Chemicals

Showing 13351–13500 of 41137 results

  • Anti-diabetic drugs of the thiazolidinedione (TZD) structural class as well as α-lipoic acid activate peroxisome proliferator-activated receptor γ (PPARγ), a nuclear transcription factor that controls glucose metabolism and lipid homeostasis. CAY10506 is a hybrid lipoic acid-TZD derivative that transactivates human PPARγ with an EC50 value of 10 µM.{14244}  

     

    Brand:
    Cayman
    SKU:10009079 - 50 mg

    Available on backorder

  • Central cannabinoid (CB1) receptor antagonists and inverse agonists exhibit therapeutic potential for obesity and drug dependence, while being devoid of psychotropic effects. CAY10508 is a potent and selective central cannabinoid (CB1) receptor inverse agonist with a Ki value of 243 nM and an EC50 of 195 nM.{14135} A 10 µM concentration of CAY10508 resulted in 100% and 35% displacement of [3H]-CP-55,940 at the CB1 and peripheral cannabinoid (CB2) receptors, respectively. A [35S]-GTPγS binding assay revealed the inverse agonist properties of CAY10508 at the CB1 receptor.  

     

    Brand:
    Cayman
    SKU:10008669 - 10 mg

    Available on backorder

  • Central cannabinoid (CB1) receptor antagonists and inverse agonists exhibit therapeutic potential for obesity and drug dependence, while being devoid of psychotropic effects. CAY10508 is a potent and selective central cannabinoid (CB1) receptor inverse agonist with a Ki value of 243 nM and an EC50 of 195 nM.{14135} A 10 µM concentration of CAY10508 resulted in 100% and 35% displacement of [3H]-CP-55,940 at the CB1 and peripheral cannabinoid (CB2) receptors, respectively. A [35S]-GTPγS binding assay revealed the inverse agonist properties of CAY10508 at the CB1 receptor.  

     

    Brand:
    Cayman
    SKU:10008669 - 25 mg

    Available on backorder

  • Central cannabinoid (CB1) receptor antagonists and inverse agonists exhibit therapeutic potential for obesity and drug dependence, while being devoid of psychotropic effects. CAY10508 is a potent and selective central cannabinoid (CB1) receptor inverse agonist with a Ki value of 243 nM and an EC50 of 195 nM.{14135} A 10 µM concentration of CAY10508 resulted in 100% and 35% displacement of [3H]-CP-55,940 at the CB1 and peripheral cannabinoid (CB2) receptors, respectively. A [35S]-GTPγS binding assay revealed the inverse agonist properties of CAY10508 at the CB1 receptor.  

     

    Brand:
    Cayman
    SKU:10008669 - 5 mg

    Available on backorder

  • Central cannabinoid (CB1) receptor antagonists and inverse agonists exhibit therapeutic potential for obesity and drug dependence, while being devoid of psychotropic effects. CAY10508 is a potent and selective central cannabinoid (CB1) receptor inverse agonist with a Ki value of 243 nM and an EC50 of 195 nM.{14135} A 10 µM concentration of CAY10508 resulted in 100% and 35% displacement of [3H]-CP-55,940 at the CB1 and peripheral cannabinoid (CB2) receptors, respectively. A [35S]-GTPγS binding assay revealed the inverse agonist properties of CAY10508 at the CB1 receptor.  

     

    Brand:
    Cayman
    SKU:10008669 - 50 mg

    Available on backorder

  • The actions of many clinical prostaglandins, including those used for estrous synchronization and for reduction of intraocular pressure, are mediated through the FP receptor.{2959} CAY10509 is an analog of PGF2α containing a thio-fluorobenzene substituent in the lower side chain. CAY10509 has an IC50 of about 30 nM when tested for binding to the recombinant human FP receptor.{14404}  

     

    Brand:
    Cayman
    SKU:10009167 - 1 mg

    Available on backorder

  • The actions of many clinical prostaglandins, including those used for estrous synchronization and for reduction of intraocular pressure, are mediated through the FP receptor.{2959} CAY10509 is an analog of PGF2α containing a thio-fluorobenzene substituent in the lower side chain. CAY10509 has an IC50 of about 30 nM when tested for binding to the recombinant human FP receptor.{14404}  

     

    Brand:
    Cayman
    SKU:10009167 - 100 µg

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  • The actions of many clinical prostaglandins, including those used for estrous synchronization and for reduction of intraocular pressure, are mediated through the FP receptor.{2959} CAY10509 is an analog of PGF2α containing a thio-fluorobenzene substituent in the lower side chain. CAY10509 has an IC50 of about 30 nM when tested for binding to the recombinant human FP receptor.{14404}  

     

    Brand:
    Cayman
    SKU:10009167 - 5 mg

    Available on backorder

  • The actions of many clinical prostaglandins, including those used for estrous synchronization and for reduction of intraocular pressure, are mediated through the FP receptor.{2959} CAY10509 is an analog of PGF2α containing a thio-fluorobenzene substituent in the lower side chain. CAY10509 has an IC50 of about 30 nM when tested for binding to the recombinant human FP receptor.{14404}  

     

    Brand:
    Cayman
    SKU:10009167 - 500 µg

    Available on backorder

  • The actions of many clinical prostaglandins, including those used for estrous synchronization and for reduction of intraocular pressure, are mediated through the FP receptor.{2959} CAY10510 is an analog of PGF2α containing an acetylenic fluorobenzene substituent in the lower side chain. CAY10510 has an IC50 of 0.5 µM when tested for binding to the recombinant human FP receptor.{14404}  

     

    Brand:
    Cayman
    SKU:10009168 - 1 mg

    Available on backorder

  • The actions of many clinical prostaglandins, including those used for estrous synchronization and for reduction of intraocular pressure, are mediated through the FP receptor.{2959} CAY10510 is an analog of PGF2α containing an acetylenic fluorobenzene substituent in the lower side chain. CAY10510 has an IC50 of 0.5 µM when tested for binding to the recombinant human FP receptor.{14404}  

     

    Brand:
    Cayman
    SKU:10009168 - 100 µg

    Available on backorder

  • The actions of many clinical prostaglandins, including those used for estrous synchronization and for reduction of intraocular pressure, are mediated through the FP receptor.{2959} CAY10510 is an analog of PGF2α containing an acetylenic fluorobenzene substituent in the lower side chain. CAY10510 has an IC50 of 0.5 µM when tested for binding to the recombinant human FP receptor.{14404}  

     

    Brand:
    Cayman
    SKU:10009168 - 5 mg

    Available on backorder

  • The actions of many clinical prostaglandins, including those used for estrous synchronization and for reduction of intraocular pressure, are mediated through the FP receptor.{2959} CAY10510 is an analog of PGF2α containing an acetylenic fluorobenzene substituent in the lower side chain. CAY10510 has an IC50 of 0.5 µM when tested for binding to the recombinant human FP receptor.{14404}  

     

    Brand:
    Cayman
    SKU:10009168 - 500 µg

    Available on backorder

  • The nuclear factor-κB (NF-κB) regulates the expression of numerous genes involved in immunity and inflammation, cellular stress responses, growth, and apoptosis. Resveratrol, a polyphenolic trans-stilbene, is a known inhibitor of the activation of NF-κB and exhibits activity against a wide variety of cancer cells. CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}  

     

    Brand:
    Cayman
    SKU:10009536 - 10 mg

    Available on backorder

  • The nuclear factor-κB (NF-κB) regulates the expression of numerous genes involved in immunity and inflammation, cellular stress responses, growth, and apoptosis. Resveratrol, a polyphenolic trans-stilbene, is a known inhibitor of the activation of NF-κB and exhibits activity against a wide variety of cancer cells. CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}  

     

    Brand:
    Cayman
    SKU:10009536 - 100 mg

    Available on backorder

  • The nuclear factor-κB (NF-κB) regulates the expression of numerous genes involved in immunity and inflammation, cellular stress responses, growth, and apoptosis. Resveratrol, a polyphenolic trans-stilbene, is a known inhibitor of the activation of NF-κB and exhibits activity against a wide variety of cancer cells. CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}  

     

    Brand:
    Cayman
    SKU:10009536 - 50 mg

    Available on backorder

  • The nuclear factor-κB (NF-κB) regulates the expression of numerous genes involved in immunity and inflammation, cellular stress responses, growth, and apoptosis. Resveratrol, a polyphenolic trans-stilbene, is a known inhibitor of the activation of NF-κB and exhibits activity against a wide variety of cancer cells. CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}  

     

    Brand:
    Cayman
    SKU:10009536 - 500 mg

    Available on backorder

  • CAY10514 is an aromatic analog of 8(S)-HETE. It acts as a dual agonist of PPARα and PPARγ with EC50 values of 0.173 and 0.642 µM, respectively.{14310}  

     

    Brand:
    Cayman
    SKU:10009017 - 1 mg

    Available on backorder

  • CAY10514 is an aromatic analog of 8(S)-HETE. It acts as a dual agonist of PPARα and PPARγ with EC50 values of 0.173 and 0.642 µM, respectively.{14310}  

     

    Brand:
    Cayman
    SKU:10009017 - 10 mg

    Available on backorder

  • CAY10514 is an aromatic analog of 8(S)-HETE. It acts as a dual agonist of PPARα and PPARγ with EC50 values of 0.173 and 0.642 µM, respectively.{14310}  

     

    Brand:
    Cayman
    SKU:10009017 - 5 mg

    Available on backorder

  • CAY10514 is an aromatic analog of 8(S)-HETE. It acts as a dual agonist of PPARα and PPARγ with EC50 values of 0.173 and 0.642 µM, respectively.{14310}  

     

    Brand:
    Cayman
    SKU:10009017 - 50 mg

    Available on backorder

  • Prostaglandin E2 (PGE2) is the major PG synthesized at sites of inflammation and plays an important role in different inflammatory diseases. It acts as a mediator of pain and inflammation and promotes bone destruction. The increased synthesis of PGE2 during inflammation can be accounted for by increased expression of both cyclooxygenase-2 (COX-2) and microsomal PGE synthase-1 (mPGES-1).{11266,12923,11537} CAY10526 is an inhibitor of PGE2 production through the selective modulation of mPGES-1 expression. It dose-dependently inhibits PGE2 production in lipopolysaccharide-stimulated RAW 264.7 cells with an IC50 value of 1.8 µM without any effect on COX-2 expression.{14793}  

     

    Brand:
    Cayman
    SKU:10010088 - 1 mg

    Available on backorder

  • Prostaglandin E2 (PGE2) is the major PG synthesized at sites of inflammation and plays an important role in different inflammatory diseases. It acts as a mediator of pain and inflammation and promotes bone destruction. The increased synthesis of PGE2 during inflammation can be accounted for by increased expression of both cyclooxygenase-2 (COX-2) and microsomal PGE synthase-1 (mPGES-1).{11266,12923,11537} CAY10526 is an inhibitor of PGE2 production through the selective modulation of mPGES-1 expression. It dose-dependently inhibits PGE2 production in lipopolysaccharide-stimulated RAW 264.7 cells with an IC50 value of 1.8 µM without any effect on COX-2 expression.{14793}  

     

    Brand:
    Cayman
    SKU:10010088 - 10 mg

    Available on backorder

  • Prostaglandin E2 (PGE2) is the major PG synthesized at sites of inflammation and plays an important role in different inflammatory diseases. It acts as a mediator of pain and inflammation and promotes bone destruction. The increased synthesis of PGE2 during inflammation can be accounted for by increased expression of both cyclooxygenase-2 (COX-2) and microsomal PGE synthase-1 (mPGES-1).{11266,12923,11537} CAY10526 is an inhibitor of PGE2 production through the selective modulation of mPGES-1 expression. It dose-dependently inhibits PGE2 production in lipopolysaccharide-stimulated RAW 264.7 cells with an IC50 value of 1.8 µM without any effect on COX-2 expression.{14793}  

     

    Brand:
    Cayman
    SKU:10010088 - 5 mg

    Available on backorder

  • TPα and TPβ are two isoforms of the human TP receptor, the G protein-coupled receptor (GPCR) that mediates the actions of thromboxane A2 (TXA2). Although their distinct physiological functions have not been fully elucidated, TPβ is believed to be responsible for vascular endothelial growth factor-induced endothelial cell differentiation and migration whereas TPα appears to be the predominant isoform expressed in platelets. CAY10535 is a TP receptor antagonist that shows ~20-fold selectivity for TPβ (IC50 = 99 nM) relative to TPα (IC50 = 1,970 nM) in the inhibition of U46619-mediated Ca2+ mobilization. This compound exhibits relatively poor activity on platelets (IC50 = 985 nM) when inhibiting U-46619-induced platelet aggregation.{14983}  

     

    Brand:
    Cayman
    SKU:10010396 - 1 mg

    Available on backorder

  • TPα and TPβ are two isoforms of the human TP receptor, the G protein-coupled receptor (GPCR) that mediates the actions of thromboxane A2 (TXA2). Although their distinct physiological functions have not been fully elucidated, TPβ is believed to be responsible for vascular endothelial growth factor-induced endothelial cell differentiation and migration whereas TPα appears to be the predominant isoform expressed in platelets. CAY10535 is a TP receptor antagonist that shows ~20-fold selectivity for TPβ (IC50 = 99 nM) relative to TPα (IC50 = 1,970 nM) in the inhibition of U46619-mediated Ca2+ mobilization. This compound exhibits relatively poor activity on platelets (IC50 = 985 nM) when inhibiting U-46619-induced platelet aggregation.{14983}  

     

    Brand:
    Cayman
    SKU:10010396 - 10 mg

    Available on backorder

  • TPα and TPβ are two isoforms of the human TP receptor, the G protein-coupled receptor (GPCR) that mediates the actions of thromboxane A2 (TXA2). Although their distinct physiological functions have not been fully elucidated, TPβ is believed to be responsible for vascular endothelial growth factor-induced endothelial cell differentiation and migration whereas TPα appears to be the predominant isoform expressed in platelets. CAY10535 is a TP receptor antagonist that shows ~20-fold selectivity for TPβ (IC50 = 99 nM) relative to TPα (IC50 = 1,970 nM) in the inhibition of U46619-mediated Ca2+ mobilization. This compound exhibits relatively poor activity on platelets (IC50 = 985 nM) when inhibiting U-46619-induced platelet aggregation.{14983}  

     

    Brand:
    Cayman
    SKU:10010396 - 5 mg

    Available on backorder

  • TPα and TPβ are two isoforms of the human TP receptor, the G protein-coupled receptor (GPCR) that mediates the actions of thromboxane A2 (TXA2). Although their distinct physiological functions have not been fully elucidated, TPβ is believed to be responsible for vascular endothelial growth factor-induced endothelial cell differentiation and migration whereas TPα appears to be the predominant isoform expressed in platelets. CAY10535 is a TP receptor antagonist that shows ~20-fold selectivity for TPβ (IC50 = 99 nM) relative to TPα (IC50 = 1,970 nM) in the inhibition of U46619-mediated Ca2+ mobilization. This compound exhibits relatively poor activity on platelets (IC50 = 985 nM) when inhibiting U-46619-induced platelet aggregation.{14983}  

     

    Brand:
    Cayman
    SKU:10010396 - 50 mg

    Available on backorder

  • Cellular prion protein (PrPc) is a cell surface glycoprotein expressed in brain, spinal cord, and several peripheral tissues that if mutated to the protease-resistant isoform PrPSc (scrapie PrP, PrPres) can result in one of several fatal neurodegenerative diseases.{10289} Prion diseases, including mad cow disease (bovine spongiform encephalopathy), scrapie, and Creutzfeldt-Jakob disease develop from the accumulation of PrPSc, an abnormally folded β-rich conformation of PrPc.{11676,7171} CAY10550 is a potent antiprion compound that inhibits the accumulation of PrPc with an IC50 value of 3 nM in both ScN2a and F3 prion-infected mouse neuroblastoma cell lines.{15077} This compound also demonstrates moderate radical scavenging activity as it inhibits the formation of hydroxyl radicals in vitro with an IC50 value of 90 µM.{15077}  

     

    Brand:
    Cayman
    SKU:10010740 - 1 mg

    Available on backorder

  • Cellular prion protein (PrPc) is a cell surface glycoprotein expressed in brain, spinal cord, and several peripheral tissues that if mutated to the protease-resistant isoform PrPSc (scrapie PrP, PrPres) can result in one of several fatal neurodegenerative diseases.{10289} Prion diseases, including mad cow disease (bovine spongiform encephalopathy), scrapie, and Creutzfeldt-Jakob disease develop from the accumulation of PrPSc, an abnormally folded β-rich conformation of PrPc.{11676,7171} CAY10550 is a potent antiprion compound that inhibits the accumulation of PrPc with an IC50 value of 3 nM in both ScN2a and F3 prion-infected mouse neuroblastoma cell lines.{15077} This compound also demonstrates moderate radical scavenging activity as it inhibits the formation of hydroxyl radicals in vitro with an IC50 value of 90 µM.{15077}  

     

    Brand:
    Cayman
    SKU:10010740 - 10 mg

    Available on backorder

  • Cellular prion protein (PrPc) is a cell surface glycoprotein expressed in brain, spinal cord, and several peripheral tissues that if mutated to the protease-resistant isoform PrPSc (scrapie PrP, PrPres) can result in one of several fatal neurodegenerative diseases.{10289} Prion diseases, including mad cow disease (bovine spongiform encephalopathy), scrapie, and Creutzfeldt-Jakob disease develop from the accumulation of PrPSc, an abnormally folded β-rich conformation of PrPc.{11676,7171} CAY10550 is a potent antiprion compound that inhibits the accumulation of PrPc with an IC50 value of 3 nM in both ScN2a and F3 prion-infected mouse neuroblastoma cell lines.{15077} This compound also demonstrates moderate radical scavenging activity as it inhibits the formation of hydroxyl radicals in vitro with an IC50 value of 90 µM.{15077}  

     

    Brand:
    Cayman
    SKU:10010740 - 25 mg

    Available on backorder

  • Cellular prion protein (PrPc) is a cell surface glycoprotein expressed in brain, spinal cord, and several peripheral tissues that if mutated to the protease-resistant isoform PrPSc (scrapie PrP, PrPres) can result in one of several fatal neurodegenerative diseases.{10289} Prion diseases, including mad cow disease (bovine spongiform encephalopathy), scrapie, and Creutzfeldt-Jakob disease develop from the accumulation of PrPSc, an abnormally folded β-rich conformation of PrPc.{11676,7171} CAY10550 is a potent antiprion compound that inhibits the accumulation of PrPc with an IC50 value of 3 nM in both ScN2a and F3 prion-infected mouse neuroblastoma cell lines.{15077} This compound also demonstrates moderate radical scavenging activity as it inhibits the formation of hydroxyl radicals in vitro with an IC50 value of 90 µM.{15077}  

     

    Brand:
    Cayman
    SKU:10010740 - 5 mg

    Available on backorder

  • Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression and are therefore promising therapeutic targets for cancer and neurodegenerative diseases. Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression and are therefore promising therapeutic targets for cancer and neurodegenerative diseases. CAY10554 is a potent inhibitor of Cdk5 and Cdk2, with IC50 values of 64 and 98 nM, respectively.{15079}  

     

    Brand:
    Cayman
    SKU:10010301 - 10 mg

    Available on backorder

  • Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression and are therefore promising therapeutic targets for cancer and neurodegenerative diseases. Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression and are therefore promising therapeutic targets for cancer and neurodegenerative diseases. CAY10554 is a potent inhibitor of Cdk5 and Cdk2, with IC50 values of 64 and 98 nM, respectively.{15079}  

     

    Brand:
    Cayman
    SKU:10010301 - 25 mg

    Available on backorder

  • Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression and are therefore promising therapeutic targets for cancer and neurodegenerative diseases. Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression and are therefore promising therapeutic targets for cancer and neurodegenerative diseases. CAY10554 is a potent inhibitor of Cdk5 and Cdk2, with IC50 values of 64 and 98 nM, respectively.{15079}  

     

    Brand:
    Cayman
    SKU:10010301 - 5 mg

    Available on backorder

  • Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression and are therefore promising therapeutic targets for cancer and neurodegenerative diseases. Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression and are therefore promising therapeutic targets for cancer and neurodegenerative diseases. CAY10554 is a potent inhibitor of Cdk5 and Cdk2, with IC50 values of 64 and 98 nM, respectively.{15079}  

     

    Brand:
    Cayman
    SKU:10010301 - 50 mg

    Available on backorder

  • The extracellular signal-regulated kinase (ERK) signal transduction pathway regulates a diverse array of cellular processes. These processes include cell survival, proliferation, motility, and differentiation and are constitutively activated in cancers involving lung, colon, pancreas, kidney, and ovary.{15420} CAY10561 is a potent, ATP-competitive inhibitor of ERK2 (Ki = 2 nM).{14786} This compound is highly selective for ERK2 compared to other kinases such as PKA (Ki = 0.39 µM) and JNK3 (Ki = 4 µM).{14786} CAY10561 inhibits proliferation of COLO 205 cells with an IC50 value of 0.54 µM.{14786}  

     

    Brand:
    Cayman
    SKU:10010043 - 1 mg

    Available on backorder

  • The extracellular signal-regulated kinase (ERK) signal transduction pathway regulates a diverse array of cellular processes. These processes include cell survival, proliferation, motility, and differentiation and are constitutively activated in cancers involving lung, colon, pancreas, kidney, and ovary.{15420} CAY10561 is a potent, ATP-competitive inhibitor of ERK2 (Ki = 2 nM).{14786} This compound is highly selective for ERK2 compared to other kinases such as PKA (Ki = 0.39 µM) and JNK3 (Ki = 4 µM).{14786} CAY10561 inhibits proliferation of COLO 205 cells with an IC50 value of 0.54 µM.{14786}  

     

    Brand:
    Cayman
    SKU:10010043 - 10 mg

    Available on backorder

  • The extracellular signal-regulated kinase (ERK) signal transduction pathway regulates a diverse array of cellular processes. These processes include cell survival, proliferation, motility, and differentiation and are constitutively activated in cancers involving lung, colon, pancreas, kidney, and ovary.{15420} CAY10561 is a potent, ATP-competitive inhibitor of ERK2 (Ki = 2 nM).{14786} This compound is highly selective for ERK2 compared to other kinases such as PKA (Ki = 0.39 µM) and JNK3 (Ki = 4 µM).{14786} CAY10561 inhibits proliferation of COLO 205 cells with an IC50 value of 0.54 µM.{14786}  

     

    Brand:
    Cayman
    SKU:10010043 - 5 mg

    Available on backorder

  • The extracellular signal-regulated kinase (ERK) signal transduction pathway regulates a diverse array of cellular processes. These processes include cell survival, proliferation, motility, and differentiation and are constitutively activated in cancers involving lung, colon, pancreas, kidney, and ovary.{15420} CAY10561 is a potent, ATP-competitive inhibitor of ERK2 (Ki = 2 nM).{14786} This compound is highly selective for ERK2 compared to other kinases such as PKA (Ki = 0.39 µM) and JNK3 (Ki = 4 µM).{14786} CAY10561 inhibits proliferation of COLO 205 cells with an IC50 value of 0.54 µM.{14786}  

     

    Brand:
    Cayman
    SKU:10010043 - 500 µg

    Available on backorder

  • Stearoyl-CoA desaturase (SCD) catalyzes the committed step of the conversion of saturated, long-chain fatty acids to monounsaturated fatty acids. The SCD1 gene is thought to play a key role in lipid homeostasis and body weight regulation.{9969,16127,15602} Thus, modulating SCD1 activity pharmacologically may be a useful tool for regulating type 2 diabetes, dyslipidemia, and obesity. CAY10566 is a potent and selective inhibitor of SCD1 that demonstrates IC50 values of 4.5 and 26 nM in mouse and human enzymatic assays, respectively.{15724} This compound inhibits the conversion of saturated, long-chain fatty acyl-CoAs to monounsaturated, long-chain fatty acyl-CoAs in HepG2 cells with IC50 values of 7.9 and 6.8 nM, respectively, when heptadecanoic acid and palmitic acid are used as the substrate.{15724}  

     

    Brand:
    Cayman
    SKU:10012562 - 1 mg

    Available on backorder

  • Stearoyl-CoA desaturase (SCD) catalyzes the committed step of the conversion of saturated, long-chain fatty acids to monounsaturated fatty acids. The SCD1 gene is thought to play a key role in lipid homeostasis and body weight regulation.{9969,16127,15602} Thus, modulating SCD1 activity pharmacologically may be a useful tool for regulating type 2 diabetes, dyslipidemia, and obesity. CAY10566 is a potent and selective inhibitor of SCD1 that demonstrates IC50 values of 4.5 and 26 nM in mouse and human enzymatic assays, respectively.{15724} This compound inhibits the conversion of saturated, long-chain fatty acyl-CoAs to monounsaturated, long-chain fatty acyl-CoAs in HepG2 cells with IC50 values of 7.9 and 6.8 nM, respectively, when heptadecanoic acid and palmitic acid are used as the substrate.{15724}  

     

    Brand:
    Cayman
    SKU:10012562 - 10 mg

    Available on backorder

  • Stearoyl-CoA desaturase (SCD) catalyzes the committed step of the conversion of saturated, long-chain fatty acids to monounsaturated fatty acids. The SCD1 gene is thought to play a key role in lipid homeostasis and body weight regulation.{9969,16127,15602} Thus, modulating SCD1 activity pharmacologically may be a useful tool for regulating type 2 diabetes, dyslipidemia, and obesity. CAY10566 is a potent and selective inhibitor of SCD1 that demonstrates IC50 values of 4.5 and 26 nM in mouse and human enzymatic assays, respectively.{15724} This compound inhibits the conversion of saturated, long-chain fatty acyl-CoAs to monounsaturated, long-chain fatty acyl-CoAs in HepG2 cells with IC50 values of 7.9 and 6.8 nM, respectively, when heptadecanoic acid and palmitic acid are used as the substrate.{15724}  

     

    Brand:
    Cayman
    SKU:10012562 - 25 mg

    Available on backorder

  • Stearoyl-CoA desaturase (SCD) catalyzes the committed step of the conversion of saturated, long-chain fatty acids to monounsaturated fatty acids. The SCD1 gene is thought to play a key role in lipid homeostasis and body weight regulation.{9969,16127,15602} Thus, modulating SCD1 activity pharmacologically may be a useful tool for regulating type 2 diabetes, dyslipidemia, and obesity. CAY10566 is a potent and selective inhibitor of SCD1 that demonstrates IC50 values of 4.5 and 26 nM in mouse and human enzymatic assays, respectively.{15724} This compound inhibits the conversion of saturated, long-chain fatty acyl-CoAs to monounsaturated, long-chain fatty acyl-CoAs in HepG2 cells with IC50 values of 7.9 and 6.8 nM, respectively, when heptadecanoic acid and palmitic acid are used as the substrate.{15724}  

     

    Brand:
    Cayman
    SKU:10012562 - 5 mg

    Available on backorder

  • Akt1, 2, and 3 are serine/threonine protein kinases in the phosphatidylinositol 3 (PI3)-kinase signalling pathway that play a critical role in the regulation of cell proliferation and survival.{12235,13740} Following recruitment of Akt to the plasma membrane, phosphorylation at threonine 308 and serine 473 (Akt1 numbering) by phosphoinositide-dependent kinases (PDK) 1 and 2 results in full activation of the enzyme. CAY10567 is an Akt1 translocation inhibitor. At a concentration of 12.5 µM, it prevents the translocation of Akt1 by apparently compromising the function of the PH domain. A structurally similar compound inhibits kinase activity in vitro with an EC50 value of 12 µM by binding to the kinase domain.{15664} CAY10567 also inhibits hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase (RdRp) with an IC50 value of 79 µM. {15663}  

     

    Brand:
    Cayman
    SKU:-
  • Akt1, 2, and 3 are serine/threonine protein kinases in the phosphatidylinositol 3 (PI3)-kinase signalling pathway that play a critical role in the regulation of cell proliferation and survival.{12235,13740} Following recruitment of Akt to the plasma membrane, phosphorylation at threonine 308 and serine 473 (Akt1 numbering) by phosphoinositide-dependent kinases (PDK) 1 and 2 results in full activation of the enzyme. CAY10567 is an Akt1 translocation inhibitor. At a concentration of 12.5 µM, it prevents the translocation of Akt1 by apparently compromising the function of the PH domain. A structurally similar compound inhibits kinase activity in vitro with an EC50 value of 12 µM by binding to the kinase domain.{15664} CAY10567 also inhibits hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase (RdRp) with an IC50 value of 79 µM. {15663}  

     

    Brand:
    Cayman
    SKU:10010233 - 1 g

    Available on backorder

  • Akt1, 2, and 3 are serine/threonine protein kinases in the phosphatidylinositol 3 (PI3)-kinase signalling pathway that play a critical role in the regulation of cell proliferation and survival.{12235,13740} Following recruitment of Akt to the plasma membrane, phosphorylation at threonine 308 and serine 473 (Akt1 numbering) by phosphoinositide-dependent kinases (PDK) 1 and 2 results in full activation of the enzyme. CAY10567 is an Akt1 translocation inhibitor. At a concentration of 12.5 µM, it prevents the translocation of Akt1 by apparently compromising the function of the PH domain. A structurally similar compound inhibits kinase activity in vitro with an EC50 value of 12 µM by binding to the kinase domain.{15664} CAY10567 also inhibits hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase (RdRp) with an IC50 value of 79 µM. {15663}  

     

    Brand:
    Cayman
    SKU:10010233 - 100 mg

    Available on backorder

  • Akt1, 2, and 3 are serine/threonine protein kinases in the phosphatidylinositol 3 (PI3)-kinase signalling pathway that play a critical role in the regulation of cell proliferation and survival.{12235,13740} Following recruitment of Akt to the plasma membrane, phosphorylation at threonine 308 and serine 473 (Akt1 numbering) by phosphoinositide-dependent kinases (PDK) 1 and 2 results in full activation of the enzyme. CAY10567 is an Akt1 translocation inhibitor. At a concentration of 12.5 µM, it prevents the translocation of Akt1 by apparently compromising the function of the PH domain. A structurally similar compound inhibits kinase activity in vitro with an EC50 value of 12 µM by binding to the kinase domain.{15664} CAY10567 also inhibits hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase (RdRp) with an IC50 value of 79 µM. {15663}  

     

    Brand:
    Cayman
    SKU:10010233 - 250 mg

    Available on backorder

  • Akt1, 2, and 3 are serine/threonine protein kinases in the phosphatidylinositol 3 (PI3)-kinase signalling pathway that play a critical role in the regulation of cell proliferation and survival.{12235,13740} Following recruitment of Akt to the plasma membrane, phosphorylation at threonine 308 and serine 473 (Akt1 numbering) by phosphoinositide-dependent kinases (PDK) 1 and 2 results in full activation of the enzyme. CAY10567 is an Akt1 translocation inhibitor. At a concentration of 12.5 µM, it prevents the translocation of Akt1 by apparently compromising the function of the PH domain. A structurally similar compound inhibits kinase activity in vitro with an EC50 value of 12 µM by binding to the kinase domain.{15664} CAY10567 also inhibits hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase (RdRp) with an IC50 value of 79 µM. {15663}  

     

    Brand:
    Cayman
    SKU:-
  • Akt1, 2, and 3 are serine/threonine protein kinases in the phosphatidylinositol 3 (PI3)-kinase signalling pathway that play a critical role in the regulation of cell proliferation and survival.{12235,13740} Following recruitment of Akt to the plasma membrane, phosphorylation at threonine 308 and serine 473 (Akt1 numbering) by phosphoinositide-dependent kinases (PDK) 1 and 2 results in full activation of the enzyme. CAY10567 is an Akt1 translocation inhibitor. At a concentration of 12.5 µM, it prevents the translocation of Akt1 by apparently compromising the function of the PH domain. A structurally similar compound inhibits kinase activity in vitro with an EC50 value of 12 µM by binding to the kinase domain.{15664} CAY10567 also inhibits hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase (RdRp) with an IC50 value of 79 µM. {15663}  

     

    Brand:
    Cayman
    SKU:10010233 - 500 mg

    Available on backorder

  • Most local anesthetics act by abolishing voltage gated sodium channel currents indiscriminately in all populations of neurons. Selective analgesia through TRPV1-mediated entry of a cationic lidocaine derivative, QX314, was recently reported.{15625} CAY10568 is a physically smaller, less hydrophobic version of QX314 designed to be even more permeable to TRPV1 ion channel when activated by agonists such as capsaicin and N-oleoyl dopamine. CAY10568 when given in combination with suitable TRPV1 agonists should produce selective blockade of the pain response while leaving motor, touch, and proprioception intact.  

     

    Brand:
    Cayman
    SKU:10012565 - 10 mg

    Available on backorder

  • Most local anesthetics act by abolishing voltage gated sodium channel currents indiscriminately in all populations of neurons. Selective analgesia through TRPV1-mediated entry of a cationic lidocaine derivative, QX314, was recently reported.{15625} CAY10568 is a physically smaller, less hydrophobic version of QX314 designed to be even more permeable to TRPV1 ion channel when activated by agonists such as capsaicin and N-oleoyl dopamine. CAY10568 when given in combination with suitable TRPV1 agonists should produce selective blockade of the pain response while leaving motor, touch, and proprioception intact.  

     

    Brand:
    Cayman
    SKU:10012565 - 100 mg

    Available on backorder

  • Most local anesthetics act by abolishing voltage gated sodium channel currents indiscriminately in all populations of neurons. Selective analgesia through TRPV1-mediated entry of a cationic lidocaine derivative, QX314, was recently reported.{15625} CAY10568 is a physically smaller, less hydrophobic version of QX314 designed to be even more permeable to TRPV1 ion channel when activated by agonists such as capsaicin and N-oleoyl dopamine. CAY10568 when given in combination with suitable TRPV1 agonists should produce selective blockade of the pain response while leaving motor, touch, and proprioception intact.  

     

    Brand:
    Cayman
    SKU:10012565 - 25 mg

    Available on backorder

  • Most local anesthetics act by abolishing voltage gated sodium channel currents indiscriminately in all populations of neurons. Selective analgesia through TRPV1-mediated entry of a cationic lidocaine derivative, QX314, was recently reported.{15625} CAY10568 is a physically smaller, less hydrophobic version of QX314 designed to be even more permeable to TRPV1 ion channel when activated by agonists such as capsaicin and N-oleoyl dopamine. CAY10568 when given in combination with suitable TRPV1 agonists should produce selective blockade of the pain response while leaving motor, touch, and proprioception intact.  

     

    Brand:
    Cayman
    SKU:10012565 - 50 mg

    Available on backorder

  • The enzyme fatty acid amide hydrolase (FAAH) is capable of hydrolyzing and inactivating anandamide and other fatty acid amides that act as agonists for the central cannabinoid (CB1) receptor.{3310} CAY10570 is a reversible competitive inhibitor of FAAH activity exhibiting an IC50 value of 1.3 µM.{14794} CAY10570 has no affinity for the human CB1 receptor and acts as a competitive inhibitor of FAAH activity without being hydrolyzed by the enzyme.{14794}  

     

    Brand:
    Cayman
    SKU:10010032 - 1 mg

    Available on backorder

  • The enzyme fatty acid amide hydrolase (FAAH) is capable of hydrolyzing and inactivating anandamide and other fatty acid amides that act as agonists for the central cannabinoid (CB1) receptor.{3310} CAY10570 is a reversible competitive inhibitor of FAAH activity exhibiting an IC50 value of 1.3 µM.{14794} CAY10570 has no affinity for the human CB1 receptor and acts as a competitive inhibitor of FAAH activity without being hydrolyzed by the enzyme.{14794}  

     

    Brand:
    Cayman
    SKU:10010032 - 10 mg

    Available on backorder

  • The enzyme fatty acid amide hydrolase (FAAH) is capable of hydrolyzing and inactivating anandamide and other fatty acid amides that act as agonists for the central cannabinoid (CB1) receptor.{3310} CAY10570 is a reversible competitive inhibitor of FAAH activity exhibiting an IC50 value of 1.3 µM.{14794} CAY10570 has no affinity for the human CB1 receptor and acts as a competitive inhibitor of FAAH activity without being hydrolyzed by the enzyme.{14794}  

     

    Brand:
    Cayman
    SKU:10010032 - 5 mg

    Available on backorder

  • The enzyme fatty acid amide hydrolase (FAAH) is capable of hydrolyzing and inactivating anandamide and other fatty acid amides that act as agonists for the central cannabinoid (CB1) receptor.{3310} CAY10570 is a reversible competitive inhibitor of FAAH activity exhibiting an IC50 value of 1.3 µM.{14794} CAY10570 has no affinity for the human CB1 receptor and acts as a competitive inhibitor of FAAH activity without being hydrolyzed by the enzyme.{14794}  

     

    Brand:
    Cayman
    SKU:10010032 - 500 µg

    Available on backorder

  • Pyridinylimidazoles, often termed CSAIDs, are a class of anti-inflammatory compounds that inhibit eicosanoid production and suppress the synthesis of cytokines in human monocytes.{16246} Because of its high specificity, one predominant pyridinylimidazole, SB203580, is frequently used to inhibit p38 MAPK, the tyrosine kinase activated by environmental stresses and inflammatory cytokines.{15737} CAY10571 is an analog of SB203580. It inhibits IL-1 production in the human monocytic cell line THP with an IC50 value of 0.20 µM and binds CSAID binding protein, a serine/threonine kinase homologous to p38, inhibiting its kinase activity with an IC50 value of 0.03 µM.{16229,13876} CAY105571 also inhibits 5-lipoxygenase production in RBL-1 cells with an IC50 value of 24 µM.{16229}  

     

    Brand:
    Cayman
    SKU:10010400 - 10 mg

    Available on backorder

  • Pyridinylimidazoles, often termed CSAIDs, are a class of anti-inflammatory compounds that inhibit eicosanoid production and suppress the synthesis of cytokines in human monocytes.{16246} Because of its high specificity, one predominant pyridinylimidazole, SB203580, is frequently used to inhibit p38 MAPK, the tyrosine kinase activated by environmental stresses and inflammatory cytokines.{15737} CAY10571 is an analog of SB203580. It inhibits IL-1 production in the human monocytic cell line THP with an IC50 value of 0.20 µM and binds CSAID binding protein, a serine/threonine kinase homologous to p38, inhibiting its kinase activity with an IC50 value of 0.03 µM.{16229,13876} CAY105571 also inhibits 5-lipoxygenase production in RBL-1 cells with an IC50 value of 24 µM.{16229}  

     

    Brand:
    Cayman
    SKU:10010400 - 25 mg

    Available on backorder

  • Pyridinylimidazoles, often termed CSAIDs, are a class of anti-inflammatory compounds that inhibit eicosanoid production and suppress the synthesis of cytokines in human monocytes.{16246} Because of its high specificity, one predominant pyridinylimidazole, SB203580, is frequently used to inhibit p38 MAPK, the tyrosine kinase activated by environmental stresses and inflammatory cytokines.{15737} CAY10571 is an analog of SB203580. It inhibits IL-1 production in the human monocytic cell line THP with an IC50 value of 0.20 µM and binds CSAID binding protein, a serine/threonine kinase homologous to p38, inhibiting its kinase activity with an IC50 value of 0.03 µM.{16229,13876} CAY105571 also inhibits 5-lipoxygenase production in RBL-1 cells with an IC50 value of 24 µM.{16229}  

     

    Brand:
    Cayman
    SKU:10010400 - 5 mg

    Available on backorder

  • The peroxisome proliferator-activated receptors (PPARs) are lipid-activated transcription factors often used as drug targets for the treatment of metabolic disorders. CAY10573 is a PPAR agonist that displays potent binding at PPARα, γ, and δ with IC50 values of 113, 50, and 223 nM, respectively. It potently transactivates PPARα, γ, and δ with EC50 values of 8, 70, and 500 nM, respectively.{14166} CAY10573 demonstrates stronger binding and functional activity for PPARγ than the antidiabetic compound rosiglitazone (IC50 = 92 nM; EC50 = 220 nM).{14166}  

     

    Brand:
    Cayman
    SKU:10008846 - 1 mg

    Available on backorder

  • The peroxisome proliferator-activated receptors (PPARs) are lipid-activated transcription factors often used as drug targets for the treatment of metabolic disorders. CAY10573 is a PPAR agonist that displays potent binding at PPARα, γ, and δ with IC50 values of 113, 50, and 223 nM, respectively. It potently transactivates PPARα, γ, and δ with EC50 values of 8, 70, and 500 nM, respectively.{14166} CAY10573 demonstrates stronger binding and functional activity for PPARγ than the antidiabetic compound rosiglitazone (IC50 = 92 nM; EC50 = 220 nM).{14166}  

     

    Brand:
    Cayman
    SKU:10008846 - 10 mg

    Available on backorder

  • The peroxisome proliferator-activated receptors (PPARs) are lipid-activated transcription factors often used as drug targets for the treatment of metabolic disorders. CAY10573 is a PPAR agonist that displays potent binding at PPARα, γ, and δ with IC50 values of 113, 50, and 223 nM, respectively. It potently transactivates PPARα, γ, and δ with EC50 values of 8, 70, and 500 nM, respectively.{14166} CAY10573 demonstrates stronger binding and functional activity for PPARγ than the antidiabetic compound rosiglitazone (IC50 = 92 nM; EC50 = 220 nM).{14166}  

     

    Brand:
    Cayman
    SKU:10008846 - 5 mg

    Available on backorder

  • The peroxisome proliferator-activated receptors (PPARs) are lipid-activated transcription factors often used as drug targets for the treatment of metabolic disorders. CAY10573 is a PPAR agonist that displays potent binding at PPARα, γ, and δ with IC50 values of 113, 50, and 223 nM, respectively. It potently transactivates PPARα, γ, and δ with EC50 values of 8, 70, and 500 nM, respectively.{14166} CAY10573 demonstrates stronger binding and functional activity for PPARγ than the antidiabetic compound rosiglitazone (IC50 = 92 nM; EC50 = 220 nM).{14166}  

     

    Brand:
    Cayman
    SKU:10008846 - 500 µg

    Available on backorder

  • Cyclin-dependent kinases (CDKs) play a key role in regulating cell division by phosphorylating distinct substrates in different phases of the cell cycle. Cell cycle deregulation in many cancers often results from altered CDK activity. Thus, CDKs are potential pharmacological targets for anticancer agents. CAY10574 is a potent, selective inhibitor of Cdk9 in vitro with an IC50 value of 0.35 µM. It is also a competitive inhibitor of Cdk2-cyclin E with respect to ATP, with Ki and IC50 values of 13.3 and 20 µM, respectively.{16228} CAY10574 reduces the population of S-phase cells of the cancer cell line HT-29 and blocks proliferation of several other cancer cell lines including MCF-7, HOS, G361, and K562 cells with IC50 values of 33, 49, 64, and 62 µM, respectively.{16228}  

     

    Brand:
    Cayman
    SKU:10011247 - 1 mg

    Available on backorder

  • Cyclin-dependent kinases (CDKs) play a key role in regulating cell division by phosphorylating distinct substrates in different phases of the cell cycle. Cell cycle deregulation in many cancers often results from altered CDK activity. Thus, CDKs are potential pharmacological targets for anticancer agents. CAY10574 is a potent, selective inhibitor of Cdk9 in vitro with an IC50 value of 0.35 µM. It is also a competitive inhibitor of Cdk2-cyclin E with respect to ATP, with Ki and IC50 values of 13.3 and 20 µM, respectively.{16228} CAY10574 reduces the population of S-phase cells of the cancer cell line HT-29 and blocks proliferation of several other cancer cell lines including MCF-7, HOS, G361, and K562 cells with IC50 values of 33, 49, 64, and 62 µM, respectively.{16228}  

     

    Brand:
    Cayman
    SKU:10011247 - 10 mg

    Available on backorder

  • Cyclin-dependent kinases (CDKs) play a key role in regulating cell division by phosphorylating distinct substrates in different phases of the cell cycle. Cell cycle deregulation in many cancers often results from altered CDK activity. Thus, CDKs are potential pharmacological targets for anticancer agents. CAY10574 is a potent, selective inhibitor of Cdk9 in vitro with an IC50 value of 0.35 µM. It is also a competitive inhibitor of Cdk2-cyclin E with respect to ATP, with Ki and IC50 values of 13.3 and 20 µM, respectively.{16228} CAY10574 reduces the population of S-phase cells of the cancer cell line HT-29 and blocks proliferation of several other cancer cell lines including MCF-7, HOS, G361, and K562 cells with IC50 values of 33, 49, 64, and 62 µM, respectively.{16228}  

     

    Brand:
    Cayman
    SKU:10011247 - 5 mg

    Available on backorder

  • Cyclin-dependent kinases (CDKs) play a key role in regulating cell division by phosphorylating distinct substrates in different phases of the cell cycle. Cell cycle deregulation in many cancers often results from altered CDK activity. Thus, CDKs are potential pharmacological targets for anticancer agents. CAY10574 is a potent, selective inhibitor of Cdk9 in vitro with an IC50 value of 0.35 µM. It is also a competitive inhibitor of Cdk2-cyclin E with respect to ATP, with Ki and IC50 values of 13.3 and 20 µM, respectively.{16228} CAY10574 reduces the population of S-phase cells of the cancer cell line HT-29 and blocks proliferation of several other cancer cell lines including MCF-7, HOS, G361, and K562 cells with IC50 values of 33, 49, 64, and 62 µM, respectively.{16228}  

     

    Brand:
    Cayman
    SKU:10011247 - 50 mg

    Available on backorder

  • The NF-κB/Rel transcription factors, known to be involved in the regulation of pro-inflammatory cytokines and the pathogenesis of a variety of diseases, are present in the cytosol in an inactive state, complexed with inhibitory IκB proteins. NF-κB is activated upon degradation of IκB following IKK-α and IKK-β phosphorylation. IKK-ε, a homolog of IKK-α and IKK-β, can also activate NF-κB. IKK-ε is expressed predominantly in immune cells and is thought to play a role in the immune response. CAY10575 is a benzimidazole analog that inhibits IKK-ε with an IC50 value of ~15.8 µM.{16237}  

     

    Brand:
    Cayman
    SKU:10011248 - 1 mg

    Available on backorder

  • The NF-κB/Rel transcription factors, known to be involved in the regulation of pro-inflammatory cytokines and the pathogenesis of a variety of diseases, are present in the cytosol in an inactive state, complexed with inhibitory IκB proteins. NF-κB is activated upon degradation of IκB following IKK-α and IKK-β phosphorylation. IKK-ε, a homolog of IKK-α and IKK-β, can also activate NF-κB. IKK-ε is expressed predominantly in immune cells and is thought to play a role in the immune response. CAY10575 is a benzimidazole analog that inhibits IKK-ε with an IC50 value of ~15.8 µM.{16237}  

     

    Brand:
    Cayman
    SKU:10011248 - 10 mg

    Available on backorder

  • The NF-κB/Rel transcription factors, known to be involved in the regulation of pro-inflammatory cytokines and the pathogenesis of a variety of diseases, are present in the cytosol in an inactive state, complexed with inhibitory IκB proteins. NF-κB is activated upon degradation of IκB following IKK-α and IKK-β phosphorylation. IKK-ε, a homolog of IKK-α and IKK-β, can also activate NF-κB. IKK-ε is expressed predominantly in immune cells and is thought to play a role in the immune response. CAY10575 is a benzimidazole analog that inhibits IKK-ε with an IC50 value of ~15.8 µM.{16237}  

     

    Brand:
    Cayman
    SKU:10011248 - 25 mg

    Available on backorder

  • The NF-κB/Rel transcription factors, known to be involved in the regulation of pro-inflammatory cytokines and the pathogenesis of a variety of diseases, are present in the cytosol in an inactive state, complexed with inhibitory IκB proteins. NF-κB is activated upon degradation of IκB following IKK-α and IKK-β phosphorylation. IKK-ε, a homolog of IKK-α and IKK-β, can also activate NF-κB. IKK-ε is expressed predominantly in immune cells and is thought to play a role in the immune response. CAY10575 is a benzimidazole analog that inhibits IKK-ε with an IC50 value of ~15.8 µM.{16237}  

     

    Brand:
    Cayman
    SKU:10011248 - 5 mg

    Available on backorder

  • The NF-κB/Rel transcription factors, known to be involved in the regulation of pro-inflammatory cytokines and the pathogenesis of a variety of diseases, are present in the cytosol in an inactive state, complexed with inhibitory IκB proteins. NF-κB is activated upon degradation of IκB following IKKα and IKKβ phosphorylation. IKKε, a homolog of IKKα and IKKβ, can also activate NF-κB. IKKε is expressed predominantly in immune cells, and is thought to play a role in the immune response. CAY10576 is a benzimidazole analog that selectively inhibits IKKε with an IC50 value of 40 nM and is essentially inactive at IKKα and IKKβ.{16237}  

     

    Brand:
    Cayman
    SKU:10011249 - 1 mg

    Available on backorder

  • The NF-κB/Rel transcription factors, known to be involved in the regulation of pro-inflammatory cytokines and the pathogenesis of a variety of diseases, are present in the cytosol in an inactive state, complexed with inhibitory IκB proteins. NF-κB is activated upon degradation of IκB following IKKα and IKKβ phosphorylation. IKKε, a homolog of IKKα and IKKβ, can also activate NF-κB. IKKε is expressed predominantly in immune cells, and is thought to play a role in the immune response. CAY10576 is a benzimidazole analog that selectively inhibits IKKε with an IC50 value of 40 nM and is essentially inactive at IKKα and IKKβ.{16237}  

     

    Brand:
    Cayman
    SKU:10011249 - 10 mg

    Available on backorder

  • The NF-κB/Rel transcription factors, known to be involved in the regulation of pro-inflammatory cytokines and the pathogenesis of a variety of diseases, are present in the cytosol in an inactive state, complexed with inhibitory IκB proteins. NF-κB is activated upon degradation of IκB following IKKα and IKKβ phosphorylation. IKKε, a homolog of IKKα and IKKβ, can also activate NF-κB. IKKε is expressed predominantly in immune cells, and is thought to play a role in the immune response. CAY10576 is a benzimidazole analog that selectively inhibits IKKε with an IC50 value of 40 nM and is essentially inactive at IKKα and IKKβ.{16237}  

     

    Brand:
    Cayman
    SKU:10011249 - 5 mg

    Available on backorder

  • The NF-κB/Rel transcription factors, known to be involved in the regulation of pro-inflammatory cytokines and the pathogenesis of a variety of diseases, are present in the cytosol in an inactive state, complexed with inhibitory IκB proteins. NF-κB is activated upon degradation of IκB following IKKα and IKKβ phosphorylation. IKKε, a homolog of IKKα and IKKβ, can also activate NF-κB. IKKε is expressed predominantly in immune cells, and is thought to play a role in the immune response. CAY10576 is a benzimidazole analog that selectively inhibits IKKε with an IC50 value of 40 nM and is essentially inactive at IKKα and IKKβ.{16237}  

     

    Brand:
    Cayman
    SKU:10011249 - 50 mg

    Available on backorder

  • Casein kinase 2 (CK2) is a serine/threonine-selective protein kinase involved in many signal transduction pathways. CK2 is known to negatively regulate apoptosis and its activity is increased in many proliferating tissues and tumors, which lends promise as an anti-cancer drug target. CAY10577 inhibits CK2 with an IC50 value of 0.8 µM.{16238}  

     

    Brand:
    Cayman
    SKU:10011256 - 1 mg

    Available on backorder

  • Casein kinase 2 (CK2) is a serine/threonine-selective protein kinase involved in many signal transduction pathways. CK2 is known to negatively regulate apoptosis and its activity is increased in many proliferating tissues and tumors, which lends promise as an anti-cancer drug target. CAY10577 inhibits CK2 with an IC50 value of 0.8 µM.{16238}  

     

    Brand:
    Cayman
    SKU:10011256 - 10 mg

    Available on backorder

  • Casein kinase 2 (CK2) is a serine/threonine-selective protein kinase involved in many signal transduction pathways. CK2 is known to negatively regulate apoptosis and its activity is increased in many proliferating tissues and tumors, which lends promise as an anti-cancer drug target. CAY10577 inhibits CK2 with an IC50 value of 0.8 µM.{16238}  

     

    Brand:
    Cayman
    SKU:10011256 - 5 mg

    Available on backorder

  • Casein kinase 2 (CK2) is a serine/threonine-selective protein kinase involved in many signal transduction pathways. CK2 is known to negatively regulate apoptosis and its activity is increased in many proliferating tissues and tumors, which lends promise as an anti-cancer drug target. CAY10577 inhibits CK2 with an IC50 value of 0.8 µM.{16238}  

     

    Brand:
    Cayman
    SKU:10011256 - 50 mg

    Available on backorder

  • Casein Kinase 2 (CK2) is a constitutive protein kinase involved in many signal transduction pathways. CK2 is known to negatively regulate apoptosis, and its activity is increased in many proliferating tissues and tumors, which lends promise as an anticancer drug target. CAY10578 is a potent inhibitor of CK2 with an IC50 value of 0.3 µM.{16239} This compound is ATP competitive, displaying a Ki value of 0.2 µM and only minimally inhibits the activities of other protein kinases (e.g., GSK3, Cdk5, and MSK1).{16239}  

     

    Brand:
    Cayman
    SKU:10011264 - 1 mg

    Available on backorder

  • Casein Kinase 2 (CK2) is a constitutive protein kinase involved in many signal transduction pathways. CK2 is known to negatively regulate apoptosis, and its activity is increased in many proliferating tissues and tumors, which lends promise as an anticancer drug target. CAY10578 is a potent inhibitor of CK2 with an IC50 value of 0.3 µM.{16239} This compound is ATP competitive, displaying a Ki value of 0.2 µM and only minimally inhibits the activities of other protein kinases (e.g., GSK3, Cdk5, and MSK1).{16239}  

     

    Brand:
    Cayman
    SKU:10011264 - 10 mg

    Available on backorder

  • Casein Kinase 2 (CK2) is a constitutive protein kinase involved in many signal transduction pathways. CK2 is known to negatively regulate apoptosis, and its activity is increased in many proliferating tissues and tumors, which lends promise as an anticancer drug target. CAY10578 is a potent inhibitor of CK2 with an IC50 value of 0.3 µM.{16239} This compound is ATP competitive, displaying a Ki value of 0.2 µM and only minimally inhibits the activities of other protein kinases (e.g., GSK3, Cdk5, and MSK1).{16239}  

     

    Brand:
    Cayman
    SKU:10011264 - 25 mg

    Available on backorder

  • Casein Kinase 2 (CK2) is a constitutive protein kinase involved in many signal transduction pathways. CK2 is known to negatively regulate apoptosis, and its activity is increased in many proliferating tissues and tumors, which lends promise as an anticancer drug target. CAY10578 is a potent inhibitor of CK2 with an IC50 value of 0.3 µM.{16239} This compound is ATP competitive, displaying a Ki value of 0.2 µM and only minimally inhibits the activities of other protein kinases (e.g., GSK3, Cdk5, and MSK1).{16239}  

     

    Brand:
    Cayman
    SKU:10011264 - 5 mg

    Available on backorder

  • Prostaglandin E2 (PGE2) activates four E prostanoid (EP) receptors, EP1-4. EP4 is a Gs protein-coupled receptor that, by elevating the second messenger cAMP, plays important roles in bone formation and resorption,{16772} cancer,{16773} and atherosclerosis.{16619} CAY10580 is an 8-aza-9-oxo-15-hydroxy saturated analog of PGE2. It selectively binds the EP4 receptor (Ki = 35 nM) relative to the EP1, EP2, and EP3 receptors (Ki = 3,000, 2,000, and >3,000 nM, respectively).{16762} CAY10580 stimulates cAMP formation in excised mouse ovaries.{16763}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • Prostaglandin E2 (PGE2) activates four E prostanoid (EP) receptors, EP1-4. EP4 is a Gs protein-coupled receptor that, by elevating the second messenger cAMP, plays important roles in bone formation and resorption,{16772} cancer,{16773} and atherosclerosis.{16619} CAY10580 is an 8-aza-9-oxo-15-hydroxy saturated analog of PGE2. It selectively binds the EP4 receptor (Ki = 35 nM) relative to the EP1, EP2, and EP3 receptors (Ki = 3,000, 2,000, and >3,000 nM, respectively).{16762} CAY10580 stimulates cAMP formation in excised mouse ovaries.{16763}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • Prostaglandin E2 (PGE2) activates four E prostanoid (EP) receptors, EP1-4. EP4 is a Gs protein-coupled receptor that, by elevating the second messenger cAMP, plays important roles in bone formation and resorption,{16772} cancer,{16773} and atherosclerosis.{16619} CAY10580 is an 8-aza-9-oxo-15-hydroxy saturated analog of PGE2. It selectively binds the EP4 receptor (Ki = 35 nM) relative to the EP1, EP2, and EP3 receptors (Ki = 3,000, 2,000, and >3,000 nM, respectively).{16762} CAY10580 stimulates cAMP formation in excised mouse ovaries.{16763}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • Prostaglandin E2 (PGE2) activates four E prostanoid (EP) receptors, EP1-4. EP4 is a Gs protein-coupled receptor that, by elevating the second messenger cAMP, plays important roles in bone formation and resorption,{16772} cancer,{16773} and atherosclerosis.{16619} CAY10580 is an 8-aza-9-oxo-15-hydroxy saturated analog of PGE2. It selectively binds the EP4 receptor (Ki = 35 nM) relative to the EP1, EP2, and EP3 receptors (Ki = 3,000, 2,000, and >3,000 nM, respectively).{16762} CAY10580 stimulates cAMP formation in excised mouse ovaries.{16763}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • The enzyme indoleamine 2,3-dioxygenase (IDO) has been implicated in mediating pathological immunosuppression associated with certain diseases, including cancer. Several naphthoquinones inhibit IDO in vitro and in cells, but at low (μM) potency.{16354} Importantly, naphthoquinones reduce tumor growth in wild type mice but not in IDO-deficient mice.{16354} CAY10581 is a naphthoquinone derivative that potently inhibits IDO (IC50 = 55 nM).{16354} It is a more potent inhibitor of IDO than annulin B or 1-methyl-d-tryptophan (1MT). CAY10581 acts as a reversible uncompetitive inhibitor of IDO and demonstrates minimal impact on cell viability at 100 μM after 24 hours.{16354}  

     

    Brand:
    Cayman
    SKU:-

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  • The enzyme indoleamine 2,3-dioxygenase (IDO) has been implicated in mediating pathological immunosuppression associated with certain diseases, including cancer. Several naphthoquinones inhibit IDO in vitro and in cells, but at low (μM) potency.{16354} Importantly, naphthoquinones reduce tumor growth in wild type mice but not in IDO-deficient mice.{16354} CAY10581 is a naphthoquinone derivative that potently inhibits IDO (IC50 = 55 nM).{16354} It is a more potent inhibitor of IDO than annulin B or 1-methyl-d-tryptophan (1MT). CAY10581 acts as a reversible uncompetitive inhibitor of IDO and demonstrates minimal impact on cell viability at 100 μM after 24 hours.{16354}  

     

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  • The enzyme indoleamine 2,3-dioxygenase (IDO) has been implicated in mediating pathological immunosuppression associated with certain diseases, including cancer. Several naphthoquinones inhibit IDO in vitro and in cells, but at low (μM) potency.{16354} Importantly, naphthoquinones reduce tumor growth in wild type mice but not in IDO-deficient mice.{16354} CAY10581 is a naphthoquinone derivative that potently inhibits IDO (IC50 = 55 nM).{16354} It is a more potent inhibitor of IDO than annulin B or 1-methyl-d-tryptophan (1MT). CAY10581 acts as a reversible uncompetitive inhibitor of IDO and demonstrates minimal impact on cell viability at 100 μM after 24 hours.{16354}  

     

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    Cayman
    SKU:-

    Out of stock

  • The enzyme indoleamine 2,3-dioxygenase (IDO) has been implicated in mediating pathological immunosuppression associated with certain diseases, including cancer. Several naphthoquinones inhibit IDO in vitro and in cells, but at low (μM) potency.{16354} Importantly, naphthoquinones reduce tumor growth in wild type mice but not in IDO-deficient mice.{16354} CAY10581 is a naphthoquinone derivative that potently inhibits IDO (IC50 = 55 nM).{16354} It is a more potent inhibitor of IDO than annulin B or 1-methyl-d-tryptophan (1MT). CAY10581 acts as a reversible uncompetitive inhibitor of IDO and demonstrates minimal impact on cell viability at 100 μM after 24 hours.{16354}  

     

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    Cayman
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  • Leukotriene B4 (LTB4) promotes a number of leukocyte functions including aggregation, stimulation of ion fluxes, superoxide anion production, chemotaxis, and chemokinesis. Two G protein-coupled receptors, BLT1 and BLT2 mediate the actions of LTB4. CAY10583 is a potent, selective full agonist for BLT2 with an EC50 value of 20 nM.{15624} It does not displace [3H]-leukotriene B4 (LTB4) binding to BLT1 at concentrations >1 µM and activates BLT2 at significantly lower concentrations than LTB4 (EC50 = 170 nM).{15624} CAY10583 dose dependently increases intracellular calcium stores and induces ERK phosphorylation in Chinese hamster ovary (CHO) cells expressing BLT2 with no effect on CHO cells expressing BLT1.{15624}  

     

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    Cayman
    SKU:10012424 - 10 mg

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  • Leukotriene B4 (LTB4) promotes a number of leukocyte functions including aggregation, stimulation of ion fluxes, superoxide anion production, chemotaxis, and chemokinesis. Two G protein-coupled receptors, BLT1 and BLT2 mediate the actions of LTB4. CAY10583 is a potent, selective full agonist for BLT2 with an EC50 value of 20 nM.{15624} It does not displace [3H]-leukotriene B4 (LTB4) binding to BLT1 at concentrations >1 µM and activates BLT2 at significantly lower concentrations than LTB4 (EC50 = 170 nM).{15624} CAY10583 dose dependently increases intracellular calcium stores and induces ERK phosphorylation in Chinese hamster ovary (CHO) cells expressing BLT2 with no effect on CHO cells expressing BLT1.{15624}  

     

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    SKU:10012424 - 25 mg

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  • Leukotriene B4 (LTB4) promotes a number of leukocyte functions including aggregation, stimulation of ion fluxes, superoxide anion production, chemotaxis, and chemokinesis. Two G protein-coupled receptors, BLT1 and BLT2 mediate the actions of LTB4. CAY10583 is a potent, selective full agonist for BLT2 with an EC50 value of 20 nM.{15624} It does not displace [3H]-leukotriene B4 (LTB4) binding to BLT1 at concentrations >1 µM and activates BLT2 at significantly lower concentrations than LTB4 (EC50 = 170 nM).{15624} CAY10583 dose dependently increases intracellular calcium stores and induces ERK phosphorylation in Chinese hamster ovary (CHO) cells expressing BLT2 with no effect on CHO cells expressing BLT1.{15624}  

     

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    Cayman
    SKU:10012424 - 5 mg

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  • Leukotriene B4 (LTB4) promotes a number of leukocyte functions including aggregation, stimulation of ion fluxes, superoxide anion production, chemotaxis, and chemokinesis. Two G protein-coupled receptors, BLT1 and BLT2 mediate the actions of LTB4. CAY10583 is a potent, selective full agonist for BLT2 with an EC50 value of 20 nM.{15624} It does not displace [3H]-leukotriene B4 (LTB4) binding to BLT1 at concentrations >1 µM and activates BLT2 at significantly lower concentrations than LTB4 (EC50 = 170 nM).{15624} CAY10583 dose dependently increases intracellular calcium stores and induces ERK phosphorylation in Chinese hamster ovary (CHO) cells expressing BLT2 with no effect on CHO cells expressing BLT1.{15624}  

     

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    SKU:10012424 - 50 mg

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  • Hypoxia-inducible factor-1 (HIF-1) is a heterodimeric transcription factor composed of a HIF-1α subunit and HIF-1β subunit. Whereas the HIF-1β subunit is constitutively expressed, the HIF-1α subunit is regulated by cellular oxygen levels and therefore plays an important role in maintaining cellular oxygen homeostasis.{11044,12428} Under normoxic conditions, HIF-1α is selectively hydroxylated on proline residues 402 and 577 and targeted for destruction by the ubiquitin-proteasome system. Under hypoxic conditions, HIF-1α accumulates and dimerizes with HIF-1β to promote the transcription of a number of genes involved in angiogenesis, glycolysis, growth factor signaling, tumor invasion, and metastasis. CAY10585 is a novel small molecule inhibitor of HIF-1α accumulation and gene transcriptional activity.{16441} In a gene reporter assay using human Hep3B and AGS cell lines, CAY10585 prevented HIF-1 transcriptional activity with IC50 values of 2.6 and 0.7 µM, respectively. It blocks HIF-1α accumulation in Hep3B cells in a concentration and time-dependent manner, with complete inhibition at a concentration of 30 µM within 12 hours. CAY10585 also significantly suppresses transcription of the HIF-1 target genes VEGF and erythropoietin at 10 µM.{16441}  

     

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    SKU:10012682 - 1 mg

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  • Hypoxia-inducible factor-1 (HIF-1) is a heterodimeric transcription factor composed of a HIF-1α subunit and HIF-1β subunit. Whereas the HIF-1β subunit is constitutively expressed, the HIF-1α subunit is regulated by cellular oxygen levels and therefore plays an important role in maintaining cellular oxygen homeostasis.{11044,12428} Under normoxic conditions, HIF-1α is selectively hydroxylated on proline residues 402 and 577 and targeted for destruction by the ubiquitin-proteasome system. Under hypoxic conditions, HIF-1α accumulates and dimerizes with HIF-1β to promote the transcription of a number of genes involved in angiogenesis, glycolysis, growth factor signaling, tumor invasion, and metastasis. CAY10585 is a novel small molecule inhibitor of HIF-1α accumulation and gene transcriptional activity.{16441} In a gene reporter assay using human Hep3B and AGS cell lines, CAY10585 prevented HIF-1 transcriptional activity with IC50 values of 2.6 and 0.7 µM, respectively. It blocks HIF-1α accumulation in Hep3B cells in a concentration and time-dependent manner, with complete inhibition at a concentration of 30 µM within 12 hours. CAY10585 also significantly suppresses transcription of the HIF-1 target genes VEGF and erythropoietin at 10 µM.{16441}  

     

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    SKU:10012682 - 10 mg

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  • Hypoxia-inducible factor-1 (HIF-1) is a heterodimeric transcription factor composed of a HIF-1α subunit and HIF-1β subunit. Whereas the HIF-1β subunit is constitutively expressed, the HIF-1α subunit is regulated by cellular oxygen levels and therefore plays an important role in maintaining cellular oxygen homeostasis.{11044,12428} Under normoxic conditions, HIF-1α is selectively hydroxylated on proline residues 402 and 577 and targeted for destruction by the ubiquitin-proteasome system. Under hypoxic conditions, HIF-1α accumulates and dimerizes with HIF-1β to promote the transcription of a number of genes involved in angiogenesis, glycolysis, growth factor signaling, tumor invasion, and metastasis. CAY10585 is a novel small molecule inhibitor of HIF-1α accumulation and gene transcriptional activity.{16441} In a gene reporter assay using human Hep3B and AGS cell lines, CAY10585 prevented HIF-1 transcriptional activity with IC50 values of 2.6 and 0.7 µM, respectively. It blocks HIF-1α accumulation in Hep3B cells in a concentration and time-dependent manner, with complete inhibition at a concentration of 30 µM within 12 hours. CAY10585 also significantly suppresses transcription of the HIF-1 target genes VEGF and erythropoietin at 10 µM.{16441}  

     

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    Cayman
    SKU:10012682 - 25 mg

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  • Hypoxia-inducible factor-1 (HIF-1) is a heterodimeric transcription factor composed of a HIF-1α subunit and HIF-1β subunit. Whereas the HIF-1β subunit is constitutively expressed, the HIF-1α subunit is regulated by cellular oxygen levels and therefore plays an important role in maintaining cellular oxygen homeostasis.{11044,12428} Under normoxic conditions, HIF-1α is selectively hydroxylated on proline residues 402 and 577 and targeted for destruction by the ubiquitin-proteasome system. Under hypoxic conditions, HIF-1α accumulates and dimerizes with HIF-1β to promote the transcription of a number of genes involved in angiogenesis, glycolysis, growth factor signaling, tumor invasion, and metastasis. CAY10585 is a novel small molecule inhibitor of HIF-1α accumulation and gene transcriptional activity.{16441} In a gene reporter assay using human Hep3B and AGS cell lines, CAY10585 prevented HIF-1 transcriptional activity with IC50 values of 2.6 and 0.7 µM, respectively. It blocks HIF-1α accumulation in Hep3B cells in a concentration and time-dependent manner, with complete inhibition at a concentration of 30 µM within 12 hours. CAY10585 also significantly suppresses transcription of the HIF-1 target genes VEGF and erythropoietin at 10 µM.{16441}  

     

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    Cayman
    SKU:10012682 - 5 mg

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  • The free fatty acid receptor 1 (FFAR1; GPR40) is highly expressed in pancreatic β-cells and activated by medium and long-chain fatty acids.{13138} There is evidence of a link between FFAR1 (GPR40) and the ability of fatty acids to amplify glucose-stimulated insulin secretion, making this signaling pathway a potential target for regulating diabetes, obesity, and other metabolic disorders.{13139,14742} CAY10587 is a selective FFAR1 (GPR40) agonist (EC50 = 32 nM) that does not exhibit activity on the related FFARs: FFAR2 (GPR43) or FFAR3 (GPR41).{16584} At 100 nM, CAY10587 increases glucose-stimulated insulin secretion in the rat insulin-secreting cell line INS-1E.{16584}  

     

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  • The free fatty acid receptor 1 (FFAR1; GPR40) is highly expressed in pancreatic β-cells and activated by medium and long-chain fatty acids.{13138} There is evidence of a link between FFAR1 (GPR40) and the ability of fatty acids to amplify glucose-stimulated insulin secretion, making this signaling pathway a potential target for regulating diabetes, obesity, and other metabolic disorders.{13139,14742} CAY10587 is a selective FFAR1 (GPR40) agonist (EC50 = 32 nM) that does not exhibit activity on the related FFARs: FFAR2 (GPR43) or FFAR3 (GPR41).{16584} At 100 nM, CAY10587 increases glucose-stimulated insulin secretion in the rat insulin-secreting cell line INS-1E.{16584}  

     

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    Cayman
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  • The free fatty acid receptor 1 (FFAR1; GPR40) is highly expressed in pancreatic β-cells and activated by medium and long-chain fatty acids.{13138} There is evidence of a link between FFAR1 (GPR40) and the ability of fatty acids to amplify glucose-stimulated insulin secretion, making this signaling pathway a potential target for regulating diabetes, obesity, and other metabolic disorders.{13139,14742} CAY10587 is a selective FFAR1 (GPR40) agonist (EC50 = 32 nM) that does not exhibit activity on the related FFARs: FFAR2 (GPR43) or FFAR3 (GPR41).{16584} At 100 nM, CAY10587 increases glucose-stimulated insulin secretion in the rat insulin-secreting cell line INS-1E.{16584}  

     

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    Cayman
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  • The free fatty acid receptor 1 (FFAR1; GPR40) is highly expressed in pancreatic β-cells and activated by medium and long-chain fatty acids.{13138} There is evidence of a link between FFAR1 (GPR40) and the ability of fatty acids to amplify glucose-stimulated insulin secretion, making this signaling pathway a potential target for regulating diabetes, obesity, and other metabolic disorders.{13139,14742} CAY10587 is a selective FFAR1 (GPR40) agonist (EC50 = 32 nM) that does not exhibit activity on the related FFARs: FFAR2 (GPR43) or FFAR3 (GPR41).{16584} At 100 nM, CAY10587 increases glucose-stimulated insulin secretion in the rat insulin-secreting cell line INS-1E.{16584}  

     

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    Cayman
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  • Microsomal Prostaglandin E2 Synthase-1 (mPGES-1), with cyclooxygenase-2 (COX-2), synthesizes PGE2, which is directly involved in signaling during inflammation, fever and pain. 5-Lipoxygenase (5-LO) initiates the synthesis of leukotrienes (LTs), which are pro-inflammatory mediators. CAY10589 is a dual inhibitor of mPGES-1 (IC50 = 1.3 μM) and 5-LO (IC50 = 1.0 μM).{16667} It effectively inhibits PGE2 and LT synthesis in both cell free and intact cell assays. CAY10589 has minor effects on COX-1 and COX-2, inhibiting these enzymes 34% and 38.8%, respectively, at 10 μM.{16667}  

     

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  • Microsomal Prostaglandin E2 Synthase-1 (mPGES-1), with cyclooxygenase-2 (COX-2), synthesizes PGE2, which is directly involved in signaling during inflammation, fever and pain. 5-Lipoxygenase (5-LO) initiates the synthesis of leukotrienes (LTs), which are pro-inflammatory mediators. CAY10589 is a dual inhibitor of mPGES-1 (IC50 = 1.3 μM) and 5-LO (IC50 = 1.0 μM).{16667} It effectively inhibits PGE2 and LT synthesis in both cell free and intact cell assays. CAY10589 has minor effects on COX-1 and COX-2, inhibiting these enzymes 34% and 38.8%, respectively, at 10 μM.{16667}  

     

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    Cayman
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  • Microsomal Prostaglandin E2 Synthase-1 (mPGES-1), with cyclooxygenase-2 (COX-2), synthesizes PGE2, which is directly involved in signaling during inflammation, fever and pain. 5-Lipoxygenase (5-LO) initiates the synthesis of leukotrienes (LTs), which are pro-inflammatory mediators. CAY10589 is a dual inhibitor of mPGES-1 (IC50 = 1.3 μM) and 5-LO (IC50 = 1.0 μM).{16667} It effectively inhibits PGE2 and LT synthesis in both cell free and intact cell assays. CAY10589 has minor effects on COX-1 and COX-2, inhibiting these enzymes 34% and 38.8%, respectively, at 10 μM.{16667}  

     

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    Cayman
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  • Phospholipase A2 (PLA2) catalyzes the hydrolysis of fatty acids at the sn-2 position of glycerophospholipids, liberating arachidonic acid for subsequent eicosanoid synthesis.{2489} Three primary types of PLA2 exist: secretory (sPLA2), calcium-dependent cytosolic (cPLA2), and calcium-independent cytosolic (iPLA2).{1474} Of these three enzymes, cPLA2 is the rate-limiting stimulus for release of arachidonic acid whereas sPLA2 amplifies the action of cPLA2 and regulates phagocytosis and foam cell formation.{14662} CAY10590, a simple amide based on (R)-γ-norleucine, is a potent and selective inhibitor of sPLA2. It exhibits 95% inhibition (XI(50) = 0.003) of sPLA2 at 0.091 mole fraction without affecting the activities of cPLA2 or iPLA2.{16718}  

     

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    Cayman
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  • Phospholipase A2 (PLA2) catalyzes the hydrolysis of fatty acids at the sn-2 position of glycerophospholipids, liberating arachidonic acid for subsequent eicosanoid synthesis.{2489} Three primary types of PLA2 exist: secretory (sPLA2), calcium-dependent cytosolic (cPLA2), and calcium-independent cytosolic (iPLA2).{1474} Of these three enzymes, cPLA2 is the rate-limiting stimulus for release of arachidonic acid whereas sPLA2 amplifies the action of cPLA2 and regulates phagocytosis and foam cell formation.{14662} CAY10590, a simple amide based on (R)-γ-norleucine, is a potent and selective inhibitor of sPLA2. It exhibits 95% inhibition (XI(50) = 0.003) of sPLA2 at 0.091 mole fraction without affecting the activities of cPLA2 or iPLA2.{16718}  

     

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    Cayman
    SKU:-
  • Phospholipase A2 (PLA2) catalyzes the hydrolysis of fatty acids at the sn-2 position of glycerophospholipids, liberating arachidonic acid for subsequent eicosanoid synthesis.{2489} Three primary types of PLA2 exist: secretory (sPLA2), calcium-dependent cytosolic (cPLA2), and calcium-independent cytosolic (iPLA2).{1474} Of these three enzymes, cPLA2 is the rate-limiting stimulus for release of arachidonic acid whereas sPLA2 amplifies the action of cPLA2 and regulates phagocytosis and foam cell formation.{14662} CAY10590, a simple amide based on (R)-γ-norleucine, is a potent and selective inhibitor of sPLA2. It exhibits 95% inhibition (XI(50) = 0.003) of sPLA2 at 0.091 mole fraction without affecting the activities of cPLA2 or iPLA2.{16718}  

     

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    Cayman
    SKU:-
  • Phospholipase A2 (PLA2) catalyzes the hydrolysis of fatty acids at the sn-2 position of glycerophospholipids, liberating arachidonic acid for subsequent eicosanoid synthesis.{2489} Three primary types of PLA2 exist: secretory (sPLA2), calcium-dependent cytosolic (cPLA2), and calcium-independent cytosolic (iPLA2).{1474} Of these three enzymes, cPLA2 is the rate-limiting stimulus for release of arachidonic acid whereas sPLA2 amplifies the action of cPLA2 and regulates phagocytosis and foam cell formation.{14662} CAY10590, a simple amide based on (R)-γ-norleucine, is a potent and selective inhibitor of sPLA2. It exhibits 95% inhibition (XI(50) = 0.003) of sPLA2 at 0.091 mole fraction without affecting the activities of cPLA2 or iPLA2.{16718}  

     

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    Cayman
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  • Sirtuins (SIRTs) represent a distinct class of trichostatin A-insensitive lysyl-deacetylases (class III HDACs). Human SIRT1 is the homolog of yeast silent information regulator 2 (Sir2) and has been shown to regulate the activity of the p53 tumor suppressor and inhibit apoptosis. Small molecule activators of SIRT1, such as resveratrol, extend lifespan in yeast and C. elegans in a manner that resembles caloric restriction. CAY10591 has been identified as an activator of the enzyme SIRT1. This compound increases fluorescence by 233% in a SIRT1 activity assay.{14683} [Activator activity was defined as the percentage of signal increase relative to signal window in the following formula: 100 x (Sample – Signallow)/(Signalhigh – Signallow)]. CAY10591 suppresses TNF-α in a dose-dependent manner. In THP-1 cells, TNF-α levels decreased from 325 pg/ml (control) to 104 and 53 pg/ml with 20 and 60 µM CAY10591, respectively. This activator also has a significant dose-dependent effect on fat mobilization in differentiated adipocytes, which would indicate the potential of SIRT1 activators for anti-obesity or anti-diabetic purposes.{14683}  

     

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    SKU:10009797 - 1 mg

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  • Sirtuins (SIRTs) represent a distinct class of trichostatin A-insensitive lysyl-deacetylases (class III HDACs). Human SIRT1 is the homolog of yeast silent information regulator 2 (Sir2) and has been shown to regulate the activity of the p53 tumor suppressor and inhibit apoptosis. Small molecule activators of SIRT1, such as resveratrol, extend lifespan in yeast and C. elegans in a manner that resembles caloric restriction. CAY10591 has been identified as an activator of the enzyme SIRT1. This compound increases fluorescence by 233% in a SIRT1 activity assay.{14683} [Activator activity was defined as the percentage of signal increase relative to signal window in the following formula: 100 x (Sample – Signallow)/(Signalhigh – Signallow)]. CAY10591 suppresses TNF-α in a dose-dependent manner. In THP-1 cells, TNF-α levels decreased from 325 pg/ml (control) to 104 and 53 pg/ml with 20 and 60 µM CAY10591, respectively. This activator also has a significant dose-dependent effect on fat mobilization in differentiated adipocytes, which would indicate the potential of SIRT1 activators for anti-obesity or anti-diabetic purposes.{14683}  

     

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    Cayman
    SKU:10009797 - 10 mg

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  • Sirtuins (SIRTs) represent a distinct class of trichostatin A-insensitive lysyl-deacetylases (class III HDACs). Human SIRT1 is the homolog of yeast silent information regulator 2 (Sir2) and has been shown to regulate the activity of the p53 tumor suppressor and inhibit apoptosis. Small molecule activators of SIRT1, such as resveratrol, extend lifespan in yeast and C. elegans in a manner that resembles caloric restriction. CAY10591 has been identified as an activator of the enzyme SIRT1. This compound increases fluorescence by 233% in a SIRT1 activity assay.{14683} [Activator activity was defined as the percentage of signal increase relative to signal window in the following formula: 100 x (Sample – Signallow)/(Signalhigh – Signallow)]. CAY10591 suppresses TNF-α in a dose-dependent manner. In THP-1 cells, TNF-α levels decreased from 325 pg/ml (control) to 104 and 53 pg/ml with 20 and 60 µM CAY10591, respectively. This activator also has a significant dose-dependent effect on fat mobilization in differentiated adipocytes, which would indicate the potential of SIRT1 activators for anti-obesity or anti-diabetic purposes.{14683}  

     

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    Cayman
    SKU:10009797 - 25 mg

    Available on backorder

  • Sirtuins (SIRTs) represent a distinct class of trichostatin A-insensitive lysyl-deacetylases (class III HDACs). Human SIRT1 is the homolog of yeast silent information regulator 2 (Sir2) and has been shown to regulate the activity of the p53 tumor suppressor and inhibit apoptosis. Small molecule activators of SIRT1, such as resveratrol, extend lifespan in yeast and C. elegans in a manner that resembles caloric restriction. CAY10591 has been identified as an activator of the enzyme SIRT1. This compound increases fluorescence by 233% in a SIRT1 activity assay.{14683} [Activator activity was defined as the percentage of signal increase relative to signal window in the following formula: 100 x (Sample – Signallow)/(Signalhigh – Signallow)]. CAY10591 suppresses TNF-α in a dose-dependent manner. In THP-1 cells, TNF-α levels decreased from 325 pg/ml (control) to 104 and 53 pg/ml with 20 and 60 µM CAY10591, respectively. This activator also has a significant dose-dependent effect on fat mobilization in differentiated adipocytes, which would indicate the potential of SIRT1 activators for anti-obesity or anti-diabetic purposes.{14683}  

     

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    Cayman
    SKU:10009797 - 5 mg

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  • Peroxisome proliferator-activated receptors (PPARs) α, δ, γ are ligand-activated nuclear transcription factors involved in the regulation of energy homeostasis as well as insulin sensitivity and glucose metabolism.{14553,16792} Pharmacologies of PPARδ receptor agonists, though relatively obscure, have recently been reported to elevate high-density lipoprotein (HDL) cholesterol and lower plasma triglyceride (TG) levels in obese insulin resistant rhesus monkeys.{11379} CAY10592 is a full PPARδ agonist (EC50 = 30 nM) in a fatty acid oxidation assay of rat L6 muscle cells with desirable oral pharmacokinetic properties.{15689} In a transactivation assay using human PPAR receptors, CAY10592 acts as a selective partial PPARδ agonist (EC50 = 53 nM) with no effect on PPARα or PPARγ activity up to 30 µM.{15689} Chronic treatment of high fat fed ApoB100/CETP-transgenic mice with CAY10592 at a dose of 20 mg/kg increases HDL levels, decreases LDL and TG levels, and improves insulin sensitivity.{15689}  

     

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    Cayman
    SKU:10012536 - 1 mg

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  • Peroxisome proliferator-activated receptors (PPARs) α, δ, γ are ligand-activated nuclear transcription factors involved in the regulation of energy homeostasis as well as insulin sensitivity and glucose metabolism.{14553,16792} Pharmacologies of PPARδ receptor agonists, though relatively obscure, have recently been reported to elevate high-density lipoprotein (HDL) cholesterol and lower plasma triglyceride (TG) levels in obese insulin resistant rhesus monkeys.{11379} CAY10592 is a full PPARδ agonist (EC50 = 30 nM) in a fatty acid oxidation assay of rat L6 muscle cells with desirable oral pharmacokinetic properties.{15689} In a transactivation assay using human PPAR receptors, CAY10592 acts as a selective partial PPARδ agonist (EC50 = 53 nM) with no effect on PPARα or PPARγ activity up to 30 µM.{15689} Chronic treatment of high fat fed ApoB100/CETP-transgenic mice with CAY10592 at a dose of 20 mg/kg increases HDL levels, decreases LDL and TG levels, and improves insulin sensitivity.{15689}  

     

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    Cayman
    SKU:10012536 - 10 mg

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  • Peroxisome proliferator-activated receptors (PPARs) α, δ, γ are ligand-activated nuclear transcription factors involved in the regulation of energy homeostasis as well as insulin sensitivity and glucose metabolism.{14553,16792} Pharmacologies of PPARδ receptor agonists, though relatively obscure, have recently been reported to elevate high-density lipoprotein (HDL) cholesterol and lower plasma triglyceride (TG) levels in obese insulin resistant rhesus monkeys.{11379} CAY10592 is a full PPARδ agonist (EC50 = 30 nM) in a fatty acid oxidation assay of rat L6 muscle cells with desirable oral pharmacokinetic properties.{15689} In a transactivation assay using human PPAR receptors, CAY10592 acts as a selective partial PPARδ agonist (EC50 = 53 nM) with no effect on PPARα or PPARγ activity up to 30 µM.{15689} Chronic treatment of high fat fed ApoB100/CETP-transgenic mice with CAY10592 at a dose of 20 mg/kg increases HDL levels, decreases LDL and TG levels, and improves insulin sensitivity.{15689}  

     

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    Cayman
    SKU:10012536 - 5 mg

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  • Phospholipase D (PLD) is an enzyme which cleaves the head group from phospholipids, producing the second messenger phosphatidic acid. Two mammalian isoforms of PLD, PLD1 and PLD2, have been identified, with multiple splice variants of each. Although the two isoforms share structural and functional features, they are regulated differently and apparently subserve distinct roles. CAY10594 is a potent PLD2 inhibitor, both in vitro (IC50 = 140 nM) and in cells (IC50 = 110 nM).{16821} It is also effective as a PLD1 inhibitor at higher concentrations (IC50 = 5.1 μM in vitro, 1.0 μM in cells).{16821} CAY10594 strongly inhibits the invasive migration of breast cancer cells in transwell assays,{16821} suggesting that PLD might be a useful target in blocking tumor cell invasion.  

     

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    Cayman
    SKU:-
  • Phospholipase D (PLD) is an enzyme which cleaves the head group from phospholipids, producing the second messenger phosphatidic acid. Two mammalian isoforms of PLD, PLD1 and PLD2, have been identified, with multiple splice variants of each. Although the two isoforms share structural and functional features, they are regulated differently and apparently subserve distinct roles. CAY10594 is a potent PLD2 inhibitor, both in vitro (IC50 = 140 nM) and in cells (IC50 = 110 nM).{16821} It is also effective as a PLD1 inhibitor at higher concentrations (IC50 = 5.1 μM in vitro, 1.0 μM in cells).{16821} CAY10594 strongly inhibits the invasive migration of breast cancer cells in transwell assays,{16821} suggesting that PLD might be a useful target in blocking tumor cell invasion.  

     

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    Cayman
    SKU:-
  • Phospholipase D (PLD) is an enzyme which cleaves the head group from phospholipids, producing the second messenger phosphatidic acid. Two mammalian isoforms of PLD, PLD1 and PLD2, have been identified, with multiple splice variants of each. Although the two isoforms share structural and functional features, they are regulated differently and apparently subserve distinct roles. CAY10594 is a potent PLD2 inhibitor, both in vitro (IC50 = 140 nM) and in cells (IC50 = 110 nM).{16821} It is also effective as a PLD1 inhibitor at higher concentrations (IC50 = 5.1 μM in vitro, 1.0 μM in cells).{16821} CAY10594 strongly inhibits the invasive migration of breast cancer cells in transwell assays,{16821} suggesting that PLD might be a useful target in blocking tumor cell invasion.  

     

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    Cayman
    SKU:-
  • Phospholipase D (PLD) is an enzyme which cleaves the head group from phospholipids, producing the second messenger phosphatidic acid. Two mammalian isoforms of PLD, PLD1 and PLD2, have been identified, with multiple splice variants of each. Although the two isoforms share structural and functional features, they are regulated differently and apparently subserve distinct roles. CAY10594 is a potent PLD2 inhibitor, both in vitro (IC50 = 140 nM) and in cells (IC50 = 110 nM).{16821} It is also effective as a PLD1 inhibitor at higher concentrations (IC50 = 5.1 μM in vitro, 1.0 μM in cells).{16821} CAY10594 strongly inhibits the invasive migration of breast cancer cells in transwell assays,{16821} suggesting that PLD might be a useful target in blocking tumor cell invasion.  

     

    Brand:
    Cayman
    SKU:-
  • The biological effects of prostaglandin D2 (PGD2) are transduced by at least two 7-transmembrane G protein-coupled receptors, designated DP1 and CRTH2/DP2. In humans, CRTH2/DP2 is expressed on Th2 cells, eosinophils, and basophils where it mediates the chemotactic activity of PGD2.{9769} CAY10595, as a racemic mixture, is a potent CRTH2/DP2 receptor antagonist that binds to the human receptor with a Ki value of 10 nM.{15596} The R enantiomer of CAY10595 is significantly more potent exhibiting Ki values of 5.3 and 5 nM at the human and murine CRTH2/DP2 receptor, respectively. The R enantiomer of CAY10595 inhibits eosinophil chemotaxis induced by 13,14-dihydro-15-keto-PGD2 with an IC50 value of 7.3 nM.{15596}  

     

    Brand:
    Cayman
    SKU:10012553 - 1 mg

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  • The biological effects of prostaglandin D2 (PGD2) are transduced by at least two 7-transmembrane G protein-coupled receptors, designated DP1 and CRTH2/DP2. In humans, CRTH2/DP2 is expressed on Th2 cells, eosinophils, and basophils where it mediates the chemotactic activity of PGD2.{9769} CAY10595, as a racemic mixture, is a potent CRTH2/DP2 receptor antagonist that binds to the human receptor with a Ki value of 10 nM.{15596} The R enantiomer of CAY10595 is significantly more potent exhibiting Ki values of 5.3 and 5 nM at the human and murine CRTH2/DP2 receptor, respectively. The R enantiomer of CAY10595 inhibits eosinophil chemotaxis induced by 13,14-dihydro-15-keto-PGD2 with an IC50 value of 7.3 nM.{15596}  

     

    Brand:
    Cayman
    SKU:10012553 - 10 mg

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  • The biological effects of prostaglandin D2 (PGD2) are transduced by at least two 7-transmembrane G protein-coupled receptors, designated DP1 and CRTH2/DP2. In humans, CRTH2/DP2 is expressed on Th2 cells, eosinophils, and basophils where it mediates the chemotactic activity of PGD2.{9769} CAY10595, as a racemic mixture, is a potent CRTH2/DP2 receptor antagonist that binds to the human receptor with a Ki value of 10 nM.{15596} The R enantiomer of CAY10595 is significantly more potent exhibiting Ki values of 5.3 and 5 nM at the human and murine CRTH2/DP2 receptor, respectively. The R enantiomer of CAY10595 inhibits eosinophil chemotaxis induced by 13,14-dihydro-15-keto-PGD2 with an IC50 value of 7.3 nM.{15596}  

     

    Brand:
    Cayman
    SKU:10012553 - 5 mg

    Available on backorder

  • The biological effects of prostaglandin D2 (PGD2) are transduced by at least two 7-transmembrane G protein-coupled receptors, designated DP1 and CRTH2/DP2. In humans, CRTH2/DP2 is expressed on Th2 cells, eosinophils, and basophils where it mediates the chemotactic activity of PGD2.{9769} CAY10597, as a racemic mixture, is a potent CRTH2/DP2 receptor antagonist that binds to the human receptor with a Ki value of 37 nM.{15596} The R enantiomer is slightly more potent exhibiting Ki values of 23 and 22 nM at the human and murine CRTH2/DP2 receptor, respectively. The R enantiomer of CAY10597 inhibits eosinophil chemotaxis induced by 13,14-dihydro-15-keto-prostaglandin D2 with an IC50 value of 40 nM.{15596}  

     

    Brand:
    Cayman
    SKU:10012539 - 1 mg

    Available on backorder

  • The biological effects of prostaglandin D2 (PGD2) are transduced by at least two 7-transmembrane G protein-coupled receptors, designated DP1 and CRTH2/DP2. In humans, CRTH2/DP2 is expressed on Th2 cells, eosinophils, and basophils where it mediates the chemotactic activity of PGD2.{9769} CAY10597, as a racemic mixture, is a potent CRTH2/DP2 receptor antagonist that binds to the human receptor with a Ki value of 37 nM.{15596} The R enantiomer is slightly more potent exhibiting Ki values of 23 and 22 nM at the human and murine CRTH2/DP2 receptor, respectively. The R enantiomer of CAY10597 inhibits eosinophil chemotaxis induced by 13,14-dihydro-15-keto-prostaglandin D2 with an IC50 value of 40 nM.{15596}  

     

    Brand:
    Cayman
    SKU:10012539 - 10 mg

    Available on backorder

  • The biological effects of prostaglandin D2 (PGD2) are transduced by at least two 7-transmembrane G protein-coupled receptors, designated DP1 and CRTH2/DP2. In humans, CRTH2/DP2 is expressed on Th2 cells, eosinophils, and basophils where it mediates the chemotactic activity of PGD2.{9769} CAY10597, as a racemic mixture, is a potent CRTH2/DP2 receptor antagonist that binds to the human receptor with a Ki value of 37 nM.{15596} The R enantiomer is slightly more potent exhibiting Ki values of 23 and 22 nM at the human and murine CRTH2/DP2 receptor, respectively. The R enantiomer of CAY10597 inhibits eosinophil chemotaxis induced by 13,14-dihydro-15-keto-prostaglandin D2 with an IC50 value of 40 nM.{15596}  

     

    Brand:
    Cayman
    SKU:10012539 - 5 mg

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  • Prostaglandin E2 (PGE2) activates four E prostanoid (EP) receptors, EP1-4. EP4 is a Gs protein-coupled receptor that, by elevating the second messenger cAMP, plays important roles in bone formation and resorption, cancer, and atherosclerosis.{16772,16773,16619} CAY10598 is a very potent agonist of EP4, binding with a Ki value of 1.2 nM.{16762} Moreover, it does not bind EP1, EP2, EP3, or other prostanoid receptors, including DP, FP, IP, and TP.{16762} First generation EP4 receptor-selective agonists have been shown to reduce inflammation, improve bone healing, provide cardio- and neuroprotection, and reduce renal dysfunction, suggesting some clinical applications for EP4 agonists.{18099,18101,18100,18103,18102}  

     

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    Cayman
    SKU:-
  • Prostaglandin E2 (PGE2) activates four E prostanoid (EP) receptors, EP1-4. EP4 is a Gs protein-coupled receptor that, by elevating the second messenger cAMP, plays important roles in bone formation and resorption, cancer, and atherosclerosis.{16772,16773,16619} CAY10598 is a very potent agonist of EP4, binding with a Ki value of 1.2 nM.{16762} Moreover, it does not bind EP1, EP2, EP3, or other prostanoid receptors, including DP, FP, IP, and TP.{16762} First generation EP4 receptor-selective agonists have been shown to reduce inflammation, improve bone healing, provide cardio- and neuroprotection, and reduce renal dysfunction, suggesting some clinical applications for EP4 agonists.{18099,18101,18100,18103,18102}  

     

    Brand:
    Cayman
    SKU:-
  • Prostaglandin E2 (PGE2) activates four E prostanoid (EP) receptors, EP1-4. EP4 is a Gs protein-coupled receptor that, by elevating the second messenger cAMP, plays important roles in bone formation and resorption, cancer, and atherosclerosis.{16772,16773,16619} CAY10598 is a very potent agonist of EP4, binding with a Ki value of 1.2 nM.{16762} Moreover, it does not bind EP1, EP2, EP3, or other prostanoid receptors, including DP, FP, IP, and TP.{16762} First generation EP4 receptor-selective agonists have been shown to reduce inflammation, improve bone healing, provide cardio- and neuroprotection, and reduce renal dysfunction, suggesting some clinical applications for EP4 agonists.{18099,18101,18100,18103,18102}  

     

    Brand:
    Cayman
    SKU:-
  • Prostaglandin E2 (PGE2) activates four E prostanoid (EP) receptors, EP1-4. EP4 is a Gs protein-coupled receptor that, by elevating the second messenger cAMP, plays important roles in bone formation and resorption, cancer, and atherosclerosis.{16772,16773,16619} CAY10598 is a very potent agonist of EP4, binding with a Ki value of 1.2 nM.{16762} Moreover, it does not bind EP1, EP2, EP3, or other prostanoid receptors, including DP, FP, IP, and TP.{16762} First generation EP4 receptor-selective agonists have been shown to reduce inflammation, improve bone healing, provide cardio- and neuroprotection, and reduce renal dysfunction, suggesting some clinical applications for EP4 agonists.{18099,18101,18100,18103,18102}  

     

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    Cayman
    SKU:-
  • Thiazolidinediones (TZDs) are a group of structurally related peroxisome proliferator-activated receptor γ (PPARγ) agonists with antidiabetic actions in vivo.{7575,8930} The prototypical compound for this class is the TZD rosiglitazone (BRL 49653), which is currently marketed for the treatment of diabetes. CAY10599 is a PPARγ agonist that is 4-fold more potent than rosiglitazone at the PPARγ receptor demonstrating an EC50 value of 0.05 µM.{17110} This compound shows high selectivity for PPARγ over PPARα (EC50 = 3.99 µM) or PPARδ (EC50 > 10 µM).{17110}  

     

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    Cayman
    SKU:-
  • Thiazolidinediones (TZDs) are a group of structurally related peroxisome proliferator-activated receptor γ (PPARγ) agonists with antidiabetic actions in vivo.{7575,8930} The prototypical compound for this class is the TZD rosiglitazone (BRL 49653), which is currently marketed for the treatment of diabetes. CAY10599 is a PPARγ agonist that is 4-fold more potent than rosiglitazone at the PPARγ receptor demonstrating an EC50 value of 0.05 µM.{17110} This compound shows high selectivity for PPARγ over PPARα (EC50 = 3.99 µM) or PPARδ (EC50 > 10 µM).{17110}  

     

    Brand:
    Cayman
    SKU:-
  • Thiazolidinediones (TZDs) are a group of structurally related peroxisome proliferator-activated receptor γ (PPARγ) agonists with antidiabetic actions in vivo.{7575,8930} The prototypical compound for this class is the TZD rosiglitazone (BRL 49653), which is currently marketed for the treatment of diabetes. CAY10599 is a PPARγ agonist that is 4-fold more potent than rosiglitazone at the PPARγ receptor demonstrating an EC50 value of 0.05 µM.{17110} This compound shows high selectivity for PPARγ over PPARα (EC50 = 3.99 µM) or PPARδ (EC50 > 10 µM).{17110}  

     

    Brand:
    Cayman
    SKU:-
  • Thiazolidinediones (TZDs) are a group of structurally related peroxisome proliferator-activated receptor γ (PPARγ) agonists with antidiabetic actions in vivo.{7575,8930} The prototypical compound for this class is the TZD rosiglitazone (BRL 49653), which is currently marketed for the treatment of diabetes. CAY10599 is a PPARγ agonist that is 4-fold more potent than rosiglitazone at the PPARγ receptor demonstrating an EC50 value of 0.05 µM.{17110} This compound shows high selectivity for PPARγ over PPARα (EC50 = 3.99 µM) or PPARδ (EC50 > 10 µM).{17110}  

     

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    Cayman
    SKU:-
  • Sirtuin 1 (SIRT1) is an evolutionarily conserved NAD-dependent protein deacetylase that has been implicated in cell metabolism, differentiation, stress and DNA damage response, and the control of multidrug resistance in cancer. SIRT1 alters gene expression by deacetylating nuclear histones, NF-κB, p53, and FOXO transcription factors. CAY10602 was derived from high throughput screening for compounds that increase SIRT1-mediated deacetylation of a SIRT1-specific substrate.{14683} Functional assays show that CAY10602 dose-dependently suppresses the NF-κB-dependent induction of TNF-α by lipopolysaccharide in THP-1 cells, with approximately 75% inhibition achieved at 60 μM, without cytotoxicity.{14683} CAY10602 is at least 10 times more potent as a suppressor of TNF-α release than resveratrol. The effects of CAY10602 in other cellular processes remain to be determined.  

     

    Brand:
    Cayman
    SKU:10009796 - 10 mg

    Available on backorder

  • Sirtuin 1 (SIRT1) is an evolutionarily conserved NAD-dependent protein deacetylase that has been implicated in cell metabolism, differentiation, stress and DNA damage response, and the control of multidrug resistance in cancer. SIRT1 alters gene expression by deacetylating nuclear histones, NF-κB, p53, and FOXO transcription factors. CAY10602 was derived from high throughput screening for compounds that increase SIRT1-mediated deacetylation of a SIRT1-specific substrate.{14683} Functional assays show that CAY10602 dose-dependently suppresses the NF-κB-dependent induction of TNF-α by lipopolysaccharide in THP-1 cells, with approximately 75% inhibition achieved at 60 μM, without cytotoxicity.{14683} CAY10602 is at least 10 times more potent as a suppressor of TNF-α release than resveratrol. The effects of CAY10602 in other cellular processes remain to be determined.  

     

    Brand:
    Cayman
    SKU:10009796 - 100 mg

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  • Sirtuin 1 (SIRT1) is an evolutionarily conserved NAD-dependent protein deacetylase that has been implicated in cell metabolism, differentiation, stress and DNA damage response, and the control of multidrug resistance in cancer. SIRT1 alters gene expression by deacetylating nuclear histones, NF-κB, p53, and FOXO transcription factors. CAY10602 was derived from high throughput screening for compounds that increase SIRT1-mediated deacetylation of a SIRT1-specific substrate.{14683} Functional assays show that CAY10602 dose-dependently suppresses the NF-κB-dependent induction of TNF-α by lipopolysaccharide in THP-1 cells, with approximately 75% inhibition achieved at 60 μM, without cytotoxicity.{14683} CAY10602 is at least 10 times more potent as a suppressor of TNF-α release than resveratrol. The effects of CAY10602 in other cellular processes remain to be determined.  

     

    Brand:
    Cayman
    SKU:10009796 - 5 mg

    Available on backorder

  • Sirtuin 1 (SIRT1) is an evolutionarily conserved NAD-dependent protein deacetylase that has been implicated in cell metabolism, differentiation, stress and DNA damage response, and the control of multidrug resistance in cancer. SIRT1 alters gene expression by deacetylating nuclear histones, NF-κB, p53, and FOXO transcription factors. CAY10602 was derived from high throughput screening for compounds that increase SIRT1-mediated deacetylation of a SIRT1-specific substrate.{14683} Functional assays show that CAY10602 dose-dependently suppresses the NF-κB-dependent induction of TNF-α by lipopolysaccharide in THP-1 cells, with approximately 75% inhibition achieved at 60 μM, without cytotoxicity.{14683} CAY10602 is at least 10 times more potent as a suppressor of TNF-α release than resveratrol. The effects of CAY10602 in other cellular processes remain to be determined.  

     

    Brand:
    Cayman
    SKU:10009796 - 50 mg

    Available on backorder

  • Histone deacetylase 6 (HDAC6) is a class II HDAC that represses transcription by removing acetyl groups from histones. In addition, HDAC6 deacetylases tubulin, which is important in regulating microtubule stability and function. CAY10603 is a potent and selective inhibitor of HDAC6 (IC50 = 0.002 nM, as compared with 271, 252, 0.42, 6851, and 90.7 nM for HDAC1, 2, 3, 8, and 10, respectively).{16594} Also, CAY10603 prevents the growth of several pancreatic cancer cell lines (IC50 = 0.1-1 μM).{16594} The HDAC6 inhibitor is more active in inhibiting cell growth than the broad spectrum HDAC inhibitor suberoylanilide hydroxamic acid (SAHA).  

     

    Brand:
    Cayman
    SKU:-
  • Histone deacetylase 6 (HDAC6) is a class II HDAC that represses transcription by removing acetyl groups from histones. In addition, HDAC6 deacetylases tubulin, which is important in regulating microtubule stability and function. CAY10603 is a potent and selective inhibitor of HDAC6 (IC50 = 0.002 nM, as compared with 271, 252, 0.42, 6851, and 90.7 nM for HDAC1, 2, 3, 8, and 10, respectively).{16594} Also, CAY10603 prevents the growth of several pancreatic cancer cell lines (IC50 = 0.1-1 μM).{16594} The HDAC6 inhibitor is more active in inhibiting cell growth than the broad spectrum HDAC inhibitor suberoylanilide hydroxamic acid (SAHA).  

     

    Brand:
    Cayman
    SKU:-
  • Histone deacetylase 6 (HDAC6) is a class II HDAC that represses transcription by removing acetyl groups from histones. In addition, HDAC6 deacetylases tubulin, which is important in regulating microtubule stability and function. CAY10603 is a potent and selective inhibitor of HDAC6 (IC50 = 0.002 nM, as compared with 271, 252, 0.42, 6851, and 90.7 nM for HDAC1, 2, 3, 8, and 10, respectively).{16594} Also, CAY10603 prevents the growth of several pancreatic cancer cell lines (IC50 = 0.1-1 μM).{16594} The HDAC6 inhibitor is more active in inhibiting cell growth than the broad spectrum HDAC inhibitor suberoylanilide hydroxamic acid (SAHA).  

     

    Brand:
    Cayman
    SKU:-
  • Histone deacetylase 6 (HDAC6) is a class II HDAC that represses transcription by removing acetyl groups from histones. In addition, HDAC6 deacetylases tubulin, which is important in regulating microtubule stability and function. CAY10603 is a potent and selective inhibitor of HDAC6 (IC50 = 0.002 nM, as compared with 271, 252, 0.42, 6851, and 90.7 nM for HDAC1, 2, 3, 8, and 10, respectively).{16594} Also, CAY10603 prevents the growth of several pancreatic cancer cell lines (IC50 = 0.1-1 μM).{16594} The HDAC6 inhibitor is more active in inhibiting cell growth than the broad spectrum HDAC inhibitor suberoylanilide hydroxamic acid (SAHA).  

     

    Brand:
    Cayman
    SKU:-
  • 5-Lipoxygenase (5-LO) initiates the synthesis of leukotrienes (LTs) from arachidonic acid, primarily in certain leukocyte populations. CAY10606 is a potent, reversible inhibitor of 5-LO, both in cell-free assays (IC50 = 86 nM) and in intact neutrophils (IC50 = 230 nM).{17244} It prevents the production of LTs in whole blood, whether 5-LO is activated with the calcium ionophore A23187 (IC50 = 1.6 μM) or formyl peptide (fMLP) following priming with lipopolysaccharide (IC50 = 830 nM). In rats subjected to carrageenan-induced pleurisy, CAY10606 significantly reduces both LT biosynthesis and the inflammatory reaction.{17244}  

     

    Brand:
    Cayman
    SKU:-
  • 5-Lipoxygenase (5-LO) initiates the synthesis of leukotrienes (LTs) from arachidonic acid, primarily in certain leukocyte populations. CAY10606 is a potent, reversible inhibitor of 5-LO, both in cell-free assays (IC50 = 86 nM) and in intact neutrophils (IC50 = 230 nM).{17244} It prevents the production of LTs in whole blood, whether 5-LO is activated with the calcium ionophore A23187 (IC50 = 1.6 μM) or formyl peptide (fMLP) following priming with lipopolysaccharide (IC50 = 830 nM). In rats subjected to carrageenan-induced pleurisy, CAY10606 significantly reduces both LT biosynthesis and the inflammatory reaction.{17244}  

     

    Brand:
    Cayman
    SKU:-
  • 5-Lipoxygenase (5-LO) initiates the synthesis of leukotrienes (LTs) from arachidonic acid, primarily in certain leukocyte populations. CAY10606 is a potent, reversible inhibitor of 5-LO, both in cell-free assays (IC50 = 86 nM) and in intact neutrophils (IC50 = 230 nM).{17244} It prevents the production of LTs in whole blood, whether 5-LO is activated with the calcium ionophore A23187 (IC50 = 1.6 μM) or formyl peptide (fMLP) following priming with lipopolysaccharide (IC50 = 830 nM). In rats subjected to carrageenan-induced pleurisy, CAY10606 significantly reduces both LT biosynthesis and the inflammatory reaction.{17244}  

     

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    Cayman
    SKU:-
  • N-Methyl-D-aspartate (NMDA) receptors are Ca2+ permeable ligand-gated channels of the central nervous system that are activated after binding of the co-agonists glutamate and glycine. CAY10608 is a propanolamine that potently, selectively, and non-competitively antagonizes the NR2B subunit of NMDA receptors (IC50 = 50 nM).{18096} It does not inhibit NR1, NR2A, NR2C, and NR2D subunits and has no significant effects on α-amino-3-hydroxy-5-methyl-4-isoxazolepropioinic acid (AMPA) or kainate receptors.{18096} CAY10608 is neuroprotective, since it prevents NMDA-triggered release of lactate dehydrogenase from cultured cortical neurons. Also, CAY10608, when administered intraperitoneally, reduces brain infarct volume resulting from transient ischemia via carotid artery occlusion.{18096}  

     

    Brand:
    Cayman
    SKU:-
  • N-Methyl-D-aspartate (NMDA) receptors are Ca2+ permeable ligand-gated channels of the central nervous system that are activated after binding of the co-agonists glutamate and glycine. CAY10608 is a propanolamine that potently, selectively, and non-competitively antagonizes the NR2B subunit of NMDA receptors (IC50 = 50 nM).{18096} It does not inhibit NR1, NR2A, NR2C, and NR2D subunits and has no significant effects on α-amino-3-hydroxy-5-methyl-4-isoxazolepropioinic acid (AMPA) or kainate receptors.{18096} CAY10608 is neuroprotective, since it prevents NMDA-triggered release of lactate dehydrogenase from cultured cortical neurons. Also, CAY10608, when administered intraperitoneally, reduces brain infarct volume resulting from transient ischemia via carotid artery occlusion.{18096}  

     

    Brand:
    Cayman
    SKU:-