Chemicals

Showing 21451–21600 of 41137 results

  • Guanosine is a purine nucleoside that is comprised of the purine base guanine attached to a ribose moiety.{46175} Mono-, di-, tri-, and cyclic monophosphorylated forms of guanosine (GMP, GDP, GTP, and cGMP, respectively) are essential for a variety of endogenous biochemical processes, such as signal transduction, metabolism, and RNA synthesis.{26065,1257,26064}  

     

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    Cayman
    SKU:27702 - 25 g

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  • Guanosine is a purine nucleoside that is comprised of the purine base guanine attached to a ribose moiety.{46175} Mono-, di-, tri-, and cyclic monophosphorylated forms of guanosine (GMP, GDP, GTP, and cGMP, respectively) are essential for a variety of endogenous biochemical processes, such as signal transduction, metabolism, and RNA synthesis.{26065,1257,26064}  

     

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    Cayman
    SKU:27702 - 5 g

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  • Guanosine 5′-triphosphate (GTP) acts as a substrate for the synthesis of RNA during the transcription process and the synthesis of DNA during DNA replication.{26064} It is generated by the citric acid cycle and provides a source of energy for protein synthesis and gluconeogenesis, activating substrates in metabolic reactions.{26065} GTP is essential for G protein-related signal transduction in second-messenger mechanisms where it is converted to GDP through the action of GTPases.{1257}  

     

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  • Guanosine 5′-triphosphate (GTP) acts as a substrate for the synthesis of RNA during the transcription process and the synthesis of DNA during DNA replication.{26064} It is generated by the citric acid cycle and provides a source of energy for protein synthesis and gluconeogenesis, activating substrates in metabolic reactions.{26065} GTP is essential for G protein-related signal transduction in second-messenger mechanisms where it is converted to GDP through the action of GTPases.{1257}  

     

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  • Guanosine 5′-triphosphate (GTP) acts as a substrate for the synthesis of RNA during the transcription process and the synthesis of DNA during DNA replication.{26064} It is generated by the citric acid cycle and provides a source of energy for protein synthesis and gluconeogenesis, activating substrates in metabolic reactions.{26065} GTP is essential for G protein-related signal transduction in second-messenger mechanisms where it is converted to GDP through the action of GTPases.{1257}  

     

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    Cayman
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  • Guanosine 5′-triphosphate (GTP) acts as a substrate for the synthesis of RNA during the transcription process and the synthesis of DNA during DNA replication.{26064} It is generated by the citric acid cycle and provides a source of energy for protein synthesis and gluconeogenesis, activating substrates in metabolic reactions.{26065} GTP is essential for G protein-related signal transduction in second-messenger mechanisms where it is converted to GDP through the action of GTPases.{1257}  

     

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    Cayman
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  • Guanylyl imidodiphosphate is a nonhydrolyzable analog of GTP that can bind to and irreversibly activate G proteins in the presence of Mg2+.{27512} This nucleotide is a potent stimulator of adenylate cyclase.{27510} Guanylyl imidodiphosphate is used in studies of protein synthesis since the process of GTP binding, hydrolysis, and release is essential for the initiation of protein translocation across the endoplasmic reticulum.{27511}  

     

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  • Guanylyl imidodiphosphate is a nonhydrolyzable analog of GTP that can bind to and irreversibly activate G proteins in the presence of Mg2+.{27512} This nucleotide is a potent stimulator of adenylate cyclase.{27510} Guanylyl imidodiphosphate is used in studies of protein synthesis since the process of GTP binding, hydrolysis, and release is essential for the initiation of protein translocation across the endoplasmic reticulum.{27511}  

     

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    Cayman
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  • Guanylyl imidodiphosphate is a nonhydrolyzable analog of GTP that can bind to and irreversibly activate G proteins in the presence of Mg2+.{27512} This nucleotide is a potent stimulator of adenylate cyclase.{27510} Guanylyl imidodiphosphate is used in studies of protein synthesis since the process of GTP binding, hydrolysis, and release is essential for the initiation of protein translocation across the endoplasmic reticulum.{27511}  

     

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    Cayman
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  • Guanylyl imidodiphosphate is a nonhydrolyzable analog of GTP that can bind to and irreversibly activate G proteins in the presence of Mg2+.{27512} This nucleotide is a potent stimulator of adenylate cyclase.{27510} Guanylyl imidodiphosphate is used in studies of protein synthesis since the process of GTP binding, hydrolysis, and release is essential for the initiation of protein translocation across the endoplasmic reticulum.{27511}  

     

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    Cayman
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  • Gue1654 is a Gβγ-signaling-biased 5-OxoETE receptor antagonist.{46628} It inhibits neutrophil and eosinophil shape change and chemotaxis induced by 5-OxoETE (Item No. 34250) but not chemoattractant C5a or prostaglandin D2 (PGD2; Item No. 12010). Gue1654 inhibits 5-OxoETE-induced Gβγ-mediated inositol monophosphate (IP1) production in HEK293 cells transiently expressing the 5-OxoETE receptor, an effect that can be blocked by the Gβγ-inhibitor gallein, but has no effect on IP1 production induced by stimulation of endogenous Gαq-linked muscarinic receptors. In a bioluminescence resonance energy transfer (BRET) assay, Gue1654 reduces the 5-OxoETE-induced, but not basal, BRET fluorescence response, indicating disruption of the interaction between ligand-activated 5-OxoETE receptor and Gβγ.  

     

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    Cayman
    SKU:29686 - 1 mg

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  • Gue1654 is a Gβγ-signaling-biased 5-OxoETE receptor antagonist.{46628} It inhibits neutrophil and eosinophil shape change and chemotaxis induced by 5-OxoETE (Item No. 34250) but not chemoattractant C5a or prostaglandin D2 (PGD2; Item No. 12010). Gue1654 inhibits 5-OxoETE-induced Gβγ-mediated inositol monophosphate (IP1) production in HEK293 cells transiently expressing the 5-OxoETE receptor, an effect that can be blocked by the Gβγ-inhibitor gallein, but has no effect on IP1 production induced by stimulation of endogenous Gαq-linked muscarinic receptors. In a bioluminescence resonance energy transfer (BRET) assay, Gue1654 reduces the 5-OxoETE-induced, but not basal, BRET fluorescence response, indicating disruption of the interaction between ligand-activated 5-OxoETE receptor and Gβγ.  

     

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    Cayman
    SKU:29686 - 10 mg

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  • Gue1654 is a Gβγ-signaling-biased 5-OxoETE receptor antagonist.{46628} It inhibits neutrophil and eosinophil shape change and chemotaxis induced by 5-OxoETE (Item No. 34250) but not chemoattractant C5a or prostaglandin D2 (PGD2; Item No. 12010). Gue1654 inhibits 5-OxoETE-induced Gβγ-mediated inositol monophosphate (IP1) production in HEK293 cells transiently expressing the 5-OxoETE receptor, an effect that can be blocked by the Gβγ-inhibitor gallein, but has no effect on IP1 production induced by stimulation of endogenous Gαq-linked muscarinic receptors. In a bioluminescence resonance energy transfer (BRET) assay, Gue1654 reduces the 5-OxoETE-induced, but not basal, BRET fluorescence response, indicating disruption of the interaction between ligand-activated 5-OxoETE receptor and Gβγ.  

     

    Brand:
    Cayman
    SKU:29686 - 25 mg

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  • Gue1654 is a Gβγ-signaling-biased 5-OxoETE receptor antagonist.{46628} It inhibits neutrophil and eosinophil shape change and chemotaxis induced by 5-OxoETE (Item No. 34250) but not chemoattractant C5a or prostaglandin D2 (PGD2; Item No. 12010). Gue1654 inhibits 5-OxoETE-induced Gβγ-mediated inositol monophosphate (IP1) production in HEK293 cells transiently expressing the 5-OxoETE receptor, an effect that can be blocked by the Gβγ-inhibitor gallein, but has no effect on IP1 production induced by stimulation of endogenous Gαq-linked muscarinic receptors. In a bioluminescence resonance energy transfer (BRET) assay, Gue1654 reduces the 5-OxoETE-induced, but not basal, BRET fluorescence response, indicating disruption of the interaction between ligand-activated 5-OxoETE receptor and Gβγ.  

     

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    Cayman
    SKU:29686 - 5 mg

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  • Guvacine is an amino acid found in A. catechu (Betel nut).{36158} It competitively inhibits GABA uptake (IC50 = 10 μM; Ki = 14 μM) in rat hippocampal brain slices.{36158,36159} In vivo, guvacine, at doses ranging from 50-100 mg/kg, decreases spontaneous activity in mice.{36158} Administration of guvacine also decreases tail flick reaction time in a rat model of morphine analgesia.{36160}  

     

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    Cayman
    SKU:23361 - 100 mg

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  • Guvacine is an amino acid found in A. catechu (Betel nut).{36158} It competitively inhibits GABA uptake (IC50 = 10 μM; Ki = 14 μM) in rat hippocampal brain slices.{36158,36159} In vivo, guvacine, at doses ranging from 50-100 mg/kg, decreases spontaneous activity in mice.{36158} Administration of guvacine also decreases tail flick reaction time in a rat model of morphine analgesia.{36160}  

     

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    Cayman
    SKU:23361 - 25 mg

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  • Guvacine is an amino acid found in A. catechu (Betel nut).{36158} It competitively inhibits GABA uptake (IC50 = 10 μM; Ki = 14 μM) in rat hippocampal brain slices.{36158,36159} In vivo, guvacine, at doses ranging from 50-100 mg/kg, decreases spontaneous activity in mice.{36158} Administration of guvacine also decreases tail flick reaction time in a rat model of morphine analgesia.{36160}  

     

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    Cayman
    SKU:23361 - 250 mg

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  • Guvacine is an amino acid found in A. catechu (Betel nut).{36158} It competitively inhibits GABA uptake (IC50 = 10 μM; Ki = 14 μM) in rat hippocampal brain slices.{36158,36159} In vivo, guvacine, at doses ranging from 50-100 mg/kg, decreases spontaneous activity in mice.{36158} Administration of guvacine also decreases tail flick reaction time in a rat model of morphine analgesia.{36160}  

     

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    Cayman
    SKU:23361 - 50 mg

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  • Guvacoline is a natural alkaloid found in areca nuts that is related to the nootropic, arecoline (Item No. 13662). Guvacoline can act as a full agonist of atrial and ileal muscarinic receptors, although at 15-fold reduced potency compared to arecoline.{28111} The metabolomics and toxicity of this compound have been reported.{28112,28113}  

     

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  • Guvacoline is a natural alkaloid found in areca nuts that is related to the nootropic, arecoline (Item No. 13662). Guvacoline can act as a full agonist of atrial and ileal muscarinic receptors, although at 15-fold reduced potency compared to arecoline.{28111} The metabolomics and toxicity of this compound have been reported.{28112,28113}  

     

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    Cayman
    SKU:-

    Out of stock

  • Guvacoline is a natural alkaloid found in areca nuts that is related to the nootropic, arecoline (Item No. 13662). Guvacoline can act as a full agonist of atrial and ileal muscarinic receptors, although at 15-fold reduced potency compared to arecoline.{28111} The metabolomics and toxicity of this compound have been reported.{28112,28113}  

     

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    Cayman
    SKU:-

    Out of stock

  • The transcription factor peroxisome proliferator-activated receptor δ (PPARδ) is a member of the superfamily of nuclear hormone receptors and is implicated both in lipid metabolism and in the regulation of genes with potential roles in neurotoxicity. GW 0742 is a selective PPARδ agonist (EC50 = 1.1 nM) that exhibits 1,000-fold selectivity over the other human PPAR subtypes.{11580} GW 0742 exhibits time-dependent neuroprotection in low KCl-induced apoptosis in cerebellar granule neuronal cultures. Despite the neuroprotective properties observed, prolonged (48h) incubation with GW 0742 produced significant inherent toxicity. This cell death was determined to be apoptotic as identified with the TUNEL assay.{14765}  

     

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    Cayman
    SKU:10006798 - 10 mg

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  • The transcription factor peroxisome proliferator-activated receptor δ (PPARδ) is a member of the superfamily of nuclear hormone receptors and is implicated both in lipid metabolism and in the regulation of genes with potential roles in neurotoxicity. GW 0742 is a selective PPARδ agonist (EC50 = 1.1 nM) that exhibits 1,000-fold selectivity over the other human PPAR subtypes.{11580} GW 0742 exhibits time-dependent neuroprotection in low KCl-induced apoptosis in cerebellar granule neuronal cultures. Despite the neuroprotective properties observed, prolonged (48h) incubation with GW 0742 produced significant inherent toxicity. This cell death was determined to be apoptotic as identified with the TUNEL assay.{14765}  

     

    Brand:
    Cayman
    SKU:10006798 - 25 mg

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  • The transcription factor peroxisome proliferator-activated receptor δ (PPARδ) is a member of the superfamily of nuclear hormone receptors and is implicated both in lipid metabolism and in the regulation of genes with potential roles in neurotoxicity. GW 0742 is a selective PPARδ agonist (EC50 = 1.1 nM) that exhibits 1,000-fold selectivity over the other human PPAR subtypes.{11580} GW 0742 exhibits time-dependent neuroprotection in low KCl-induced apoptosis in cerebellar granule neuronal cultures. Despite the neuroprotective properties observed, prolonged (48h) incubation with GW 0742 produced significant inherent toxicity. This cell death was determined to be apoptotic as identified with the TUNEL assay.{14765}  

     

    Brand:
    Cayman
    SKU:10006798 - 5 mg

    Available on backorder

  • The transcription factor peroxisome proliferator-activated receptor δ (PPARδ) is a member of the superfamily of nuclear hormone receptors and is implicated both in lipid metabolism and in the regulation of genes with potential roles in neurotoxicity. GW 0742 is a selective PPARδ agonist (EC50 = 1.1 nM) that exhibits 1,000-fold selectivity over the other human PPAR subtypes.{11580} GW 0742 exhibits time-dependent neuroprotection in low KCl-induced apoptosis in cerebellar granule neuronal cultures. Despite the neuroprotective properties observed, prolonged (48h) incubation with GW 0742 produced significant inherent toxicity. This cell death was determined to be apoptotic as identified with the TUNEL assay.{14765}  

     

    Brand:
    Cayman
    SKU:10006798 - 50 mg

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  • GPR40 (free fatty acid receptor 1; FFAR1) is a G protein-coupled receptor (GPCR) that is activated by saturated and unsaturated long chain fatty acids. It is thought to play a role in the potentiation of insulin secretion by fatty acids in a glucose-sensitive manner. GW 1100 is a selective antagonist of GPR40-mediated Ca2+ elevations in HEK293 cells stimulated by GW 9508 (an agonist of both GPR40 and GPR120 (FFAR4), another GPCR activated by long chain fatty acids) or linoleic acid with a pIC50 value equal to 5.99. However at concentrations up to 10 μM, GW 1100 has no effect on GPR120-mediated stimulation of intracellular Ca2+ release induced by either GW 9508 or linoleic acid.{14194} In the MIN6 mouse insulinoma cell line, 1 μM GW 1100 inhibits the potentiating effects of GW 9508 and linoleic acid on glucose-stimulated insulin secretion.{14194}  

     

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    SKU:10008908 - 10 mg

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  • GPR40 (free fatty acid receptor 1; FFAR1) is a G protein-coupled receptor (GPCR) that is activated by saturated and unsaturated long chain fatty acids. It is thought to play a role in the potentiation of insulin secretion by fatty acids in a glucose-sensitive manner. GW 1100 is a selective antagonist of GPR40-mediated Ca2+ elevations in HEK293 cells stimulated by GW 9508 (an agonist of both GPR40 and GPR120 (FFAR4), another GPCR activated by long chain fatty acids) or linoleic acid with a pIC50 value equal to 5.99. However at concentrations up to 10 μM, GW 1100 has no effect on GPR120-mediated stimulation of intracellular Ca2+ release induced by either GW 9508 or linoleic acid.{14194} In the MIN6 mouse insulinoma cell line, 1 μM GW 1100 inhibits the potentiating effects of GW 9508 and linoleic acid on glucose-stimulated insulin secretion.{14194}  

     

    Brand:
    Cayman
    SKU:10008908 - 25 mg

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  • GPR40 (free fatty acid receptor 1; FFAR1) is a G protein-coupled receptor (GPCR) that is activated by saturated and unsaturated long chain fatty acids. It is thought to play a role in the potentiation of insulin secretion by fatty acids in a glucose-sensitive manner. GW 1100 is a selective antagonist of GPR40-mediated Ca2+ elevations in HEK293 cells stimulated by GW 9508 (an agonist of both GPR40 and GPR120 (FFAR4), another GPCR activated by long chain fatty acids) or linoleic acid with a pIC50 value equal to 5.99. However at concentrations up to 10 μM, GW 1100 has no effect on GPR120-mediated stimulation of intracellular Ca2+ release induced by either GW 9508 or linoleic acid.{14194} In the MIN6 mouse insulinoma cell line, 1 μM GW 1100 inhibits the potentiating effects of GW 9508 and linoleic acid on glucose-stimulated insulin secretion.{14194}  

     

    Brand:
    Cayman
    SKU:10008908 - 5 mg

    Available on backorder

  • GPR40 (free fatty acid receptor 1; FFAR1) is a G protein-coupled receptor (GPCR) that is activated by saturated and unsaturated long chain fatty acids. It is thought to play a role in the potentiation of insulin secretion by fatty acids in a glucose-sensitive manner. GW 1100 is a selective antagonist of GPR40-mediated Ca2+ elevations in HEK293 cells stimulated by GW 9508 (an agonist of both GPR40 and GPR120 (FFAR4), another GPCR activated by long chain fatty acids) or linoleic acid with a pIC50 value equal to 5.99. However at concentrations up to 10 μM, GW 1100 has no effect on GPR120-mediated stimulation of intracellular Ca2+ release induced by either GW 9508 or linoleic acid.{14194} In the MIN6 mouse insulinoma cell line, 1 μM GW 1100 inhibits the potentiating effects of GW 9508 and linoleic acid on glucose-stimulated insulin secretion.{14194}  

     

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    Cayman
    SKU:10008908 - 50 mg

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  • Peroxisome proliferator-activated receptor (PPAR) γ is a nuclear receptor that, when activated, regulates fatty acid storage and glucose metabolism.{15751} The best known class of PPARγ ligands are the thiazolidinediones, including troglitazone (Item No. 71750) and rosiglitazone (Item No. 71740).{8461} GW 1929 is a non-thiazolidinedione activator of PPARγ that binds with a Ki value of 1.4 nM, with greater than 1,000-fold selectivity over other PPAR subtypes.{25251} It has anti-hyperglycemic and anti-hyperlipidemic activity when given orally in mouse and rat models of type 2 diabetes.{25251,25253} Both in vitro and in vivo effects of GW 1929 on PPARγ greatly exceed those produced by troglitazone.{25251,25253} In addition, GW 1929 has neuroprotective effects in global cerebral ischemic-reperfusion injury that are related to reduced inflammation and apoptotic DNA fragmentation.{25252}  

     

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  • Peroxisome proliferator-activated receptor (PPAR) γ is a nuclear receptor that, when activated, regulates fatty acid storage and glucose metabolism.{15751} The best known class of PPARγ ligands are the thiazolidinediones, including troglitazone (Item No. 71750) and rosiglitazone (Item No. 71740).{8461} GW 1929 is a non-thiazolidinedione activator of PPARγ that binds with a Ki value of 1.4 nM, with greater than 1,000-fold selectivity over other PPAR subtypes.{25251} It has anti-hyperglycemic and anti-hyperlipidemic activity when given orally in mouse and rat models of type 2 diabetes.{25251,25253} Both in vitro and in vivo effects of GW 1929 on PPARγ greatly exceed those produced by troglitazone.{25251,25253} In addition, GW 1929 has neuroprotective effects in global cerebral ischemic-reperfusion injury that are related to reduced inflammation and apoptotic DNA fragmentation.{25252}  

     

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    Cayman
    SKU:-
  • Peroxisome proliferator-activated receptor (PPAR) γ is a nuclear receptor that, when activated, regulates fatty acid storage and glucose metabolism.{15751} The best known class of PPARγ ligands are the thiazolidinediones, including troglitazone (Item No. 71750) and rosiglitazone (Item No. 71740).{8461} GW 1929 is a non-thiazolidinedione activator of PPARγ that binds with a Ki value of 1.4 nM, with greater than 1,000-fold selectivity over other PPAR subtypes.{25251} It has anti-hyperglycemic and anti-hyperlipidemic activity when given orally in mouse and rat models of type 2 diabetes.{25251,25253} Both in vitro and in vivo effects of GW 1929 on PPARγ greatly exceed those produced by troglitazone.{25251,25253} In addition, GW 1929 has neuroprotective effects in global cerebral ischemic-reperfusion injury that are related to reduced inflammation and apoptotic DNA fragmentation.{25252}  

     

    Brand:
    Cayman
    SKU:-
  • Peroxisome proliferator-activated receptor (PPAR) γ is a nuclear receptor that, when activated, regulates fatty acid storage and glucose metabolism.{15751} The best known class of PPARγ ligands are the thiazolidinediones, including troglitazone (Item No. 71750) and rosiglitazone (Item No. 71740).{8461} GW 1929 is a non-thiazolidinedione activator of PPARγ that binds with a Ki value of 1.4 nM, with greater than 1,000-fold selectivity over other PPAR subtypes.{25251} It has anti-hyperglycemic and anti-hyperlipidemic activity when given orally in mouse and rat models of type 2 diabetes.{25251,25253} Both in vitro and in vivo effects of GW 1929 on PPARγ greatly exceed those produced by troglitazone.{25251,25253} In addition, GW 1929 has neuroprotective effects in global cerebral ischemic-reperfusion injury that are related to reduced inflammation and apoptotic DNA fragmentation.{25252}  

     

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    Cayman
    SKU:-
  • cFMS kinase is the cellular homolog of the v-FMS oncogene product of the Susan McDonough strain of the feline sarcoma virus. It can autophosphorlyate colony-stimulating factor (CSF-1), which promotes the survival, proliferation, and differentiation of mononuclear phagocytes. GW 2580 selectively inhibits cFMS kinase (IC50 = 0.03 μM), preventing CSF-1-induced monocyte growth with an IC50 value of 0.14 μM.{25081} At 75-100 mg/kg, it has been shown to inhibit joint connective tissue and bone degradation in mouse models of arthritis.{25081}  

     

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    Cayman
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  • cFMS kinase is the cellular homolog of the v-FMS oncogene product of the Susan McDonough strain of the feline sarcoma virus. It can autophosphorlyate colony-stimulating factor (CSF-1), which promotes the survival, proliferation, and differentiation of mononuclear phagocytes. GW 2580 selectively inhibits cFMS kinase (IC50 = 0.03 μM), preventing CSF-1-induced monocyte growth with an IC50 value of 0.14 μM.{25081} At 75-100 mg/kg, it has been shown to inhibit joint connective tissue and bone degradation in mouse models of arthritis.{25081}  

     

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    Cayman
    SKU:-
  • cFMS kinase is the cellular homolog of the v-FMS oncogene product of the Susan McDonough strain of the feline sarcoma virus. It can autophosphorlyate colony-stimulating factor (CSF-1), which promotes the survival, proliferation, and differentiation of mononuclear phagocytes. GW 2580 selectively inhibits cFMS kinase (IC50 = 0.03 μM), preventing CSF-1-induced monocyte growth with an IC50 value of 0.14 μM.{25081} At 75-100 mg/kg, it has been shown to inhibit joint connective tissue and bone degradation in mouse models of arthritis.{25081}  

     

    Brand:
    Cayman
    SKU:-
  • cFMS kinase is the cellular homolog of the v-FMS oncogene product of the Susan McDonough strain of the feline sarcoma virus. It can autophosphorlyate colony-stimulating factor (CSF-1), which promotes the survival, proliferation, and differentiation of mononuclear phagocytes. GW 2580 selectively inhibits cFMS kinase (IC50 = 0.03 μM), preventing CSF-1-induced monocyte growth with an IC50 value of 0.14 μM.{25081} At 75-100 mg/kg, it has been shown to inhibit joint connective tissue and bone degradation in mouse models of arthritis.{25081}  

     

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    Cayman
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  • GW 311616A is an inhibitor of neutrophil elastase (Ki = 0.31 nM).{45465} It is selective for human neutrophil elastase (IC50 = 22 nM) over trypsin, cathepsin G, and plasmin (IC50s = >100 µM for all), as well as chymotrypsin and tissue plasminogen activator (IC50s = >3 µM for all), in a cell-free assay. GW 311616A inhibits neutrophil elastase activity in isolated dog whole blood and in the liver in a mouse model of liver ischemia-reperfusion injury when administered at a dose of 2 mg/kg.{45465},{45466}  

     

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    SKU:27957 - 1 mg

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  • GW 311616A is an inhibitor of neutrophil elastase (Ki = 0.31 nM).{45465} It is selective for human neutrophil elastase (IC50 = 22 nM) over trypsin, cathepsin G, and plasmin (IC50s = >100 µM for all), as well as chymotrypsin and tissue plasminogen activator (IC50s = >3 µM for all), in a cell-free assay. GW 311616A inhibits neutrophil elastase activity in isolated dog whole blood and in the liver in a mouse model of liver ischemia-reperfusion injury when administered at a dose of 2 mg/kg.{45465},{45466}  

     

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    Cayman
    SKU:27957 - 10 mg

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  • GW 311616A is an inhibitor of neutrophil elastase (Ki = 0.31 nM).{45465} It is selective for human neutrophil elastase (IC50 = 22 nM) over trypsin, cathepsin G, and plasmin (IC50s = >100 µM for all), as well as chymotrypsin and tissue plasminogen activator (IC50s = >3 µM for all), in a cell-free assay. GW 311616A inhibits neutrophil elastase activity in isolated dog whole blood and in the liver in a mouse model of liver ischemia-reperfusion injury when administered at a dose of 2 mg/kg.{45465},{45466}  

     

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    Cayman
    SKU:27957 - 5 mg

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  • The liver X receptors, LXRα and LXRβ, are nuclear receptors that act as ligand-dependent transcription factors.{24819} They modulate cholesterol, fatty acids, and glucose homeostasis. GW 3965 is an orally-active agonist of LXRα and LXRβ, activating the human isoforms with EC50 values of 190 and 30 nM, respectively.{10881} It alters LXR-regulated gene expression in mice and rats, affecting pathways related to glucose and lipid metabolism.{10881,24822,24821} GW 3965 also affects inflammation and pressor responses through LXRα and LXRβ.{10880,24823,24820}  

     

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    SKU:10054 - 1 mg

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  • The liver X receptors, LXRα and LXRβ, are nuclear receptors that act as ligand-dependent transcription factors.{24819} They modulate cholesterol, fatty acids, and glucose homeostasis. GW 3965 is an orally-active agonist of LXRα and LXRβ, activating the human isoforms with EC50 values of 190 and 30 nM, respectively.{10881} It alters LXR-regulated gene expression in mice and rats, affecting pathways related to glucose and lipid metabolism.{10881,24822,24821} GW 3965 also affects inflammation and pressor responses through LXRα and LXRβ.{10880,24823,24820}  

     

    Brand:
    Cayman
    SKU:10054 - 10 mg

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  • The liver X receptors, LXRα and LXRβ, are nuclear receptors that act as ligand-dependent transcription factors.{24819} They modulate cholesterol, fatty acids, and glucose homeostasis. GW 3965 is an orally-active agonist of LXRα and LXRβ, activating the human isoforms with EC50 values of 190 and 30 nM, respectively.{10881} It alters LXR-regulated gene expression in mice and rats, affecting pathways related to glucose and lipid metabolism.{10881,24822,24821} GW 3965 also affects inflammation and pressor responses through LXRα and LXRβ.{10880,24823,24820}  

     

    Brand:
    Cayman
    SKU:10054 - 5 mg

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  • GW 405833 is a partial agonist of the cannabinoid CB2 receptor (EC50 = 0.65 nM).{16338} It is selective for CB2, binding with a Ki value of 14 nM compared to that of CB1 with a Ki value of 2.04 µM.{16338} GW 405833 demonstrates anti-inflammatory and antihyperalgesic properties in animal models of inflammation and pain.{16338}  

     

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    Cayman
    SKU:20219 -

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  • GW 405833 is a partial agonist of the cannabinoid CB2 receptor (EC50 = 0.65 nM).{16338} It is selective for CB2, binding with a Ki value of 14 nM compared to that of CB1 with a Ki value of 2.04 µM.{16338} GW 405833 demonstrates anti-inflammatory and antihyperalgesic properties in animal models of inflammation and pain.{16338}  

     

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    Cayman
    SKU:20219 -

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  • GW 405833 is a partial agonist of the cannabinoid CB2 receptor (EC50 = 0.65 nM).{16338} It is selective for CB2, binding with a Ki value of 14 nM compared to that of CB1 with a Ki value of 2.04 µM.{16338} GW 405833 demonstrates anti-inflammatory and antihyperalgesic properties in animal models of inflammation and pain.{16338}  

     

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    Cayman
    SKU:20219 -

    Available on backorder

  • GW 405833 is a partial agonist of the cannabinoid CB2 receptor (EC50 = 0.65 nM).{16338} It is selective for CB2, binding with a Ki value of 14 nM compared to that of CB1 with a Ki value of 2.04 µM.{16338} GW 405833 demonstrates anti-inflammatory and antihyperalgesic properties in animal models of inflammation and pain.{16338}  

     

    Brand:
    Cayman
    SKU:20219 -

    Available on backorder

  • Farnesoid X receptor (FXR) is a nuclear receptor that acts as a bile acid sensor, protecting cells and organs against bile acid toxicity.{15284} GW 4064 is a selective agonist of FXR (EC50 = 15 nM).{12563} It displays no activity at other nuclear receptors, including the retinoic acid receptor, at concentrations up to 1 μM.{12563} GW 4064 is used to elucidate the role of FXR in dyslipidemia, diabetes, obesity, and cancer.{25476,25477,25475,25474,25473}  

     

    Brand:
    Cayman
    SKU:10006611 - 1 mg

    Available on backorder

  • Farnesoid X receptor (FXR) is a nuclear receptor that acts as a bile acid sensor, protecting cells and organs against bile acid toxicity.{15284} GW 4064 is a selective agonist of FXR (EC50 = 15 nM).{12563} It displays no activity at other nuclear receptors, including the retinoic acid receptor, at concentrations up to 1 μM.{12563} GW 4064 is used to elucidate the role of FXR in dyslipidemia, diabetes, obesity, and cancer.{25476,25477,25475,25474,25473}  

     

    Brand:
    Cayman
    SKU:10006611 - 10 mg

    Available on backorder

  • Farnesoid X receptor (FXR) is a nuclear receptor that acts as a bile acid sensor, protecting cells and organs against bile acid toxicity.{15284} GW 4064 is a selective agonist of FXR (EC50 = 15 nM).{12563} It displays no activity at other nuclear receptors, including the retinoic acid receptor, at concentrations up to 1 μM.{12563} GW 4064 is used to elucidate the role of FXR in dyslipidemia, diabetes, obesity, and cancer.{25476,25477,25475,25474,25473}  

     

    Brand:
    Cayman
    SKU:10006611 - 5 mg

    Available on backorder

  • The high affinity nerve growth factor (NGF) receptor, also known as NGF tyrosine kinase receptor A (TrkA), is involved in the development and maturation of the nervous system. Aberrant expression is associated with certain forms of cancer and congenital insensitivity to pain with anhidrosis.{27678,27676} GW 441756 is a potent inhibitor of TrkA (IC50 = 2 nM).{27675} It displays >100-fold selectivity over a panel of related kinases.{27675} GW 441756 has been used to clarify the role of TrkA in regulating gene expression in neuroblastoma cells and, more recently, in amyloid-β protein precursor cleavage in neuroglioma cells.{27677,27674}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • The high affinity nerve growth factor (NGF) receptor, also known as NGF tyrosine kinase receptor A (TrkA), is involved in the development and maturation of the nervous system. Aberrant expression is associated with certain forms of cancer and congenital insensitivity to pain with anhidrosis.{27678,27676} GW 441756 is a potent inhibitor of TrkA (IC50 = 2 nM).{27675} It displays >100-fold selectivity over a panel of related kinases.{27675} GW 441756 has been used to clarify the role of TrkA in regulating gene expression in neuroblastoma cells and, more recently, in amyloid-β protein precursor cleavage in neuroglioma cells.{27677,27674}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • The high affinity nerve growth factor (NGF) receptor, also known as NGF tyrosine kinase receptor A (TrkA), is involved in the development and maturation of the nervous system. Aberrant expression is associated with certain forms of cancer and congenital insensitivity to pain with anhidrosis.{27678,27676} GW 441756 is a potent inhibitor of TrkA (IC50 = 2 nM).{27675} It displays >100-fold selectivity over a panel of related kinases.{27675} GW 441756 has been used to clarify the role of TrkA in regulating gene expression in neuroblastoma cells and, more recently, in amyloid-β protein precursor cleavage in neuroglioma cells.{27677,27674}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • Neutral sphingomyelinases mediate the release of ceramide from sphingomyelin in cellular membranes and can be activated by certain stresses. Ceramide can act as a signaling molecule in its own right, or it can be further processed to generate sphingosine (and sphingosine-1-phosphate). GW 4869 is an inhibitor of neutral sphingomyelinase (IC50 = 1 μM).{17163} It is selective for neutral sphingomyelinase over acid sphingomyelinase at concentrations up to 150 μM as well as B. cereus PC-PLC, human lyso-PAF PLC, and bovine PP2A at 10 μM. GW 4869 inhibits TNF-α-induced sphingomyelin hydrolysis by 100% when used at a concentration of 20 μM and TNF-α-induced cell death in MCF-7 cells.{17163,17164} It also reduces the inhibitory effects of oxidized 1-palmitoyl-2-arachidonyl-sn-glycero-3-phosphatidylcholine (OxPAPC) and the 5-keto-6-octendioic acid ester of 2-lysophosphatidylethanolamine (KOdiA-PE) on LPS-induction of IL-8 in human aortic endothelial cells.{17165} In vivo, GW 4869 (1 mg/kg) reverses hypoxia-induced pulmonary vasoconstriction in rats.{17166}  

     

    Brand:
    Cayman
    SKU:-
  • Neutral sphingomyelinases mediate the release of ceramide from sphingomyelin in cellular membranes and can be activated by certain stresses. Ceramide can act as a signaling molecule in its own right, or it can be further processed to generate sphingosine (and sphingosine-1-phosphate). GW 4869 is an inhibitor of neutral sphingomyelinase (IC50 = 1 μM).{17163} It is selective for neutral sphingomyelinase over acid sphingomyelinase at concentrations up to 150 μM as well as B. cereus PC-PLC, human lyso-PAF PLC, and bovine PP2A at 10 μM. GW 4869 inhibits TNF-α-induced sphingomyelin hydrolysis by 100% when used at a concentration of 20 μM and TNF-α-induced cell death in MCF-7 cells.{17163,17164} It also reduces the inhibitory effects of oxidized 1-palmitoyl-2-arachidonyl-sn-glycero-3-phosphatidylcholine (OxPAPC) and the 5-keto-6-octendioic acid ester of 2-lysophosphatidylethanolamine (KOdiA-PE) on LPS-induction of IL-8 in human aortic endothelial cells.{17165} In vivo, GW 4869 (1 mg/kg) reverses hypoxia-induced pulmonary vasoconstriction in rats.{17166}  

     

    Brand:
    Cayman
    SKU:-
  • Neutral sphingomyelinases mediate the release of ceramide from sphingomyelin in cellular membranes and can be activated by certain stresses. Ceramide can act as a signaling molecule in its own right, or it can be further processed to generate sphingosine (and sphingosine-1-phosphate). GW 4869 is an inhibitor of neutral sphingomyelinase (IC50 = 1 μM).{17163} It is selective for neutral sphingomyelinase over acid sphingomyelinase at concentrations up to 150 μM as well as B. cereus PC-PLC, human lyso-PAF PLC, and bovine PP2A at 10 μM. GW 4869 inhibits TNF-α-induced sphingomyelin hydrolysis by 100% when used at a concentration of 20 μM and TNF-α-induced cell death in MCF-7 cells.{17163,17164} It also reduces the inhibitory effects of oxidized 1-palmitoyl-2-arachidonyl-sn-glycero-3-phosphatidylcholine (OxPAPC) and the 5-keto-6-octendioic acid ester of 2-lysophosphatidylethanolamine (KOdiA-PE) on LPS-induction of IL-8 in human aortic endothelial cells.{17165} In vivo, GW 4869 (1 mg/kg) reverses hypoxia-induced pulmonary vasoconstriction in rats.{17166}  

     

    Brand:
    Cayman
    SKU:-
  • Neutral sphingomyelinases mediate the release of ceramide from sphingomyelin in cellular membranes and can be activated by certain stresses. Ceramide can act as a signaling molecule in its own right, or it can be further processed to generate sphingosine (and sphingosine-1-phosphate). GW 4869 is an inhibitor of neutral sphingomyelinase (IC50 = 1 μM).{17163} It is selective for neutral sphingomyelinase over acid sphingomyelinase at concentrations up to 150 μM as well as B. cereus PC-PLC, human lyso-PAF PLC, and bovine PP2A at 10 μM. GW 4869 inhibits TNF-α-induced sphingomyelin hydrolysis by 100% when used at a concentration of 20 μM and TNF-α-induced cell death in MCF-7 cells.{17163,17164} It also reduces the inhibitory effects of oxidized 1-palmitoyl-2-arachidonyl-sn-glycero-3-phosphatidylcholine (OxPAPC) and the 5-keto-6-octendioic acid ester of 2-lysophosphatidylethanolamine (KOdiA-PE) on LPS-induction of IL-8 in human aortic endothelial cells.{17165} In vivo, GW 4869 (1 mg/kg) reverses hypoxia-induced pulmonary vasoconstriction in rats.{17166}  

     

    Brand:
    Cayman
    SKU:-
  • Peroxisome proliferator-activated receptor δ (PPARδ) stimulation or over-expression in adipocytes leads to increased fatty acid oxidation, improved exercise tolerance, and resistance to obesity.{11581} GW 501516 is the first highly selective synthetic PPARδ agonist available. GW 501516 binds to human PPARδ with an IC50 value of 1 nM, and is at least 100-fold selective for PPARδ compared to PPARα and PPARγ.{11580} In obese primates, GW 501516 increases high density lipoprotein cholesterol and apolipoprotein A-1 specific reverse cholesterol transport.{11379} GW 501516 is therefore a model compound for a new type of obesity therapeutic, as well as a selective pharmacological tool for understanding lipid metabolism.  

     

    Brand:
    Cayman
    SKU:10004272 - 1 mg

    Available on backorder

  • Peroxisome proliferator-activated receptor δ (PPARδ) stimulation or over-expression in adipocytes leads to increased fatty acid oxidation, improved exercise tolerance, and resistance to obesity.{11581} GW 501516 is the first highly selective synthetic PPARδ agonist available. GW 501516 binds to human PPARδ with an IC50 value of 1 nM, and is at least 100-fold selective for PPARδ compared to PPARα and PPARγ.{11580} In obese primates, GW 501516 increases high density lipoprotein cholesterol and apolipoprotein A-1 specific reverse cholesterol transport.{11379} GW 501516 is therefore a model compound for a new type of obesity therapeutic, as well as a selective pharmacological tool for understanding lipid metabolism.  

     

    Brand:
    Cayman
    SKU:10004272 - 10 mg

    Available on backorder

  • Peroxisome proliferator-activated receptor δ (PPARδ) stimulation or over-expression in adipocytes leads to increased fatty acid oxidation, improved exercise tolerance, and resistance to obesity.{11581} GW 501516 is the first highly selective synthetic PPARδ agonist available. GW 501516 binds to human PPARδ with an IC50 value of 1 nM, and is at least 100-fold selective for PPARδ compared to PPARα and PPARγ.{11580} In obese primates, GW 501516 increases high density lipoprotein cholesterol and apolipoprotein A-1 specific reverse cholesterol transport.{11379} GW 501516 is therefore a model compound for a new type of obesity therapeutic, as well as a selective pharmacological tool for understanding lipid metabolism.  

     

    Brand:
    Cayman
    SKU:10004272 - 5 mg

    Available on backorder

  • Raf-1 is a proto-oncogene serine/threonine protein kinase that signals from Ras to the MAPK/ERK signaling pathway.{14539,15155} This pathway mediates basic cellular functions, including proliferation, differentiation, and survival.{14539} GW 5074 is a potent, selective, and cell-permeable inhibitor of Raf-1 (IC50 = 9 nM).{24584} It blocks phosphorylation of ERK1/2 by 90% in cells stimulated with epidermal growth factor when given at 5 µM.{24584} GW 5074 shows more than 100-fold selectivity for Raf-1 versus several related kinases.{24584}  

     

    Brand:
    Cayman
    SKU:10010368 - 1 mg

    Available on backorder

  • Raf-1 is a proto-oncogene serine/threonine protein kinase that signals from Ras to the MAPK/ERK signaling pathway.{14539,15155} This pathway mediates basic cellular functions, including proliferation, differentiation, and survival.{14539} GW 5074 is a potent, selective, and cell-permeable inhibitor of Raf-1 (IC50 = 9 nM).{24584} It blocks phosphorylation of ERK1/2 by 90% in cells stimulated with epidermal growth factor when given at 5 µM.{24584} GW 5074 shows more than 100-fold selectivity for Raf-1 versus several related kinases.{24584}  

     

    Brand:
    Cayman
    SKU:10010368 - 10 mg

    Available on backorder

  • Raf-1 is a proto-oncogene serine/threonine protein kinase that signals from Ras to the MAPK/ERK signaling pathway.{14539,15155} This pathway mediates basic cellular functions, including proliferation, differentiation, and survival.{14539} GW 5074 is a potent, selective, and cell-permeable inhibitor of Raf-1 (IC50 = 9 nM).{24584} It blocks phosphorylation of ERK1/2 by 90% in cells stimulated with epidermal growth factor when given at 5 µM.{24584} GW 5074 shows more than 100-fold selectivity for Raf-1 versus several related kinases.{24584}  

     

    Brand:
    Cayman
    SKU:10010368 - 25 mg

    Available on backorder

  • Raf-1 is a proto-oncogene serine/threonine protein kinase that signals from Ras to the MAPK/ERK signaling pathway.{14539,15155} This pathway mediates basic cellular functions, including proliferation, differentiation, and survival.{14539} GW 5074 is a potent, selective, and cell-permeable inhibitor of Raf-1 (IC50 = 9 nM).{24584} It blocks phosphorylation of ERK1/2 by 90% in cells stimulated with epidermal growth factor when given at 5 µM.{24584} GW 5074 shows more than 100-fold selectivity for Raf-1 versus several related kinases.{24584}  

     

    Brand:
    Cayman
    SKU:10010368 - 5 mg

    Available on backorder

  • The peroxisome proliferator-activated receptors (PPARs) α, γ, and δ are ligand-activated transcription factors that play a key role in lipid homeostasis. Activation of PPARα results in increased clearance of triglyceride (TG) rich very low-density lipoprotein (VLDL) via a reduction in plasma levels of ApoCIII and in upregulation of ApoA1, the principal lipoprotein component of HDL.{14733} GW 590735 is a potent and selective agonist of PPARα with an EC50 value of 4 nM for the expression a GAL4-responsive reporter gene and at least 500-fold selectivity versus PPARγ and PPARδ.{14733}  

     

    Brand:
    Cayman
    SKU:10009880 - 1 mg

    Available on backorder

  • The peroxisome proliferator-activated receptors (PPARs) α, γ, and δ are ligand-activated transcription factors that play a key role in lipid homeostasis. Activation of PPARα results in increased clearance of triglyceride (TG) rich very low-density lipoprotein (VLDL) via a reduction in plasma levels of ApoCIII and in upregulation of ApoA1, the principal lipoprotein component of HDL.{14733} GW 590735 is a potent and selective agonist of PPARα with an EC50 value of 4 nM for the expression a GAL4-responsive reporter gene and at least 500-fold selectivity versus PPARγ and PPARδ.{14733}  

     

    Brand:
    Cayman
    SKU:10009880 - 10 mg

    Available on backorder

  • The peroxisome proliferator-activated receptors (PPARs) α, γ, and δ are ligand-activated transcription factors that play a key role in lipid homeostasis. Activation of PPARα results in increased clearance of triglyceride (TG) rich very low-density lipoprotein (VLDL) via a reduction in plasma levels of ApoCIII and in upregulation of ApoA1, the principal lipoprotein component of HDL.{14733} GW 590735 is a potent and selective agonist of PPARα with an EC50 value of 4 nM for the expression a GAL4-responsive reporter gene and at least 500-fold selectivity versus PPARγ and PPARδ.{14733}  

     

    Brand:
    Cayman
    SKU:10009880 - 25 mg

    Available on backorder

  • The peroxisome proliferator-activated receptors (PPARs) α, γ, and δ are ligand-activated transcription factors that play a key role in lipid homeostasis. Activation of PPARα results in increased clearance of triglyceride (TG) rich very low-density lipoprotein (VLDL) via a reduction in plasma levels of ApoCIII and in upregulation of ApoA1, the principal lipoprotein component of HDL.{14733} GW 590735 is a potent and selective agonist of PPARα with an EC50 value of 4 nM for the expression a GAL4-responsive reporter gene and at least 500-fold selectivity versus PPARγ and PPARδ.{14733}  

     

    Brand:
    Cayman
    SKU:10009880 - 5 mg

    Available on backorder

  • GW 610 is an antitumor benzothiazole that shows growth-inhibitory activity against several cancer cell lines. In MCF-7 and MDA 468 human cancer cell lines, potent antiproliferative activity (growth inhibition (GI50) (4-aminophenyl)benzothiazoles, GW 610 is not reliant on induction of cytochrome P 1A1 (CYP1A1) expression for antitumor activity.  

     

    Brand:
    Cayman
    SKU:10008313 - 1 mg

    Available on backorder

  • GW 610 is an antitumor benzothiazole that shows growth-inhibitory activity against several cancer cell lines. In MCF-7 and MDA 468 human cancer cell lines, potent antiproliferative activity (growth inhibition (GI50) (4-aminophenyl)benzothiazoles, GW 610 is not reliant on induction of cytochrome P 1A1 (CYP1A1) expression for antitumor activity.  

     

    Brand:
    Cayman
    SKU:10008313 - 10 mg

    Available on backorder

  • GW 610 is an antitumor benzothiazole that shows growth-inhibitory activity against several cancer cell lines. In MCF-7 and MDA 468 human cancer cell lines, potent antiproliferative activity (growth inhibition (GI50) (4-aminophenyl)benzothiazoles, GW 610 is not reliant on induction of cytochrome P 1A1 (CYP1A1) expression for antitumor activity.  

     

    Brand:
    Cayman
    SKU:10008313 - 5 mg

    Available on backorder

  • GW 610 is an antitumor benzothiazole that shows growth-inhibitory activity against several cancer cell lines. In MCF-7 and MDA 468 human cancer cell lines, potent antiproliferative activity (growth inhibition (GI50) (4-aminophenyl)benzothiazoles, GW 610 is not reliant on induction of cytochrome P 1A1 (CYP1A1) expression for antitumor activity.  

     

    Brand:
    Cayman
    SKU:10008313 - 50 mg

    Available on backorder

  • The effects of prostaglandin E2 (PGE2) are transduced by at least four distinct receptors designated EP1, EP2, EP3, and EP4.{1422} GW 627368X is a potent and selective competitive antagonist of the EP4 receptor with additional human TP receptor affinity. In competition radioligand bioassays, GW 627368X had affinity for human EP4 and TP receptors with Ki values of 100 nM and 158 nM, respectively.{14284} Affinity for all other human prostanoid receptors is >5.0 µM. In human washed platelets, GW 627368X produced 100% inhibition of U-46619 (EC100)-induced aggregation at a concentration of 10 µM.  

     

    Brand:
    Cayman
    SKU:10009162 - 1 mg

    Available on backorder

  • The effects of prostaglandin E2 (PGE2) are transduced by at least four distinct receptors designated EP1, EP2, EP3, and EP4.{1422} GW 627368X is a potent and selective competitive antagonist of the EP4 receptor with additional human TP receptor affinity. In competition radioligand bioassays, GW 627368X had affinity for human EP4 and TP receptors with Ki values of 100 nM and 158 nM, respectively.{14284} Affinity for all other human prostanoid receptors is >5.0 µM. In human washed platelets, GW 627368X produced 100% inhibition of U-46619 (EC100)-induced aggregation at a concentration of 10 µM.  

     

    Brand:
    Cayman
    SKU:10009162 - 10 mg

    Available on backorder

  • The effects of prostaglandin E2 (PGE2) are transduced by at least four distinct receptors designated EP1, EP2, EP3, and EP4.{1422} GW 627368X is a potent and selective competitive antagonist of the EP4 receptor with additional human TP receptor affinity. In competition radioligand bioassays, GW 627368X had affinity for human EP4 and TP receptors with Ki values of 100 nM and 158 nM, respectively.{14284} Affinity for all other human prostanoid receptors is >5.0 µM. In human washed platelets, GW 627368X produced 100% inhibition of U-46619 (EC100)-induced aggregation at a concentration of 10 µM.  

     

    Brand:
    Cayman
    SKU:10009162 - 25 mg

    Available on backorder

  • The effects of prostaglandin E2 (PGE2) are transduced by at least four distinct receptors designated EP1, EP2, EP3, and EP4.{1422} GW 627368X is a potent and selective competitive antagonist of the EP4 receptor with additional human TP receptor affinity. In competition radioligand bioassays, GW 627368X had affinity for human EP4 and TP receptors with Ki values of 100 nM and 158 nM, respectively.{14284} Affinity for all other human prostanoid receptors is >5.0 µM. In human washed platelets, GW 627368X produced 100% inhibition of U-46619 (EC100)-induced aggregation at a concentration of 10 µM.  

     

    Brand:
    Cayman
    SKU:10009162 - 5 mg

    Available on backorder

  • The peroxisome proliferator-activated receptor α (PPARα) is a nuclear receptor that regulates the expression of genes involved in fatty acid metabolism, lipoprotein synthesis and metabolism, and inflammation.{7654,14916,20898} GW 6471 is an antagonist of PPARα (IC50 = 240 nM).{23912} It drives the displacement of coactivators from PPARα and promotes the recruitment of co-repressor proteins like nuclear co-repressor.{23912} GW 6471 is used in cell-free, cell lysate, and whole cell systems to examine the impact of PPARα antagonism.{23911,23910,23913}  

     

    Brand:
    Cayman
    SKU:11697 - 1 mg

    Available on backorder

  • The peroxisome proliferator-activated receptor α (PPARα) is a nuclear receptor that regulates the expression of genes involved in fatty acid metabolism, lipoprotein synthesis and metabolism, and inflammation.{7654,14916,20898} GW 6471 is an antagonist of PPARα (IC50 = 240 nM).{23912} It drives the displacement of coactivators from PPARα and promotes the recruitment of co-repressor proteins like nuclear co-repressor.{23912} GW 6471 is used in cell-free, cell lysate, and whole cell systems to examine the impact of PPARα antagonism.{23911,23910,23913}  

     

    Brand:
    Cayman
    SKU:11697 - 10 mg

    Available on backorder

  • The peroxisome proliferator-activated receptor α (PPARα) is a nuclear receptor that regulates the expression of genes involved in fatty acid metabolism, lipoprotein synthesis and metabolism, and inflammation.{7654,14916,20898} GW 6471 is an antagonist of PPARα (IC50 = 240 nM).{23912} It drives the displacement of coactivators from PPARα and promotes the recruitment of co-repressor proteins like nuclear co-repressor.{23912} GW 6471 is used in cell-free, cell lysate, and whole cell systems to examine the impact of PPARα antagonism.{23911,23910,23913}  

     

    Brand:
    Cayman
    SKU:11697 - 25 mg

    Available on backorder

  • The peroxisome proliferator-activated receptor α (PPARα) is a nuclear receptor that regulates the expression of genes involved in fatty acid metabolism, lipoprotein synthesis and metabolism, and inflammation.{7654,14916,20898} GW 6471 is an antagonist of PPARα (IC50 = 240 nM).{23912} It drives the displacement of coactivators from PPARα and promotes the recruitment of co-repressor proteins like nuclear co-repressor.{23912} GW 6471 is used in cell-free, cell lysate, and whole cell systems to examine the impact of PPARα antagonism.{23911,23910,23913}  

     

    Brand:
    Cayman
    SKU:11697 - 5 mg

    Available on backorder

  • Peroxisome proliferator-activated receptor-α (PPARα) is a ligand-activated transcription factor involved in the regulation of lipid homeostasis.{6374,4136} Activation of PPARα results in expression of a variety of genes, particularly those involved in fatty acid β-oxidation, binding, and transport.{11955} GW 7647 is a potent, selective agonist of human and murine PPARα{14085} It activates human PPARα, PPARγ, and PPARδ with EC50 values of 0.006, 1.1 and 6.2 µM, respectively, in a GAL4-PPAR binding assay. Similar EC50 values of 0.001, 1.3, and 2.9 were observed with the murine receptors. GW 7647 lowered triglycerides 93% and 60% in fat-fed hamsters and rats, respectively, at a dose of 3 mg/kg.{14085}  

     

    Brand:
    Cayman
    SKU:10008613 - 1 mg

    Available on backorder

  • Peroxisome proliferator-activated receptor-α (PPARα) is a ligand-activated transcription factor involved in the regulation of lipid homeostasis.{6374,4136} Activation of PPARα results in expression of a variety of genes, particularly those involved in fatty acid β-oxidation, binding, and transport.{11955} GW 7647 is a potent, selective agonist of human and murine PPARα{14085} It activates human PPARα, PPARγ, and PPARδ with EC50 values of 0.006, 1.1 and 6.2 µM, respectively, in a GAL4-PPAR binding assay. Similar EC50 values of 0.001, 1.3, and 2.9 were observed with the murine receptors. GW 7647 lowered triglycerides 93% and 60% in fat-fed hamsters and rats, respectively, at a dose of 3 mg/kg.{14085}  

     

    Brand:
    Cayman
    SKU:10008613 - 10 mg

    Available on backorder

  • Peroxisome proliferator-activated receptor-α (PPARα) is a ligand-activated transcription factor involved in the regulation of lipid homeostasis.{6374,4136} Activation of PPARα results in expression of a variety of genes, particularly those involved in fatty acid β-oxidation, binding, and transport.{11955} GW 7647 is a potent, selective agonist of human and murine PPARα{14085} It activates human PPARα, PPARγ, and PPARδ with EC50 values of 0.006, 1.1 and 6.2 µM, respectively, in a GAL4-PPAR binding assay. Similar EC50 values of 0.001, 1.3, and 2.9 were observed with the murine receptors. GW 7647 lowered triglycerides 93% and 60% in fat-fed hamsters and rats, respectively, at a dose of 3 mg/kg.{14085}  

     

    Brand:
    Cayman
    SKU:10008613 - 25 mg

    Available on backorder

  • Peroxisome proliferator-activated receptor-α (PPARα) is a ligand-activated transcription factor involved in the regulation of lipid homeostasis.{6374,4136} Activation of PPARα results in expression of a variety of genes, particularly those involved in fatty acid β-oxidation, binding, and transport.{11955} GW 7647 is a potent, selective agonist of human and murine PPARα{14085} It activates human PPARα, PPARγ, and PPARδ with EC50 values of 0.006, 1.1 and 6.2 µM, respectively, in a GAL4-PPAR binding assay. Similar EC50 values of 0.001, 1.3, and 2.9 were observed with the murine receptors. GW 7647 lowered triglycerides 93% and 60% in fat-fed hamsters and rats, respectively, at a dose of 3 mg/kg.{14085}  

     

    Brand:
    Cayman
    SKU:10008613 - 5 mg

    Available on backorder

  • GW 766994 is an antagonist of chemokine (C-C motif) receptor 3 (CCR3) with a Ki value of 13.8 nM in an assay of eosinophil chemotaxis induced by chemokine (C-C motif) ligand 11 (CCL11).{50126} It decreases CCL11-induced cyclin-dependent kinase 5 (Cdk5) and tau phosphorylation and production of amyloid β (1-42) (Aβ42) in isolated mouse hippocampal neurons when used at a concentration of 10 µM.{50127}  

     

    Brand:
    Cayman
    SKU:28431 - 1 mg

    Available on backorder

  • GW 766994 is an antagonist of chemokine (C-C motif) receptor 3 (CCR3) with a Ki value of 13.8 nM in an assay of eosinophil chemotaxis induced by chemokine (C-C motif) ligand 11 (CCL11).{50126} It decreases CCL11-induced cyclin-dependent kinase 5 (Cdk5) and tau phosphorylation and production of amyloid β (1-42) (Aβ42) in isolated mouse hippocampal neurons when used at a concentration of 10 µM.{50127}  

     

    Brand:
    Cayman
    SKU:28431 - 5 mg

    Available on backorder

  • GW 788388 is a selective inhibitor of transforming growth factor-β (TGF-β) type 1 receptor (TGFBR1 or ALK5; IC50 = 18 nM).{27870} It inhibits the expression of collagen type I in cells (IC50 = 93 nM) and in mice when given orally at 10 mg/kg once a day.{27870} As TGF-β stimulates fibrosis in a range of tissues, GW 788388 reduces typical features of fibrosis, including tissue remodeling, increased expression of α-smooth muscle actin and production of collagen I.{27872,27874,27875} GW 788388 also blocks TGF-β-mediated production of VEGF by fibroblasts, as well as subsequent angiogenesis in vitro.{27873} Inhibition of ALK5 signaling by GW 788388 also induces hypertrophy in femoral growth plates in rats.{27871}  

     

    Brand:
    Cayman
    SKU:-
  • GW 788388 is a selective inhibitor of transforming growth factor-β (TGF-β) type 1 receptor (TGFBR1 or ALK5; IC50 = 18 nM).{27870} It inhibits the expression of collagen type I in cells (IC50 = 93 nM) and in mice when given orally at 10 mg/kg once a day.{27870} As TGF-β stimulates fibrosis in a range of tissues, GW 788388 reduces typical features of fibrosis, including tissue remodeling, increased expression of α-smooth muscle actin and production of collagen I.{27872,27874,27875} GW 788388 also blocks TGF-β-mediated production of VEGF by fibroblasts, as well as subsequent angiogenesis in vitro.{27873} Inhibition of ALK5 signaling by GW 788388 also induces hypertrophy in femoral growth plates in rats.{27871}  

     

    Brand:
    Cayman
    SKU:-
  • GW 788388 is a selective inhibitor of transforming growth factor-β (TGF-β) type 1 receptor (TGFBR1 or ALK5; IC50 = 18 nM).{27870} It inhibits the expression of collagen type I in cells (IC50 = 93 nM) and in mice when given orally at 10 mg/kg once a day.{27870} As TGF-β stimulates fibrosis in a range of tissues, GW 788388 reduces typical features of fibrosis, including tissue remodeling, increased expression of α-smooth muscle actin and production of collagen I.{27872,27874,27875} GW 788388 also blocks TGF-β-mediated production of VEGF by fibroblasts, as well as subsequent angiogenesis in vitro.{27873} Inhibition of ALK5 signaling by GW 788388 also induces hypertrophy in femoral growth plates in rats.{27871}  

     

    Brand:
    Cayman
    SKU:-
  • GW 788388 is a selective inhibitor of transforming growth factor-β (TGF-β) type 1 receptor (TGFBR1 or ALK5; IC50 = 18 nM).{27870} It inhibits the expression of collagen type I in cells (IC50 = 93 nM) and in mice when given orally at 10 mg/kg once a day.{27870} As TGF-β stimulates fibrosis in a range of tissues, GW 788388 reduces typical features of fibrosis, including tissue remodeling, increased expression of α-smooth muscle actin and production of collagen I.{27872,27874,27875} GW 788388 also blocks TGF-β-mediated production of VEGF by fibroblasts, as well as subsequent angiogenesis in vitro.{27873} Inhibition of ALK5 signaling by GW 788388 also induces hypertrophy in femoral growth plates in rats.{27871}  

     

    Brand:
    Cayman
    SKU:-
  • GW 803430 is an antagonist of melanin-concentrating hormone receptor 1 (MCH1; IC50 = 0.5 nM).{45224} It reduces cumulative body weight and food intake in diet-induced obese rats when administered at doses of 1 and 3 mg/kg.{45225} GW 803430 (10 and 30 mg/kg) decreases marble-burying behavior in mice, indicating anxiolytic activity, but does not affect performance in the rotorod test. It also reduces immobility time in the forced swim and tail suspension tests in mice at doses of 3 and 10 mg/kg, respectively, indicating antidepressant-like activity.  

     

    Brand:
    Cayman
    SKU:-
  • GW 803430 is an antagonist of melanin-concentrating hormone receptor 1 (MCH1; IC50 = 0.5 nM).{45224} It reduces cumulative body weight and food intake in diet-induced obese rats when administered at doses of 1 and 3 mg/kg.{45225} GW 803430 (10 and 30 mg/kg) decreases marble-burying behavior in mice, indicating anxiolytic activity, but does not affect performance in the rotorod test. It also reduces immobility time in the forced swim and tail suspension tests in mice at doses of 3 and 10 mg/kg, respectively, indicating antidepressant-like activity.  

     

    Brand:
    Cayman
    SKU:-
  • GW 803430 is an antagonist of melanin-concentrating hormone receptor 1 (MCH1; IC50 = 0.5 nM).{45224} It reduces cumulative body weight and food intake in diet-induced obese rats when administered at doses of 1 and 3 mg/kg.{45225} GW 803430 (10 and 30 mg/kg) decreases marble-burying behavior in mice, indicating anxiolytic activity, but does not affect performance in the rotorod test. It also reduces immobility time in the forced swim and tail suspension tests in mice at doses of 3 and 10 mg/kg, respectively, indicating antidepressant-like activity.  

     

    Brand:
    Cayman
    SKU:-
  • GW 803430 is an antagonist of melanin-concentrating hormone receptor 1 (MCH1; IC50 = 0.5 nM).{45224} It reduces cumulative body weight and food intake in diet-induced obese rats when administered at doses of 1 and 3 mg/kg.{45225} GW 803430 (10 and 30 mg/kg) decreases marble-burying behavior in mice, indicating anxiolytic activity, but does not affect performance in the rotorod test. It also reduces immobility time in the forced swim and tail suspension tests in mice at doses of 3 and 10 mg/kg, respectively, indicating antidepressant-like activity.  

     

    Brand:
    Cayman
    SKU:-
  • The peripheral cannabinoid (CB2) receptor is a G protein-coupled receptor (GPCR) that is localized predominantly in immune cells, monocytes, macrophages, and in several peripheral organs and binds the active component of cannabis, Δ9-tetrahydrocannabinol, as well as anandamide, an endogenous CB receptor ligand.{15353} GW 842166X is a peripheral cannabinoid (CB2) receptor agonist with ED50 values of 91 and 63 nM in rat and human, respectively.{14965} When administered orally to rats in the Freund’s complete adjuvant (FCA) model of inflammatory pain, GW 842166X is highly potent with an ED50 value of 0.1 mg/kg and full reversal of hyperalgesia at 0.3 mg/kg.{14965}  

     

    Brand:
    Cayman
    SKU:10010372 - 1 mg

    Available on backorder

  • The peripheral cannabinoid (CB2) receptor is a G protein-coupled receptor (GPCR) that is localized predominantly in immune cells, monocytes, macrophages, and in several peripheral organs and binds the active component of cannabis, Δ9-tetrahydrocannabinol, as well as anandamide, an endogenous CB receptor ligand.{15353} GW 842166X is a peripheral cannabinoid (CB2) receptor agonist with ED50 values of 91 and 63 nM in rat and human, respectively.{14965} When administered orally to rats in the Freund’s complete adjuvant (FCA) model of inflammatory pain, GW 842166X is highly potent with an ED50 value of 0.1 mg/kg and full reversal of hyperalgesia at 0.3 mg/kg.{14965}  

     

    Brand:
    Cayman
    SKU:10010372 - 10 mg

    Available on backorder

  • The peripheral cannabinoid (CB2) receptor is a G protein-coupled receptor (GPCR) that is localized predominantly in immune cells, monocytes, macrophages, and in several peripheral organs and binds the active component of cannabis, Δ9-tetrahydrocannabinol, as well as anandamide, an endogenous CB receptor ligand.{15353} GW 842166X is a peripheral cannabinoid (CB2) receptor agonist with ED50 values of 91 and 63 nM in rat and human, respectively.{14965} When administered orally to rats in the Freund’s complete adjuvant (FCA) model of inflammatory pain, GW 842166X is highly potent with an ED50 value of 0.1 mg/kg and full reversal of hyperalgesia at 0.3 mg/kg.{14965}  

     

    Brand:
    Cayman
    SKU:10010372 - 25 mg

    Available on backorder

  • The peripheral cannabinoid (CB2) receptor is a G protein-coupled receptor (GPCR) that is localized predominantly in immune cells, monocytes, macrophages, and in several peripheral organs and binds the active component of cannabis, Δ9-tetrahydrocannabinol, as well as anandamide, an endogenous CB receptor ligand.{15353} GW 842166X is a peripheral cannabinoid (CB2) receptor agonist with ED50 values of 91 and 63 nM in rat and human, respectively.{14965} When administered orally to rats in the Freund’s complete adjuvant (FCA) model of inflammatory pain, GW 842166X is highly potent with an ED50 value of 0.1 mg/kg and full reversal of hyperalgesia at 0.3 mg/kg.{14965}  

     

    Brand:
    Cayman
    SKU:10010372 - 5 mg

    Available on backorder

  • Four G protein-coupled receptors, EP1-4, initiate cellular signaling in response to prostaglandin PGE2. The receptor EP1 acts via Gαq to evoke diverse effects, including renal vasoconstriction, bronchoconstriction, hyperalgesia, allodynia, gastric protection, hyperthermia, and sleep inhibition. GW 848687X is a potent and selective EP1 receptor antagonist (IC50 = 2.5 nM).{14997} It has >400-fold selectivity for EP1 relative to the other EP receptor subtypes, the PGD2 receptor, DP1, and the prostacyclin receptor, IP. GW 848687X is a potent and selective EP1 receptor antagonist (IC50 = 2.5 nM).{14997} It has >400-fold selectivity for EP1 relative to the other EP receptor subtypes, the PGD2 receptor, DP1, and the prostacyclin receptor, IP. GW 848687X has 30-fold selectivity over the thromboxane A2 receptor, TP, acting as a functional antagonist at this receptor at higher levels.{14997} Its actions against the FP and CRTH2/DP2 receptors have not been characterized. In vivo, GW 848687X has an excellent oral pharmacokinetic profile, with oral bioavailability at 54% in rats and 53% in dogs with a half-life of two hours in both species.{14997} In a rat model of chronic inflammatory joint pain, GW 848687X shows complete anti-hyperalgesic activity with an ED50 value of 1.3 mg/kg.{14997}  

     

    Brand:
    Cayman
    SKU:10010410 - 1 mg

    Available on backorder

  • Four G protein-coupled receptors, EP1-4, initiate cellular signaling in response to prostaglandin PGE2. The receptor EP1 acts via Gαq to evoke diverse effects, including renal vasoconstriction, bronchoconstriction, hyperalgesia, allodynia, gastric protection, hyperthermia, and sleep inhibition. GW 848687X is a potent and selective EP1 receptor antagonist (IC50 = 2.5 nM).{14997} It has >400-fold selectivity for EP1 relative to the other EP receptor subtypes, the PGD2 receptor, DP1, and the prostacyclin receptor, IP. GW 848687X is a potent and selective EP1 receptor antagonist (IC50 = 2.5 nM).{14997} It has >400-fold selectivity for EP1 relative to the other EP receptor subtypes, the PGD2 receptor, DP1, and the prostacyclin receptor, IP. GW 848687X has 30-fold selectivity over the thromboxane A2 receptor, TP, acting as a functional antagonist at this receptor at higher levels.{14997} Its actions against the FP and CRTH2/DP2 receptors have not been characterized. In vivo, GW 848687X has an excellent oral pharmacokinetic profile, with oral bioavailability at 54% in rats and 53% in dogs with a half-life of two hours in both species.{14997} In a rat model of chronic inflammatory joint pain, GW 848687X shows complete anti-hyperalgesic activity with an ED50 value of 1.3 mg/kg.{14997}  

     

    Brand:
    Cayman
    SKU:10010410 - 5 mg

    Available on backorder

  • Four G protein-coupled receptors, EP1-4, initiate cellular signaling in response to prostaglandin PGE2. The receptor EP1 acts via Gαq to evoke diverse effects, including renal vasoconstriction, bronchoconstriction, hyperalgesia, allodynia, gastric protection, hyperthermia, and sleep inhibition. GW 848687X is a potent and selective EP1 receptor antagonist (IC50 = 2.5 nM).{14997} It has >400-fold selectivity for EP1 relative to the other EP receptor subtypes, the PGD2 receptor, DP1, and the prostacyclin receptor, IP. GW 848687X is a potent and selective EP1 receptor antagonist (IC50 = 2.5 nM).{14997} It has >400-fold selectivity for EP1 relative to the other EP receptor subtypes, the PGD2 receptor, DP1, and the prostacyclin receptor, IP. GW 848687X has 30-fold selectivity over the thromboxane A2 receptor, TP, acting as a functional antagonist at this receptor at higher levels.{14997} Its actions against the FP and CRTH2/DP2 receptors have not been characterized. In vivo, GW 848687X has an excellent oral pharmacokinetic profile, with oral bioavailability at 54% in rats and 53% in dogs with a half-life of two hours in both species.{14997} In a rat model of chronic inflammatory joint pain, GW 848687X shows complete anti-hyperalgesic activity with an ED50 value of 1.3 mg/kg.{14997}  

     

    Brand:
    Cayman
    SKU:10010410 - 500 µg

    Available on backorder

  • GW 856553X is a selective inhibitor of p38α and p38β MAPK (pKi = 8.1 and 7.6, respectively in isolated enzyme assays).{34614} It inhibits TNF-α production (IC50 = 31 nM) in human peripheral blood mononuclear cells.{34615} It improves survival and normalizes blood pressure in rats with hypertension induced by a high salt and fat diet.{34614} It also has positive effects on cardiac remodeling and reduces HDL, LDL, and triglycerides in rats. In a clinical trial of patients with acute myocardial infarction, GW 856553X did not reduce the risk of major ischemic cardiovascular events.{34616}  

     

    Brand:
    Cayman
    SKU:-
  • GW 856553X is a selective inhibitor of p38α and p38β MAPK (pKi = 8.1 and 7.6, respectively in isolated enzyme assays).{34614} It inhibits TNF-α production (IC50 = 31 nM) in human peripheral blood mononuclear cells.{34615} It improves survival and normalizes blood pressure in rats with hypertension induced by a high salt and fat diet.{34614} It also has positive effects on cardiac remodeling and reduces HDL, LDL, and triglycerides in rats. In a clinical trial of patients with acute myocardial infarction, GW 856553X did not reduce the risk of major ischemic cardiovascular events.{34616}  

     

    Brand:
    Cayman
    SKU:-
  • GW 856553X is a selective inhibitor of p38α and p38β MAPK (pKi = 8.1 and 7.6, respectively in isolated enzyme assays).{34614} It inhibits TNF-α production (IC50 = 31 nM) in human peripheral blood mononuclear cells.{34615} It improves survival and normalizes blood pressure in rats with hypertension induced by a high salt and fat diet.{34614} It also has positive effects on cardiac remodeling and reduces HDL, LDL, and triglycerides in rats. In a clinical trial of patients with acute myocardial infarction, GW 856553X did not reduce the risk of major ischemic cardiovascular events.{34616}  

     

    Brand:
    Cayman
    SKU:-
  • GW 856553X is a selective inhibitor of p38α and p38β MAPK (pKi = 8.1 and 7.6, respectively in isolated enzyme assays).{34614} It inhibits TNF-α production (IC50 = 31 nM) in human peripheral blood mononuclear cells.{34615} It improves survival and normalizes blood pressure in rats with hypertension induced by a high salt and fat diet.{34614} It also has positive effects on cardiac remodeling and reduces HDL, LDL, and triglycerides in rats. In a clinical trial of patients with acute myocardial infarction, GW 856553X did not reduce the risk of major ischemic cardiovascular events.{34616}  

     

    Brand:
    Cayman
    SKU:-
  • GW 9508 is a small-molecule agonist of GPR40/FFA1 (EC50 = 47.8 nM for calcium mobilization in HEK293 cells).{14194} It is selective for GPR40/FFA1 over GPR120/FFA4 (EC50 = 3,467 nM), as well as GPR43/FFA2 and GPR41/FFA3 (EC50s = >50 µM).{14194} GW 9508 potentiates glucose-stimulated and potassium chloride-mediated insulin secretion in MIN6 pancreatic β-cells but does not affect glucose-stimulated insulin secretion in primary rat or mouse islet cells.{14194} It increases phosphorylation of AMP-activated protein kinase (AMPK) and acyl-CoA carboxylase (ACC), indicating AMPK and ACC activation, and decreases hepatic lipid accumulation in a mouse model of high-cholesterol diet-induced hepatic steatosis when administered at a dose of 100 mg/kg per day for three days.{43588}  

     

    Brand:
    Cayman
    SKU:10008907 - 10 mg

    Available on backorder

  • GW 9508 is a small-molecule agonist of GPR40/FFA1 (EC50 = 47.8 nM for calcium mobilization in HEK293 cells).{14194} It is selective for GPR40/FFA1 over GPR120/FFA4 (EC50 = 3,467 nM), as well as GPR43/FFA2 and GPR41/FFA3 (EC50s = >50 µM).{14194} GW 9508 potentiates glucose-stimulated and potassium chloride-mediated insulin secretion in MIN6 pancreatic β-cells but does not affect glucose-stimulated insulin secretion in primary rat or mouse islet cells.{14194} It increases phosphorylation of AMP-activated protein kinase (AMPK) and acyl-CoA carboxylase (ACC), indicating AMPK and ACC activation, and decreases hepatic lipid accumulation in a mouse model of high-cholesterol diet-induced hepatic steatosis when administered at a dose of 100 mg/kg per day for three days.{43588}  

     

    Brand:
    Cayman
    SKU:10008907 - 100 mg

    Available on backorder

  • GW 9508 is a small-molecule agonist of GPR40/FFA1 (EC50 = 47.8 nM for calcium mobilization in HEK293 cells).{14194} It is selective for GPR40/FFA1 over GPR120/FFA4 (EC50 = 3,467 nM), as well as GPR43/FFA2 and GPR41/FFA3 (EC50s = >50 µM).{14194} GW 9508 potentiates glucose-stimulated and potassium chloride-mediated insulin secretion in MIN6 pancreatic β-cells but does not affect glucose-stimulated insulin secretion in primary rat or mouse islet cells.{14194} It increases phosphorylation of AMP-activated protein kinase (AMPK) and acyl-CoA carboxylase (ACC), indicating AMPK and ACC activation, and decreases hepatic lipid accumulation in a mouse model of high-cholesterol diet-induced hepatic steatosis when administered at a dose of 100 mg/kg per day for three days.{43588}  

     

    Brand:
    Cayman
    SKU:10008907 - 5 mg

    Available on backorder

  • GW 9508 is a small-molecule agonist of GPR40/FFA1 (EC50 = 47.8 nM for calcium mobilization in HEK293 cells).{14194} It is selective for GPR40/FFA1 over GPR120/FFA4 (EC50 = 3,467 nM), as well as GPR43/FFA2 and GPR41/FFA3 (EC50s = >50 µM).{14194} GW 9508 potentiates glucose-stimulated and potassium chloride-mediated insulin secretion in MIN6 pancreatic β-cells but does not affect glucose-stimulated insulin secretion in primary rat or mouse islet cells.{14194} It increases phosphorylation of AMP-activated protein kinase (AMPK) and acyl-CoA carboxylase (ACC), indicating AMPK and ACC activation, and decreases hepatic lipid accumulation in a mouse model of high-cholesterol diet-induced hepatic steatosis when administered at a dose of 100 mg/kg per day for three days.{43588}  

     

    Brand:
    Cayman
    SKU:10008907 - 50 mg

    Available on backorder

  • Peroxisome proliferator-activated receptor α (PPARα) is a ligand-activated transcription factor found predominantly in the liver that is involved in the regulation of lipid homeostasis.{6374,4136} Activation of PPARα results in expression of a variety of genes, particularly those involved in fatty acid β-oxidation, binding, and transport. {11955} GW 9578 is a potent agonist of PPARα that activates the murine and human receptors with EC50 values of 0.005 and 0.05 µM, respectively.{7768} GW 9578 is highly selective for PPARα compared to PPARγ and PPARδ, which it activates in murine at EC50 values of 0.15 and 2.6 µM, respectively and in human at 1.0 and 1.4 µM, respectively.{7768} GW 9578 is a potent lipid lowering agent that may reduce insulin resistance. When 0.2 mg/kg GW 9578 was given orally once daily for three days, serum total LDL cholesterol was decreased 40-60% in male Sprague-Dawely rats.{7768} Obese Zucker rats treated with 5 mg/kg GW 9578 for nine days had markedly reduced serum insulin concentrations compared to controls.{8548}  

     

    Brand:
    Cayman
    SKU:10011211 - 1 mg

    Available on backorder

  • Peroxisome proliferator-activated receptor α (PPARα) is a ligand-activated transcription factor found predominantly in the liver that is involved in the regulation of lipid homeostasis.{6374,4136} Activation of PPARα results in expression of a variety of genes, particularly those involved in fatty acid β-oxidation, binding, and transport. {11955} GW 9578 is a potent agonist of PPARα that activates the murine and human receptors with EC50 values of 0.005 and 0.05 µM, respectively.{7768} GW 9578 is highly selective for PPARα compared to PPARγ and PPARδ, which it activates in murine at EC50 values of 0.15 and 2.6 µM, respectively and in human at 1.0 and 1.4 µM, respectively.{7768} GW 9578 is a potent lipid lowering agent that may reduce insulin resistance. When 0.2 mg/kg GW 9578 was given orally once daily for three days, serum total LDL cholesterol was decreased 40-60% in male Sprague-Dawely rats.{7768} Obese Zucker rats treated with 5 mg/kg GW 9578 for nine days had markedly reduced serum insulin concentrations compared to controls.{8548}  

     

    Brand:
    Cayman
    SKU:10011211 - 10 mg

    Available on backorder

  • Peroxisome proliferator-activated receptor α (PPARα) is a ligand-activated transcription factor found predominantly in the liver that is involved in the regulation of lipid homeostasis.{6374,4136} Activation of PPARα results in expression of a variety of genes, particularly those involved in fatty acid β-oxidation, binding, and transport. {11955} GW 9578 is a potent agonist of PPARα that activates the murine and human receptors with EC50 values of 0.005 and 0.05 µM, respectively.{7768} GW 9578 is highly selective for PPARα compared to PPARγ and PPARδ, which it activates in murine at EC50 values of 0.15 and 2.6 µM, respectively and in human at 1.0 and 1.4 µM, respectively.{7768} GW 9578 is a potent lipid lowering agent that may reduce insulin resistance. When 0.2 mg/kg GW 9578 was given orally once daily for three days, serum total LDL cholesterol was decreased 40-60% in male Sprague-Dawely rats.{7768} Obese Zucker rats treated with 5 mg/kg GW 9578 for nine days had markedly reduced serum insulin concentrations compared to controls.{8548}  

     

    Brand:
    Cayman
    SKU:10011211 - 5 mg

    Available on backorder

  • Peroxisome proliferator-activated receptor α (PPARα) is a ligand-activated transcription factor found predominantly in the liver that is involved in the regulation of lipid homeostasis.{6374,4136} Activation of PPARα results in expression of a variety of genes, particularly those involved in fatty acid β-oxidation, binding, and transport. {11955} GW 9578 is a potent agonist of PPARα that activates the murine and human receptors with EC50 values of 0.005 and 0.05 µM, respectively.{7768} GW 9578 is highly selective for PPARα compared to PPARγ and PPARδ, which it activates in murine at EC50 values of 0.15 and 2.6 µM, respectively and in human at 1.0 and 1.4 µM, respectively.{7768} GW 9578 is a potent lipid lowering agent that may reduce insulin resistance. When 0.2 mg/kg GW 9578 was given orally once daily for three days, serum total LDL cholesterol was decreased 40-60% in male Sprague-Dawely rats.{7768} Obese Zucker rats treated with 5 mg/kg GW 9578 for nine days had markedly reduced serum insulin concentrations compared to controls.{8548}  

     

    Brand:
    Cayman
    SKU:10011211 - 500 µg

    Available on backorder

  • The peroxisome proliferator-activated receptor γ (PPARγ) is the nuclear receptor responsible for transducing the therapeutic activity of the thiazolidinediones. Thiazolidinediones are a group of structurally related synthetic PPARγ agonists with antidiabetic actions in vivo.{7575,8224} Rosiglitazone (BRL 49653) is a prototypical thiazolidinedione and has served as a reference compound for this class.{8241} There are many PPARγ agonists, including 15-deoxy-Δ12,14-prostaglandin J2 and azelaoyl PAF, which are naturally derived.{8461,8930} However, only a few antagonists have been reported.{8953} GW 9662 blocks the PPARγ-induced differentiation of monocytes to osteoclasts by >90% at a dose of 0.1 µM.{8953} It is therefore a much more potent antagonist than BADGE, which is another reported PPARγ antagonist.{9318}  

     

    Brand:
    Cayman
    SKU:70785 - 1 mg

    Available on backorder

  • The peroxisome proliferator-activated receptor γ (PPARγ) is the nuclear receptor responsible for transducing the therapeutic activity of the thiazolidinediones. Thiazolidinediones are a group of structurally related synthetic PPARγ agonists with antidiabetic actions in vivo.{7575,8224} Rosiglitazone (BRL 49653) is a prototypical thiazolidinedione and has served as a reference compound for this class.{8241} There are many PPARγ agonists, including 15-deoxy-Δ12,14-prostaglandin J2 and azelaoyl PAF, which are naturally derived.{8461,8930} However, only a few antagonists have been reported.{8953} GW 9662 blocks the PPARγ-induced differentiation of monocytes to osteoclasts by >90% at a dose of 0.1 µM.{8953} It is therefore a much more potent antagonist than BADGE, which is another reported PPARγ antagonist.{9318}  

     

    Brand:
    Cayman
    SKU:70785 - 10 mg

    Available on backorder

  • The peroxisome proliferator-activated receptor γ (PPARγ) is the nuclear receptor responsible for transducing the therapeutic activity of the thiazolidinediones. Thiazolidinediones are a group of structurally related synthetic PPARγ agonists with antidiabetic actions in vivo.{7575,8224} Rosiglitazone (BRL 49653) is a prototypical thiazolidinedione and has served as a reference compound for this class.{8241} There are many PPARγ agonists, including 15-deoxy-Δ12,14-prostaglandin J2 and azelaoyl PAF, which are naturally derived.{8461,8930} However, only a few antagonists have been reported.{8953} GW 9662 blocks the PPARγ-induced differentiation of monocytes to osteoclasts by >90% at a dose of 0.1 µM.{8953} It is therefore a much more potent antagonist than BADGE, which is another reported PPARγ antagonist.{9318}  

     

    Brand:
    Cayman
    SKU:70785 - 5 mg

    Available on backorder

  • The peroxisome proliferator-activated receptor γ (PPARγ) is the nuclear receptor responsible for transducing the therapeutic activity of the thiazolidinediones. Thiazolidinediones are a group of structurally related synthetic PPARγ agonists with antidiabetic actions in vivo.{7575,8224} Rosiglitazone (BRL 49653) is a prototypical thiazolidinedione and has served as a reference compound for this class.{8241} There are many PPARγ agonists, including 15-deoxy-Δ12,14-prostaglandin J2 and azelaoyl PAF, which are naturally derived.{8461,8930} However, only a few antagonists have been reported.{8953} GW 9662 blocks the PPARγ-induced differentiation of monocytes to osteoclasts by >90% at a dose of 0.1 µM.{8953} It is therefore a much more potent antagonist than BADGE, which is another reported PPARγ antagonist.{9318}  

     

    Brand:
    Cayman
    SKU:70785 - 50 mg

    Available on backorder

  • GW843682X is a reversible, cell-permeable polo-like kinase (PLK) inhibitor.{42972} It selectively inhibits Plk1 and Plk3 (IC50s = 2.2 and 9.1 nM, respectively) over PDGFR1β, VEGFR2, Aurora A, and Cdk2/cyclin A (IC50s = 160, 360, 4,800, and 7,600 nM, respectively), as well as over 30 other kinases, in a cell-free assay. GW843682X also inhibits Plk1 activity in vitro in HeLa cells (IC50 = 0.14 μM in a reporter assay using chimeric Plk1). It inhibits growth in nine cancer cell lines in a panel (IC50s = 0.11-0.7 μM) but not of PC3 human prostate cancer cells (IC50 = 6.82 µM) or non-cancerous human diploid fibroblasts (HDFs; IC50 = 6.14 μM). GW843682X inhibits growth of MES-SA human uterine sarcoma cells, as well as of the drug-resistant, P-glycoprotein-expressing MES-SA/Dx5 subline (IC50s = 0.21 and 0.21 μM, respectively). It also inhibits the growth of patient-derived leukemia cells (IC50s = 2/M cell cycle arrest and apoptosis of H460 human lung and PALL-2 and MOLM13 human leukemia cancer cells in a concentration-dependent manner.{42972,42973}  

     

    Brand:
    Cayman
    SKU:28759 - 1 mg

    Available on backorder

  • GW843682X is a reversible, cell-permeable polo-like kinase (PLK) inhibitor.{42972} It selectively inhibits Plk1 and Plk3 (IC50s = 2.2 and 9.1 nM, respectively) over PDGFR1β, VEGFR2, Aurora A, and Cdk2/cyclin A (IC50s = 160, 360, 4,800, and 7,600 nM, respectively), as well as over 30 other kinases, in a cell-free assay. GW843682X also inhibits Plk1 activity in vitro in HeLa cells (IC50 = 0.14 μM in a reporter assay using chimeric Plk1). It inhibits growth in nine cancer cell lines in a panel (IC50s = 0.11-0.7 μM) but not of PC3 human prostate cancer cells (IC50 = 6.82 µM) or non-cancerous human diploid fibroblasts (HDFs; IC50 = 6.14 μM). GW843682X inhibits growth of MES-SA human uterine sarcoma cells, as well as of the drug-resistant, P-glycoprotein-expressing MES-SA/Dx5 subline (IC50s = 0.21 and 0.21 μM, respectively). It also inhibits the growth of patient-derived leukemia cells (IC50s = 2/M cell cycle arrest and apoptosis of H460 human lung and PALL-2 and MOLM13 human leukemia cancer cells in a concentration-dependent manner.{42972,42973}  

     

    Brand:
    Cayman
    SKU:28759 - 10 mg

    Available on backorder

  • GW843682X is a reversible, cell-permeable polo-like kinase (PLK) inhibitor.{42972} It selectively inhibits Plk1 and Plk3 (IC50s = 2.2 and 9.1 nM, respectively) over PDGFR1β, VEGFR2, Aurora A, and Cdk2/cyclin A (IC50s = 160, 360, 4,800, and 7,600 nM, respectively), as well as over 30 other kinases, in a cell-free assay. GW843682X also inhibits Plk1 activity in vitro in HeLa cells (IC50 = 0.14 μM in a reporter assay using chimeric Plk1). It inhibits growth in nine cancer cell lines in a panel (IC50s = 0.11-0.7 μM) but not of PC3 human prostate cancer cells (IC50 = 6.82 µM) or non-cancerous human diploid fibroblasts (HDFs; IC50 = 6.14 μM). GW843682X inhibits growth of MES-SA human uterine sarcoma cells, as well as of the drug-resistant, P-glycoprotein-expressing MES-SA/Dx5 subline (IC50s = 0.21 and 0.21 μM, respectively). It also inhibits the growth of patient-derived leukemia cells (IC50s = 2/M cell cycle arrest and apoptosis of H460 human lung and PALL-2 and MOLM13 human leukemia cancer cells in a concentration-dependent manner.{42972,42973}  

     

    Brand:
    Cayman
    SKU:28759 - 5 mg

    Available on backorder

  • Gymnemagenin is the aglycone core of gymnemic acids A and B, triterpenoid sweetness inhibitors derived from G. sylvestre.{39213} It is used as a biomarker for the quantification of gymnemic acids in medicinal plant extracts.{39214}  

     

    Brand:
    Cayman
    SKU:11713 - 1 mg

    Available on backorder

  • Gymnemagenin is the aglycone core of gymnemic acids A and B, triterpenoid sweetness inhibitors derived from G. sylvestre.{39213} It is used as a biomarker for the quantification of gymnemic acids in medicinal plant extracts.{39214}  

     

    Brand:
    Cayman
    SKU:11713 - 5 mg

    Available on backorder

  • Gymnemagenin is the aglycone core of gymnemic acids A and B, triterpenoid sweetness inhibitors derived from G. sylvestre.{39213} It is used as a biomarker for the quantification of gymnemic acids in medicinal plant extracts.{39214}  

     

    Brand:
    Cayman
    SKU:11713 - 500 µg

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  • Gymnemic acid I is a triterpene glycoside that has been found in G. sylvestre and has antihyperglycemic activities.{45515,45513} It inhibits glucose-induced phosphorylation of serine 70 on S6 kinase (S6K1) and serine 2448 on mTOR, caspase-3 activity, and apoptosis, as well as increases autophagy in MIN-6 pancreatic β cells when used at a concentration of 5 µg/ml.{45515} Gymnemic acid I has been used as a reference compound to compare the potency of plant-derived sweet taste inhibitors.{45513}  

     

    Brand:
    Cayman
    SKU:28495 - 1 mg

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  • Gymnemic acid I is a triterpene glycoside that has been found in G. sylvestre and has antihyperglycemic activities.{45515,45513} It inhibits glucose-induced phosphorylation of serine 70 on S6 kinase (S6K1) and serine 2448 on mTOR, caspase-3 activity, and apoptosis, as well as increases autophagy in MIN-6 pancreatic β cells when used at a concentration of 5 µg/ml.{45515} Gymnemic acid I has been used as a reference compound to compare the potency of plant-derived sweet taste inhibitors.{45513}  

     

    Brand:
    Cayman
    SKU:28495 - 5 mg

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  • Gymnoascolide A is a fungal metabolite originally isolated from G. reessii that has fungicidal and vasodilatory activities.{45999,55000} It is active against the phytopathogenic fungus S. nodorum (MIC = 13 µg/ml) but not C. albicans, B. subtilis, or the ruminant pathogenic nematode H. contortus in an agar diffusion assay.{45999,55000} Gymnoascolide A (1 µM) inhibits calcium-induced contractions in isolated rat aortic rings.{55000}  

     

    Brand:
    Cayman
    SKU:28585 - 1 mg

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  • Gypenoside IX is a dammarane-type triterpene saponin that has been found in P. notoginseng.{48933} It prevents increases in inducible nitric oxide synthase (iNOS), IL-6, and TNF-α levels, as well as phosphorylation of NF-κB, IκB, p38 MAPK, and Akt, induced by LPS and TNF-α in rat C6 glial cells when used at a concentration of 25 μM.{48934} In vivo, gypenoside IX (30 mg/kg per day) reduces LPS-induced increases in NF-κB, IκB, p38 MAPK, and Akt phosphorylation in mouse brain cortex.  

     

    Brand:
    Cayman
    SKU:29705 - 10 mg

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  • Gypenoside IX is a dammarane-type triterpene saponin that has been found in P. notoginseng.{48933} It prevents increases in inducible nitric oxide synthase (iNOS), IL-6, and TNF-α levels, as well as phosphorylation of NF-κB, IκB, p38 MAPK, and Akt, induced by LPS and TNF-α in rat C6 glial cells when used at a concentration of 25 μM.{48934} In vivo, gypenoside IX (30 mg/kg per day) reduces LPS-induced increases in NF-κB, IκB, p38 MAPK, and Akt phosphorylation in mouse brain cortex.  

     

    Brand:
    Cayman
    SKU:29705 - 25 mg

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  • Gypenoside IX is a dammarane-type triterpene saponin that has been found in P. notoginseng.{48933} It prevents increases in inducible nitric oxide synthase (iNOS), IL-6, and TNF-α levels, as well as phosphorylation of NF-κB, IκB, p38 MAPK, and Akt, induced by LPS and TNF-α in rat C6 glial cells when used at a concentration of 25 μM.{48934} In vivo, gypenoside IX (30 mg/kg per day) reduces LPS-induced increases in NF-κB, IκB, p38 MAPK, and Akt phosphorylation in mouse brain cortex.  

     

    Brand:
    Cayman
    SKU:29705 - 5 mg

    Available on backorder

  • Gypenoside IX is a dammarane-type triterpene saponin that has been found in P. notoginseng.{48933} It prevents increases in inducible nitric oxide synthase (iNOS), IL-6, and TNF-α levels, as well as phosphorylation of NF-κB, IκB, p38 MAPK, and Akt, induced by LPS and TNF-α in rat C6 glial cells when used at a concentration of 25 μM.{48934} In vivo, gypenoside IX (30 mg/kg per day) reduces LPS-induced increases in NF-κB, IκB, p38 MAPK, and Akt phosphorylation in mouse brain cortex.  

     

    Brand:
    Cayman
    SKU:29705 - 50 mg

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  • Hydrogen sulfide (H2S) is a gaseous mediator which, like nitric oxide (NO), has numerous profound actions in mammalian physiology. GYY 4137 is a water-soluble, slow-releasing hydrogen sulfide (H2S) donor.{17169} When given intravenously, it demonstrates vasodilator and anti-hypertensive activity in rats, in either the acute (L-NAME-induced) or chronic (spontaneously hypertensive) hypertension models.{17169} Intravenous GYY 4137 also protects against endotoxic shock in rats, inhibiting tumor necrosis factor-α, interleukin (IL)-1β, and IL-6 production and reducing NF-κB activation, iNOS and cyclooxygenase-2 expression, and NO and prostaglandin E2 generation.{17285}  

     

    Brand:
    Cayman
    SKU:-
  • Hydrogen sulfide (H2S) is a gaseous mediator which, like nitric oxide (NO), has numerous profound actions in mammalian physiology. GYY 4137 is a water-soluble, slow-releasing hydrogen sulfide (H2S) donor.{17169} When given intravenously, it demonstrates vasodilator and anti-hypertensive activity in rats, in either the acute (L-NAME-induced) or chronic (spontaneously hypertensive) hypertension models.{17169} Intravenous GYY 4137 also protects against endotoxic shock in rats, inhibiting tumor necrosis factor-α, interleukin (IL)-1β, and IL-6 production and reducing NF-κB activation, iNOS and cyclooxygenase-2 expression, and NO and prostaglandin E2 generation.{17285}  

     

    Brand:
    Cayman
    SKU:-
  • Hydrogen sulfide (H2S) is a gaseous mediator which, like nitric oxide (NO), has numerous profound actions in mammalian physiology. GYY 4137 is a water-soluble, slow-releasing hydrogen sulfide (H2S) donor.{17169} When given intravenously, it demonstrates vasodilator and anti-hypertensive activity in rats, in either the acute (L-NAME-induced) or chronic (spontaneously hypertensive) hypertension models.{17169} Intravenous GYY 4137 also protects against endotoxic shock in rats, inhibiting tumor necrosis factor-α, interleukin (IL)-1β, and IL-6 production and reducing NF-κB activation, iNOS and cyclooxygenase-2 expression, and NO and prostaglandin E2 generation.{17285}  

     

    Brand:
    Cayman
    SKU:-
  • Hydrogen sulfide (H2S) is a gaseous mediator which, like nitric oxide (NO), has numerous profound actions in mammalian physiology. GYY 4137 is a water-soluble, slow-releasing hydrogen sulfide (H2S) donor.{17169} When given intravenously, it demonstrates vasodilator and anti-hypertensive activity in rats, in either the acute (L-NAME-induced) or chronic (spontaneously hypertensive) hypertension models.{17169} Intravenous GYY 4137 also protects against endotoxic shock in rats, inhibiting tumor necrosis factor-α, interleukin (IL)-1β, and IL-6 production and reducing NF-κB activation, iNOS and cyclooxygenase-2 expression, and NO and prostaglandin E2 generation.{17285}  

     

    Brand:
    Cayman
    SKU:-
  • GZD-824 is an orally available inhibitor of a broad spectrum of Bcr/Abl tyrosine kinase mutants including T315I (IC50s = 0.34 and 0.68 nM for wild-type Bcr/Abl and Bcr/AblT315I, respectively).{33583} It has been shown to suppress the proliferation of Bcr/Abl-positive K562 and Ku812 human chronic myelogenous leukemia cells (IC50s = 0.2 and 0.13 nM, respectively) and induce tumor regression in mouse xenograft tumor models driven by either wild-type or mutant Bcr/Abl.{33583}  

     

    Brand:
    Cayman
    SKU:21508 -

    Out of stock

  • GZD-824 is an orally available inhibitor of a broad spectrum of Bcr/Abl tyrosine kinase mutants including T315I (IC50s = 0.34 and 0.68 nM for wild-type Bcr/Abl and Bcr/AblT315I, respectively).{33583} It has been shown to suppress the proliferation of Bcr/Abl-positive K562 and Ku812 human chronic myelogenous leukemia cells (IC50s = 0.2 and 0.13 nM, respectively) and induce tumor regression in mouse xenograft tumor models driven by either wild-type or mutant Bcr/Abl.{33583}  

     

    Brand:
    Cayman
    SKU:21508 -

    Out of stock

  • GZD-824 is an orally available inhibitor of a broad spectrum of Bcr/Abl tyrosine kinase mutants including T315I (IC50s = 0.34 and 0.68 nM for wild-type Bcr/Abl and Bcr/AblT315I, respectively).{33583} It has been shown to suppress the proliferation of Bcr/Abl-positive K562 and Ku812 human chronic myelogenous leukemia cells (IC50s = 0.2 and 0.13 nM, respectively) and induce tumor regression in mouse xenograft tumor models driven by either wild-type or mutant Bcr/Abl.{33583}  

     

    Brand:
    Cayman
    SKU:21508 -

    Out of stock

  • GZD-824 is an orally available inhibitor of a broad spectrum of Bcr/Abl tyrosine kinase mutants including T315I (IC50s = 0.34 and 0.68 nM for wild-type Bcr/Abl and Bcr/AblT315I, respectively).{33583} It has been shown to suppress the proliferation of Bcr/Abl-positive K562 and Ku812 human chronic myelogenous leukemia cells (IC50s = 0.2 and 0.13 nM, respectively) and induce tumor regression in mouse xenograft tumor models driven by either wild-type or mutant Bcr/Abl.{33583}  

     

    Brand:
    Cayman
    SKU:21508 -

    Out of stock

  • H-151 is an inhibitor of stimulator of interferon genes (STING).{35390} It forms an adduct with mouse STING in serum and acts in an irreversible manner. It inhibits the type I interferon (IFN) response and reduces the phosphorylation of TBK1 and palmitoylation of human STING (hsSTING) in vitro. It also reduces increases in mouse serum levels of IFN-β and IL-6 induced by the STING agonist 10-carboxymethyl-9-acridanone (CMA).  

     

    Brand:
    Cayman
    SKU:25857 - 10 mg

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  • H-151 is an inhibitor of stimulator of interferon genes (STING).{35390} It forms an adduct with mouse STING in serum and acts in an irreversible manner. It inhibits the type I interferon (IFN) response and reduces the phosphorylation of TBK1 and palmitoylation of human STING (hsSTING) in vitro. It also reduces increases in mouse serum levels of IFN-β and IL-6 induced by the STING agonist 10-carboxymethyl-9-acridanone (CMA).  

     

    Brand:
    Cayman
    SKU:25857 - 100 mg

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  • H-151 is an inhibitor of stimulator of interferon genes (STING).{35390} It forms an adduct with mouse STING in serum and acts in an irreversible manner. It inhibits the type I interferon (IFN) response and reduces the phosphorylation of TBK1 and palmitoylation of human STING (hsSTING) in vitro. It also reduces increases in mouse serum levels of IFN-β and IL-6 induced by the STING agonist 10-carboxymethyl-9-acridanone (CMA).  

     

    Brand:
    Cayman
    SKU:25857 - 5 mg

    Available on backorder

  • H-151 is an inhibitor of stimulator of interferon genes (STING).{35390} It forms an adduct with mouse STING in serum and acts in an irreversible manner. It inhibits the type I interferon (IFN) response and reduces the phosphorylation of TBK1 and palmitoylation of human STING (hsSTING) in vitro. It also reduces increases in mouse serum levels of IFN-β and IL-6 induced by the STING agonist 10-carboxymethyl-9-acridanone (CMA).  

     

    Brand:
    Cayman
    SKU:25857 - 50 mg

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  • H-7 is a non-selective inhibitor of protein kinases (PKs; IC50s = 20, 36, 7, and 420 μM for PKC, A, G, and M, respectively).{38451} It has been widely used to characterize the functional roles of PKC in a multitude of cellular processes.{38451,38450}  

     

    Brand:
    Cayman
    SKU:21434 -

    Out of stock

  • H-7 is a non-selective inhibitor of protein kinases (PKs; IC50s = 20, 36, 7, and 420 μM for PKC, A, G, and M, respectively).{38451} It has been widely used to characterize the functional roles of PKC in a multitude of cellular processes.{38451,38450}  

     

    Brand:
    Cayman
    SKU:21434 -

    Out of stock

  • H-7 is a non-selective inhibitor of protein kinases (PKs; IC50s = 20, 36, 7, and 420 μM for PKC, A, G, and M, respectively).{38451} It has been widely used to characterize the functional roles of PKC in a multitude of cellular processes.{38451,38450}  

     

    Brand:
    Cayman
    SKU:21434 -

    Out of stock

  • H-7 is a non-selective inhibitor of protein kinases (PKs; IC50s = 20, 36, 7, and 420 μM for PKC, A, G, and M, respectively).{38451} It has been widely used to characterize the functional roles of PKC in a multitude of cellular processes.{38451,38450}  

     

    Brand:
    Cayman
    SKU:21434 -

    Out of stock

  • The H series isoquinolinesulfonamide protein kinase (PK) inhibitors are widely used to block signaling pathways to elucidate mechanisms of cellular regulation and signal transduction. H-8, an isoquinolinesulfonamide protein kinase (PK) inhibitor, is a potent inhibitor of PKA and PKG and shows moderate inhibition for PKC and MLCK with Ki values of 1.2, 0.48, 15, and 68 µM, respectively.{16039,16079,16080} H-8 can disrupt transcriptional elongation by inhibiting cyclin C/Cdk8 and cyclin H/Cdk7/p36 CTD kinase activity with IC50 values of 47 and 6.2 µM, respectively.{15207}  

     

    Brand:
    Cayman
    SKU:10010249 - 10 mg

    Available on backorder

  • The H series isoquinolinesulfonamide protein kinase (PK) inhibitors are widely used to block signaling pathways to elucidate mechanisms of cellular regulation and signal transduction. H-8, an isoquinolinesulfonamide protein kinase (PK) inhibitor, is a potent inhibitor of PKA and PKG and shows moderate inhibition for PKC and MLCK with Ki values of 1.2, 0.48, 15, and 68 µM, respectively.{16039,16079,16080} H-8 can disrupt transcriptional elongation by inhibiting cyclin C/Cdk8 and cyclin H/Cdk7/p36 CTD kinase activity with IC50 values of 47 and 6.2 µM, respectively.{15207}  

     

    Brand:
    Cayman
    SKU:10010249 - 25 mg

    Available on backorder

  • The H series isoquinolinesulfonamide protein kinase (PK) inhibitors are widely used to block signaling pathways to elucidate mechanisms of cellular regulation and signal transduction. H-8, an isoquinolinesulfonamide protein kinase (PK) inhibitor, is a potent inhibitor of PKA and PKG and shows moderate inhibition for PKC and MLCK with Ki values of 1.2, 0.48, 15, and 68 µM, respectively.{16039,16079,16080} H-8 can disrupt transcriptional elongation by inhibiting cyclin C/Cdk8 and cyclin H/Cdk7/p36 CTD kinase activity with IC50 values of 47 and 6.2 µM, respectively.{15207}  

     

    Brand:
    Cayman
    SKU:10010249 - 5 mg

    Available on backorder

  • The H series isoquinolinesulfonamide protein kinase (PK) inhibitors are widely used to block signaling pathways to elucidate mechanisms of cellular regulation and signal transduction. H-8, an isoquinolinesulfonamide protein kinase (PK) inhibitor, is a potent inhibitor of PKA and PKG and shows moderate inhibition for PKC and MLCK with Ki values of 1.2, 0.48, 15, and 68 µM, respectively.{16039,16079,16080} H-8 can disrupt transcriptional elongation by inhibiting cyclin C/Cdk8 and cyclin H/Cdk7/p36 CTD kinase activity with IC50 values of 47 and 6.2 µM, respectively.{15207}  

     

    Brand:
    Cayman
    SKU:10010249 - 50 mg

    Available on backorder