. 12054), an inhibitor of JMJD3. GSK-J5 is a pyridine regio-isomer of GSK-J4. Like GSK-J4, this isomer is cell-permeable and hydrolyzed to a free base.{21388} However, the free base is a weak inhibitor of JMJD3 (IC50 > 100 μM), making it an ideal inactive control molecule for elucidating the functional role of JMJD3 inhibition.{21388}  

     

    Brand:
    Cayman
    SKU:12074 - 10 mg

    Available on backorder

  • The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer.{19496,19494} GSK-J4 (Item No. 12073) is a cell-permeable prodrug which is modified by intracellular esterases to give GSK-J1 (Item No. 12054), an inhibitor of JMJD3. GSK-J5 is a pyridine regio-isomer of GSK-J4. Like GSK-J4, this isomer is cell-permeable and hydrolyzed to a free base.{21388} However, the free base is a weak inhibitor of JMJD3 (IC50 > 100 μM), making it an ideal inactive control molecule for elucidating the functional role of JMJD3 inhibition.{21388}  

     

    Brand:
    Cayman
    SKU:12074 - 5 mg

    Available on backorder

  • The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer.{19496,19494} GSK-J4 (Item No. 12073) is a cell-permeable prodrug which is modified by intracellular esterases to give GSK-J1 (Item No. 12054), an inhibitor of JMJD3. GSK-J5 is a pyridine regio-isomer of GSK-J4. Like GSK-J4, this isomer is cell-permeable and hydrolyzed to a free base.{21388} However, the free base is a weak inhibitor of JMJD3 (IC50 > 100 μM), making it an ideal inactive control molecule for elucidating the functional role of JMJD3 inhibition.{21388}  

     

    Brand:
    Cayman
    SKU:12074 - 50 mg

    Available on backorder

  • Lysine-specific demethylase 1 (LSD1) belongs to the family of flavin adenine dinucleotide (FAD)-dependent amine oxidases that include monoamine oxidases (MAOs) and polyamine oxidase (PAO).{12422} LSD1 specifically demethylates mono- and dimethylated histone H3 lysine 4, resulting in transcriptional repression.{14724} It also controls the tumor suppressor activity of p53 by demethylating a specific p53 lysine residue (LYS370).{15022} GSK-LSD1 is an irreversible, mechanism-based inhibitor of LSD1 (IC50 = 16 nM) that is >1,000-fold selective over the closely related FAD-utilizing enzymes LSD2, MAO-A, and MAO-B.{27091} GSK-LSD1 induces gene expression changes in various cancer cell lines, inhibiting their proliferation (EC50s Structural Genomics Consortium (SGC) website for more information.  

     

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    Cayman
    SKU:-

    Out of stock

  • Lysine-specific demethylase 1 (LSD1) belongs to the family of flavin adenine dinucleotide (FAD)-dependent amine oxidases that include monoamine oxidases (MAOs) and polyamine oxidase (PAO).{12422} LSD1 specifically demethylates mono- and dimethylated histone H3 lysine 4, resulting in transcriptional repression.{14724} It also controls the tumor suppressor activity of p53 by demethylating a specific p53 lysine residue (LYS370).{15022} GSK-LSD1 is an irreversible, mechanism-based inhibitor of LSD1 (IC50 = 16 nM) that is >1,000-fold selective over the closely related FAD-utilizing enzymes LSD2, MAO-A, and MAO-B.{27091} GSK-LSD1 induces gene expression changes in various cancer cell lines, inhibiting their proliferation (EC50s Structural Genomics Consortium (SGC) website for more information.  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • Lysine-specific demethylase 1 (LSD1) belongs to the family of flavin adenine dinucleotide (FAD)-dependent amine oxidases that include monoamine oxidases (MAOs) and polyamine oxidase (PAO).{12422} LSD1 specifically demethylates mono- and dimethylated histone H3 lysine 4, resulting in transcriptional repression.{14724} It also controls the tumor suppressor activity of p53 by demethylating a specific p53 lysine residue (LYS370).{15022} GSK-LSD1 is an irreversible, mechanism-based inhibitor of LSD1 (IC50 = 16 nM) that is >1,000-fold selective over the closely related FAD-utilizing enzymes LSD2, MAO-A, and MAO-B.{27091} GSK-LSD1 induces gene expression changes in various cancer cell lines, inhibiting their proliferation (EC50s Structural Genomics Consortium (SGC) website for more information.  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • Lysine-specific demethylase 1 (LSD1) belongs to the family of flavin adenine dinucleotide (FAD)-dependent amine oxidases that include monoamine oxidases (MAOs) and polyamine oxidase (PAO).{12422} LSD1 specifically demethylates mono- and dimethylated histone H3 lysine 4, resulting in transcriptional repression.{14724} It also controls the tumor suppressor activity of p53 by demethylating a specific p53 lysine residue (LYS370).{15022} GSK-LSD1 is an irreversible, mechanism-based inhibitor of LSD1 (IC50 = 16 nM) that is >1,000-fold selective over the closely related FAD-utilizing enzymes LSD2, MAO-A, and MAO-B.{27091} GSK-LSD1 induces gene expression changes in various cancer cell lines, inhibiting their proliferation (EC50s Structural Genomics Consortium (SGC) website for more information.  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • GSK0660 is the first reported antagonist of PPARβ/δ (IC50 = 155 nM) with no measurable affinity for PPARα or PPARγ (IC50s ≥ 10 μM).{32576} Because of the limited bioavailability of GSK0660, the related compound GSK3787 (Item No. 15219) was developed as a selective PPARβ/δ antagonist with more suitable pharmacokinetic properties.{24665}  

     

    Brand:
    Cayman
    SKU:-