Cayman

Showing 26401–26550 of 45550 results

  • KJ Pyr 9 is a cell-permeable inhibitor of c-Myc (Kd = 6.5 nM) that interferes with Myc-Max complex formation in cells.{31163,31164} It preferentially blocks the proliferation of c-Myc-overexpressing cells, reducing Myc-driven gene expression.{31163} KJ Pyr 9 also potently blocks cell growth directed by overexpression of v-Myc, while less effectively blocking N-Myc- and L-Myc-dependent proliferation.{31164} It is effective in vivo, reducing the growth of breast cancer MDA-MB-231 xenografts in mice.{31163}  

     

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  • KJ Pyr 9 is a cell-permeable inhibitor of c-Myc (Kd = 6.5 nM) that interferes with Myc-Max complex formation in cells.{31163,31164} It preferentially blocks the proliferation of c-Myc-overexpressing cells, reducing Myc-driven gene expression.{31163} KJ Pyr 9 also potently blocks cell growth directed by overexpression of v-Myc, while less effectively blocking N-Myc- and L-Myc-dependent proliferation.{31164} It is effective in vivo, reducing the growth of breast cancer MDA-MB-231 xenografts in mice.{31163}  

     

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  • KJ Pyr 9 is a cell-permeable inhibitor of c-Myc (Kd = 6.5 nM) that interferes with Myc-Max complex formation in cells.{31163,31164} It preferentially blocks the proliferation of c-Myc-overexpressing cells, reducing Myc-driven gene expression.{31163} KJ Pyr 9 also potently blocks cell growth directed by overexpression of v-Myc, while less effectively blocking N-Myc- and L-Myc-dependent proliferation.{31164} It is effective in vivo, reducing the growth of breast cancer MDA-MB-231 xenografts in mice.{31163}  

     

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  • The cryptochrome proteins CRY1 and CRY2, which play central roles in maintaining the circadian clock, are expressed and then degraded in a rhythmic pattern.{14833,21468} KL001 is a cell-permeable carbazolic compound which directly interacts with and stabilizes CRY1 and CRY2, preventing ubiquitin-dependent degradation while lengthening the circadian period (IC50 = 0.82-14 μM).{21468} As the expression of some gluconeogenic genes is both circadian and cryptochrome-dependent, KL001 effectively inhibits glucagon-induced gluconeogenesis in primary hepatocytes.{21468} This product can be used to study the regulation of cryptochrome-dependent physiology and aid in the development of clock-based therapeutics of diabetes.  

     

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  • The cryptochrome proteins CRY1 and CRY2, which play central roles in maintaining the circadian clock, are expressed and then degraded in a rhythmic pattern.{14833,21468} KL001 is a cell-permeable carbazolic compound which directly interacts with and stabilizes CRY1 and CRY2, preventing ubiquitin-dependent degradation while lengthening the circadian period (IC50 = 0.82-14 μM).{21468} As the expression of some gluconeogenic genes is both circadian and cryptochrome-dependent, KL001 effectively inhibits glucagon-induced gluconeogenesis in primary hepatocytes.{21468} This product can be used to study the regulation of cryptochrome-dependent physiology and aid in the development of clock-based therapeutics of diabetes.  

     

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  • The cryptochrome proteins CRY1 and CRY2, which play central roles in maintaining the circadian clock, are expressed and then degraded in a rhythmic pattern.{14833,21468} KL001 is a cell-permeable carbazolic compound which directly interacts with and stabilizes CRY1 and CRY2, preventing ubiquitin-dependent degradation while lengthening the circadian period (IC50 = 0.82-14 μM).{21468} As the expression of some gluconeogenic genes is both circadian and cryptochrome-dependent, KL001 effectively inhibits glucagon-induced gluconeogenesis in primary hepatocytes.{21468} This product can be used to study the regulation of cryptochrome-dependent physiology and aid in the development of clock-based therapeutics of diabetes.  

     

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  • The rabbit anti-KLH polyclonal antibody is intended for use as a negative control rabbit antibody for use with experiments utilizing a primary antibody from rabbit. It may also be used to detect KLH from biological samples. This antibody has a detection limit for KLH to the low nanogram level but little or no cross reactivity to protein samples (cell or tissue lysates) derived from mammals.  

     

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    SKU:14046 - 1 ea

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  • Immunogen: KLH protein • Host: Rabbit • Applications: ELISA and WB  

     

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    SKU:14046- 1 ea

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  • Immunogen: KLH protein • Host: Rabbit • Applications: ELISA and WB  

     

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    Cayman
    SKU:14046- 1 ea
  • KLH45 is an inhibitor of the phospholipase DDHD domain containing 2 (DDHD2; IC50 = 1.3 nM).{43899} It is selective for DDHD2 over greater than 50 serine hydrolases, including DDHD1 and Sec23ip, but does inhibit α/β-hydrolase domain-containing protein 6 (ABHD6). It inhibits DDHD2 and ABHD6 in Neuro2A cells when used at a concentration of less than 10 nM and inhibits DDHD2 by greater than 95% at a concentration of 25 nM. KLH45 (2 µM) prevents increases in triacylglycerol (TAG) hydrolase activity in HEK293T cell lysates expressing recombinant DDHD2 and incubated with a radiolabeled TAG substrate. It decreases TAG levels in the CNS of mice when administered at a dose of 20 mg/kg twice per day for four days. KLH45 (2 µM) also reverses DDHD2-induced lipid droplet reduction in COS-7 cells expressing recombinant DDHD2 and loaded with oleic acid.{43900}  

     

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    SKU:19889 -

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  • KLH45 is an inhibitor of the phospholipase DDHD domain containing 2 (DDHD2; IC50 = 1.3 nM).{43899} It is selective for DDHD2 over greater than 50 serine hydrolases, including DDHD1 and Sec23ip, but does inhibit α/β-hydrolase domain-containing protein 6 (ABHD6). It inhibits DDHD2 and ABHD6 in Neuro2A cells when used at a concentration of less than 10 nM and inhibits DDHD2 by greater than 95% at a concentration of 25 nM. KLH45 (2 µM) prevents increases in triacylglycerol (TAG) hydrolase activity in HEK293T cell lysates expressing recombinant DDHD2 and incubated with a radiolabeled TAG substrate. It decreases TAG levels in the CNS of mice when administered at a dose of 20 mg/kg twice per day for four days. KLH45 (2 µM) also reverses DDHD2-induced lipid droplet reduction in COS-7 cells expressing recombinant DDHD2 and loaded with oleic acid.{43900}  

     

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    SKU:19889 -

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  • KLH45 is an inhibitor of the phospholipase DDHD domain containing 2 (DDHD2; IC50 = 1.3 nM).{43899} It is selective for DDHD2 over greater than 50 serine hydrolases, including DDHD1 and Sec23ip, but does inhibit α/β-hydrolase domain-containing protein 6 (ABHD6). It inhibits DDHD2 and ABHD6 in Neuro2A cells when used at a concentration of less than 10 nM and inhibits DDHD2 by greater than 95% at a concentration of 25 nM. KLH45 (2 µM) prevents increases in triacylglycerol (TAG) hydrolase activity in HEK293T cell lysates expressing recombinant DDHD2 and incubated with a radiolabeled TAG substrate. It decreases TAG levels in the CNS of mice when administered at a dose of 20 mg/kg twice per day for four days. KLH45 (2 µM) also reverses DDHD2-induced lipid droplet reduction in COS-7 cells expressing recombinant DDHD2 and loaded with oleic acid.{43900}  

     

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    Cayman
    SKU:19889 -

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  • KLH45 is an inhibitor of the phospholipase DDHD domain containing 2 (DDHD2; IC50 = 1.3 nM).{43899} It is selective for DDHD2 over greater than 50 serine hydrolases, including DDHD1 and Sec23ip, but does inhibit α/β-hydrolase domain-containing protein 6 (ABHD6). It inhibits DDHD2 and ABHD6 in Neuro2A cells when used at a concentration of less than 10 nM and inhibits DDHD2 by greater than 95% at a concentration of 25 nM. KLH45 (2 µM) prevents increases in triacylglycerol (TAG) hydrolase activity in HEK293T cell lysates expressing recombinant DDHD2 and incubated with a radiolabeled TAG substrate. It decreases TAG levels in the CNS of mice when administered at a dose of 20 mg/kg twice per day for four days. KLH45 (2 µM) also reverses DDHD2-induced lipid droplet reduction in COS-7 cells expressing recombinant DDHD2 and loaded with oleic acid.{43900}  

     

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    SKU:19889 -

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  • KM 11060 is a small molecule that corrects the processing of cystic fibrosis transmembrane conductance regulator (CFTR) proteins bearing the F508 deletion (F508del) mutation carried by 90% of cystic fibrosis patients.{36264} It increases cell surface expression and restores chloride transport function of F508del-CFTRs in BHK cells at a concentration of 10 μM. KM 11060 restores F508del-CFTR function, as measured by cAMP-stimulated iodide efflux, in CFBE41o- human airway epithelial cells at a concentration of 10 nM. It also restores the secretory response to approximately 51% of wild-type levels ex vivo in ileum isolated from F508del-CFTR mice at a concentration of 20 μM.  

     

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    Cayman
    SKU:23481 - 10 mg

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  • KM 11060 is a small molecule that corrects the processing of cystic fibrosis transmembrane conductance regulator (CFTR) proteins bearing the F508 deletion (F508del) mutation carried by 90% of cystic fibrosis patients.{36264} It increases cell surface expression and restores chloride transport function of F508del-CFTRs in BHK cells at a concentration of 10 μM. KM 11060 restores F508del-CFTR function, as measured by cAMP-stimulated iodide efflux, in CFBE41o- human airway epithelial cells at a concentration of 10 nM. It also restores the secretory response to approximately 51% of wild-type levels ex vivo in ileum isolated from F508del-CFTR mice at a concentration of 20 μM.  

     

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    Cayman
    SKU:23481 - 25 mg

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  • KM 11060 is a small molecule that corrects the processing of cystic fibrosis transmembrane conductance regulator (CFTR) proteins bearing the F508 deletion (F508del) mutation carried by 90% of cystic fibrosis patients.{36264} It increases cell surface expression and restores chloride transport function of F508del-CFTRs in BHK cells at a concentration of 10 μM. KM 11060 restores F508del-CFTR function, as measured by cAMP-stimulated iodide efflux, in CFBE41o- human airway epithelial cells at a concentration of 10 nM. It also restores the secretory response to approximately 51% of wild-type levels ex vivo in ileum isolated from F508del-CFTR mice at a concentration of 20 μM.  

     

    Brand:
    Cayman
    SKU:23481 - 5 mg

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  • KM 11060 is a small molecule that corrects the processing of cystic fibrosis transmembrane conductance regulator (CFTR) proteins bearing the F508 deletion (F508del) mutation carried by 90% of cystic fibrosis patients.{36264} It increases cell surface expression and restores chloride transport function of F508del-CFTRs in BHK cells at a concentration of 10 μM. KM 11060 restores F508del-CFTR function, as measured by cAMP-stimulated iodide efflux, in CFBE41o- human airway epithelial cells at a concentration of 10 nM. It also restores the secretory response to approximately 51% of wild-type levels ex vivo in ileum isolated from F508del-CFTR mice at a concentration of 20 μM.  

     

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    Cayman
    SKU:23481 - 50 mg

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  • Because selective activation of peripheral cannabinoid (CB2) receptors in rat C-6 glioma cells has been shown to induce apoptosis through enhanced ceramide synthesis de novo, CB2 agonists present potential as anti glioma agents.{19828} KM 233 is a Δ8-tetrahydrocannabinol analog with a dimethyl substitution that exhibits high binding affinity for both the CB1 and CB2 receptors with 13-fold selectivity for the CB2 receptor (Kis = 12.3 and 0.91 nM, respectively).{19834} Demonstrating good lipophilicity and ability to penetrate the blood brain barrier, KM 233 inhibits human U87 glioma cell proliferation in vitro with an IC50 value of 1.4 μM and significantly reduces U87 glioma tumor size in vivo at a dose of 2 mg/kg in a SCID mouse xenograft side-pocket model.{19835}  

     

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    Cayman
    SKU:10640 - 1 mg

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  • Because selective activation of peripheral cannabinoid (CB2) receptors in rat C-6 glioma cells has been shown to induce apoptosis through enhanced ceramide synthesis de novo, CB2 agonists present potential as anti glioma agents.{19828} KM 233 is a Δ8-tetrahydrocannabinol analog with a dimethyl substitution that exhibits high binding affinity for both the CB1 and CB2 receptors with 13-fold selectivity for the CB2 receptor (Kis = 12.3 and 0.91 nM, respectively).{19834} Demonstrating good lipophilicity and ability to penetrate the blood brain barrier, KM 233 inhibits human U87 glioma cell proliferation in vitro with an IC50 value of 1.4 μM and significantly reduces U87 glioma tumor size in vivo at a dose of 2 mg/kg in a SCID mouse xenograft side-pocket model.{19835}  

     

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    Cayman
    SKU:10640 - 10 mg

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  • Because selective activation of peripheral cannabinoid (CB2) receptors in rat C-6 glioma cells has been shown to induce apoptosis through enhanced ceramide synthesis de novo, CB2 agonists present potential as anti glioma agents.{19828} KM 233 is a Δ8-tetrahydrocannabinol analog with a dimethyl substitution that exhibits high binding affinity for both the CB1 and CB2 receptors with 13-fold selectivity for the CB2 receptor (Kis = 12.3 and 0.91 nM, respectively).{19834} Demonstrating good lipophilicity and ability to penetrate the blood brain barrier, KM 233 inhibits human U87 glioma cell proliferation in vitro with an IC50 value of 1.4 μM and significantly reduces U87 glioma tumor size in vivo at a dose of 2 mg/kg in a SCID mouse xenograft side-pocket model.{19835}  

     

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    Cayman
    SKU:10640 - 25 mg

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  • Because selective activation of peripheral cannabinoid (CB2) receptors in rat C-6 glioma cells has been shown to induce apoptosis through enhanced ceramide synthesis de novo, CB2 agonists present potential as anti glioma agents.{19828} KM 233 is a Δ8-tetrahydrocannabinol analog with a dimethyl substitution that exhibits high binding affinity for both the CB1 and CB2 receptors with 13-fold selectivity for the CB2 receptor (Kis = 12.3 and 0.91 nM, respectively).{19834} Demonstrating good lipophilicity and ability to penetrate the blood brain barrier, KM 233 inhibits human U87 glioma cell proliferation in vitro with an IC50 value of 1.4 μM and significantly reduces U87 glioma tumor size in vivo at a dose of 2 mg/kg in a SCID mouse xenograft side-pocket model.{19835}  

     

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    Cayman
    SKU:10640 - 5 mg

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  • Endocannabinoids such as 2-arachidonoyl glycerol (2-AG) and arachidonoyl ethanolamide are biologically active lipids that are involved in a number of synaptic processes including activation of cannabinoid receptors. Monoacylglycerol lipase (MAGL) is a serine hydrolase responsible for the hydrolysis of 2-AG to arachidonic acid and glycerol, thus terminating its biological function. KML29 is an O-hexafluoroisopropyl carbamate analog of JZL 184 (Item No. 13158) that potently and selectively inhibits MAGL (IC50s = 15, 43, and 5.9 nM in mouse, rat, and human brain proteomes, respectively) over FAAH (IC50s >50 μM).{20923} At 5-20 mg/kg, KML29 dose-dependently blocks mouse brain MAGL activity in vivo, without any measurable effect on FAAH activity.{20923} As a second generation MAGL inhibitor, KML29 supersedes the low-level cross reactivity that JZL 184 displays for FAAH yet still maintains comparable potency to its parent compound.  

     

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    Cayman
    SKU:11777 - 10 mg

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  • Endocannabinoids such as 2-arachidonoyl glycerol (2-AG) and arachidonoyl ethanolamide are biologically active lipids that are involved in a number of synaptic processes including activation of cannabinoid receptors. Monoacylglycerol lipase (MAGL) is a serine hydrolase responsible for the hydrolysis of 2-AG to arachidonic acid and glycerol, thus terminating its biological function. KML29 is an O-hexafluoroisopropyl carbamate analog of JZL 184 (Item No. 13158) that potently and selectively inhibits MAGL (IC50s = 15, 43, and 5.9 nM in mouse, rat, and human brain proteomes, respectively) over FAAH (IC50s >50 μM).{20923} At 5-20 mg/kg, KML29 dose-dependently blocks mouse brain MAGL activity in vivo, without any measurable effect on FAAH activity.{20923} As a second generation MAGL inhibitor, KML29 supersedes the low-level cross reactivity that JZL 184 displays for FAAH yet still maintains comparable potency to its parent compound.  

     

    Brand:
    Cayman
    SKU:11777 - 100 mg

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  • Endocannabinoids such as 2-arachidonoyl glycerol (2-AG) and arachidonoyl ethanolamide are biologically active lipids that are involved in a number of synaptic processes including activation of cannabinoid receptors. Monoacylglycerol lipase (MAGL) is a serine hydrolase responsible for the hydrolysis of 2-AG to arachidonic acid and glycerol, thus terminating its biological function. KML29 is an O-hexafluoroisopropyl carbamate analog of JZL 184 (Item No. 13158) that potently and selectively inhibits MAGL (IC50s = 15, 43, and 5.9 nM in mouse, rat, and human brain proteomes, respectively) over FAAH (IC50s >50 μM).{20923} At 5-20 mg/kg, KML29 dose-dependently blocks mouse brain MAGL activity in vivo, without any measurable effect on FAAH activity.{20923} As a second generation MAGL inhibitor, KML29 supersedes the low-level cross reactivity that JZL 184 displays for FAAH yet still maintains comparable potency to its parent compound.  

     

    Brand:
    Cayman
    SKU:11777 - 5 mg

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  • Endocannabinoids such as 2-arachidonoyl glycerol (2-AG) and arachidonoyl ethanolamide are biologically active lipids that are involved in a number of synaptic processes including activation of cannabinoid receptors. Monoacylglycerol lipase (MAGL) is a serine hydrolase responsible for the hydrolysis of 2-AG to arachidonic acid and glycerol, thus terminating its biological function. KML29 is an O-hexafluoroisopropyl carbamate analog of JZL 184 (Item No. 13158) that potently and selectively inhibits MAGL (IC50s = 15, 43, and 5.9 nM in mouse, rat, and human brain proteomes, respectively) over FAAH (IC50s >50 μM).{20923} At 5-20 mg/kg, KML29 dose-dependently blocks mouse brain MAGL activity in vivo, without any measurable effect on FAAH activity.{20923} As a second generation MAGL inhibitor, KML29 supersedes the low-level cross reactivity that JZL 184 displays for FAAH yet still maintains comparable potency to its parent compound.  

     

    Brand:
    Cayman
    SKU:11777 - 50 mg

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  • The prostaglandin E receptor 4 (EP4) is one of four G protein-coupled receptors that mediate the actions of prostaglandin E2 (PGE2; Item No. 14010). Binding of PGE2 to the EP4 receptor causes an increase in intracellular cyclic AMP, which plays important roles in bone formation and resorption, cancer, and atherosclerosis.{16772,16773,16619,24126} KMN-80 is a substituted γ-lactam (pyrrolidinone) derivative of PGE1 (Item No. 13010) that acts as a selective and potent agonist of EP4 with an IC50 value of 3 nM (IC50 = 1.4 μM for EP3 and > 10 μM for all other prostanoid receptors).{25026} In functional assays it has been shown to stimulate secreted alkaline phosphatase gene reporter activity in EP4-transfected HEK293 cells with an EC50 value of 0.19 nM, demonstrating >5,000 and 50,000-fold selectivity against EP2 and TP, respectively.{25026} KMN-80 can induce the differentiation of bone marrow stem cells from both young and aged rats into osteoblasts in vitro (EC50s = 20 and 153 nM, respectively) and exhibits favorable tolerability up to at least 10 μM, whereas the EP4 agonist L-902,688 (Item No. 10007712) is highly cytotoxic at similar concentrations in these cells.{25027} KMN-80 has been used to repair calvarial defects in an in vivo rat craniomaxillofacial reconstruction model (rate of reduction in defect size equivalent to BMP-2 treated rats) and to promote bone formation in a rat incisor tooth socket model.{25027}  

     

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  • The prostaglandin E receptor 4 (EP4) is one of four G protein-coupled receptors that mediate the actions of prostaglandin E2 (PGE2; Item No. 14010). Binding of PGE2 to the EP4 receptor causes an increase in intracellular cyclic AMP, which plays important roles in bone formation and resorption, cancer, and atherosclerosis.{16772,16773,16619,24126} KMN-80 is a substituted γ-lactam (pyrrolidinone) derivative of PGE1 (Item No. 13010) that acts as a selective and potent agonist of EP4 with an IC50 value of 3 nM (IC50 = 1.4 μM for EP3 and > 10 μM for all other prostanoid receptors).{25026} In functional assays it has been shown to stimulate secreted alkaline phosphatase gene reporter activity in EP4-transfected HEK293 cells with an EC50 value of 0.19 nM, demonstrating >5,000 and 50,000-fold selectivity against EP2 and TP, respectively.{25026} KMN-80 can induce the differentiation of bone marrow stem cells from both young and aged rats into osteoblasts in vitro (EC50s = 20 and 153 nM, respectively) and exhibits favorable tolerability up to at least 10 μM, whereas the EP4 agonist L-902,688 (Item No. 10007712) is highly cytotoxic at similar concentrations in these cells.{25027} KMN-80 has been used to repair calvarial defects in an in vivo rat craniomaxillofacial reconstruction model (rate of reduction in defect size equivalent to BMP-2 treated rats) and to promote bone formation in a rat incisor tooth socket model.{25027}  

     

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  • The prostaglandin E receptor 4 (EP4) is one of four G protein-coupled receptors that mediate the actions of prostaglandin E2 (PGE2; Item No. 14010). Binding of PGE2 to the EP4 receptor causes an increase in intracellular cyclic AMP, which plays important roles in bone formation and resorption, cancer, and atherosclerosis.{16772,16773,16619,24126} KMN-80 is a substituted γ-lactam (pyrrolidinone) derivative of PGE1 (Item No. 13010) that acts as a selective and potent agonist of EP4 with an IC50 value of 3 nM (IC50 = 1.4 μM for EP3 and > 10 μM for all other prostanoid receptors).{25026} In functional assays it has been shown to stimulate secreted alkaline phosphatase gene reporter activity in EP4-transfected HEK293 cells with an EC50 value of 0.19 nM, demonstrating >5,000 and 50,000-fold selectivity against EP2 and TP, respectively.{25026} KMN-80 can induce the differentiation of bone marrow stem cells from both young and aged rats into osteoblasts in vitro (EC50s = 20 and 153 nM, respectively) and exhibits favorable tolerability up to at least 10 μM, whereas the EP4 agonist L-902,688 (Item No. 10007712) is highly cytotoxic at similar concentrations in these cells.{25027} KMN-80 has been used to repair calvarial defects in an in vivo rat craniomaxillofacial reconstruction model (rate of reduction in defect size equivalent to BMP-2 treated rats) and to promote bone formation in a rat incisor tooth socket model.{25027}  

     

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  • KN-62 is a selective, cell permeable inhibitor of Ca2+/calmodulin-dependent kinase type II (CaMKII; IC50 = 900 nM).{17252} It does not affect the activity of several other kinases when tested at 10 µM.{12847} KN-62 also acts as a non-competitive antagonist of the purinergic receptor P2RX7 (IC50 = 15 nM).{17253}  

     

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  • KN-62 is a selective, cell permeable inhibitor of Ca2+/calmodulin-dependent kinase type II (CaMKII; IC50 = 900 nM).{17252} It does not affect the activity of several other kinases when tested at 10 µM.{12847} KN-62 also acts as a non-competitive antagonist of the purinergic receptor P2RX7 (IC50 = 15 nM).{17253}  

     

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  • KN-62 is a selective, cell permeable inhibitor of Ca2+/calmodulin-dependent kinase type II (CaMKII; IC50 = 900 nM).{17252} It does not affect the activity of several other kinases when tested at 10 µM.{12847} KN-62 also acts as a non-competitive antagonist of the purinergic receptor P2RX7 (IC50 = 15 nM).{17253}  

     

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    Cayman
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  • KN-62 is a selective, cell permeable inhibitor of Ca2+/calmodulin-dependent kinase type II (CaMKII; IC50 = 900 nM).{17252} It does not affect the activity of several other kinases when tested at 10 µM.{12847} KN-62 also acts as a non-competitive antagonist of the purinergic receptor P2RX7 (IC50 = 15 nM).{17253}  

     

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  • KN-92 is an inactive derivative of KN-93, the selective inhibitor of Ca2+/calmodulin-dependent kinase type II (CaMKII).{17325} At concentrations up to 25 μM, KN-92 is ineffective at inhibiting CaMKII or arresting cell growth of NIH 3T3 fibroblasts.{19487} It is intended to be used as a control compound in studies designed to elucidate the antagonist activities of KN-93 (Item No. 13319).  

     

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    Cayman
    SKU:9000890 - 1 mg

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  • KN-92 is an inactive derivative of KN-93, the selective inhibitor of Ca2+/calmodulin-dependent kinase type II (CaMKII).{17325} At concentrations up to 25 μM, KN-92 is ineffective at inhibiting CaMKII or arresting cell growth of NIH 3T3 fibroblasts.{19487} It is intended to be used as a control compound in studies designed to elucidate the antagonist activities of KN-93 (Item No. 13319).  

     

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    Cayman
    SKU:9000890 - 10 mg

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  • KN-92 is an inactive derivative of KN-93, the selective inhibitor of Ca2+/calmodulin-dependent kinase type II (CaMKII).{17325} At concentrations up to 25 μM, KN-92 is ineffective at inhibiting CaMKII or arresting cell growth of NIH 3T3 fibroblasts.{19487} It is intended to be used as a control compound in studies designed to elucidate the antagonist activities of KN-93 (Item No. 13319).  

     

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    Cayman
    SKU:9000890 - 5 mg

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  • KN-93 is a selective inhibitor of Ca2+/calmodulin-dependent kinase type II (CaMKII), competitively blocking CaM binding to the kinase (Ki = 370 nM).{17325} It does not affect the activities of PKA, PKC, MLCK, or Ca2+-phosphodiesterase.{17325} It inhibits histamine-induced aminopyrine uptake in parietal cells (IC50 = 300 nM).{17326} More recently, KN-93 has been used to implicate roles for CaMKII in Ca2+-induced Ca2+ release in cardiac myocytes, constitutive phosphorylation of 5-lipoxygenase in 3T3 cells, and Ca2+-dependent activation of HIF-1α in colon cancer cells.{17327,17328,17329}  

     

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  • KN-93 is a selective inhibitor of Ca2+/calmodulin-dependent kinase type II (CaMKII), competitively blocking CaM binding to the kinase (Ki = 370 nM).{17325} It does not affect the activities of PKA, PKC, MLCK, or Ca2+-phosphodiesterase.{17325} It inhibits histamine-induced aminopyrine uptake in parietal cells (IC50 = 300 nM).{17326} More recently, KN-93 has been used to implicate roles for CaMKII in Ca2+-induced Ca2+ release in cardiac myocytes, constitutive phosphorylation of 5-lipoxygenase in 3T3 cells, and Ca2+-dependent activation of HIF-1α in colon cancer cells.{17327,17328,17329}  

     

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    Cayman
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  • KN-93 is a selective inhibitor of Ca2+/calmodulin-dependent kinase type II (CaMKII), competitively blocking CaM binding to the kinase (Ki = 370 nM).{17325} It does not affect the activities of PKA, PKC, MLCK, or Ca2+-phosphodiesterase.{17325} It inhibits histamine-induced aminopyrine uptake in parietal cells (IC50 = 300 nM).{17326} More recently, KN-93 has been used to implicate roles for CaMKII in Ca2+-induced Ca2+ release in cardiac myocytes, constitutive phosphorylation of 5-lipoxygenase in 3T3 cells, and Ca2+-dependent activation of HIF-1α in colon cancer cells.{17327,17328,17329}  

     

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    Cayman
    SKU:-
  • KN-93 is a selective inhibitor of Ca2+/calmodulin-dependent kinase type II (CaMKII), competitively blocking CaM binding to the kinase (Ki = 370 nM).{17325} It does not affect the activities of PKA, PKC, MLCK, or Ca2+-phosphodiesterase.{17325} It inhibits histamine-induced aminopyrine uptake in parietal cells (IC50 = 300 nM).{17326} More recently, KN-93 has been used to implicate roles for CaMKII in Ca2+-induced Ca2+ release in cardiac myocytes, constitutive phosphorylation of 5-lipoxygenase in 3T3 cells, and Ca2+-dependent activation of HIF-1α in colon cancer cells.{17327,17328,17329}  

     

    Brand:
    Cayman
    SKU:-
  • KN-93 is a selective inhibitor of Ca2+/calmodulin-dependent kinase type II (CaMKII), competitively blocking CaM binding to the kinase (Ki = 370 nM).{17325} It does not affect the activities of PKA, PKC, MLCK, or Ca2+-phosphodiesterase.{17325} It inhibits histamine-induced aminopyrine uptake in parietal cells (IC50 = 300 nM).{17326} More recently, KN-93 has been used to implicate roles for CaMKII in Ca2+-induced Ca2+ release in cardiac myocytes, constitutive phosphorylation of 5-lipoxygenase in 3T3 cells, and Ca2+-dependent activation of HIF-1α in colon cancer cells.{17327,17328,17329}  

     

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    Cayman
    SKU:-
  • KN-93 is a selective inhibitor of Ca2+/calmodulin-dependent kinase type II (CaMKII), competitively blocking CaM binding to the kinase (Ki = 370 nM).{17325} It does not affect the activities of PKA, PKC, MLCK, or Ca2+-phosphodiesterase.{17325} It inhibits histamine-induced aminopyrine uptake in parietal cells (IC50 = 300 nM).{17326} More recently, KN-93 has been used to implicate roles for CaMKII in Ca2+-induced Ca2+ release in cardiac myocytes, constitutive phosphorylation of 5-lipoxygenase in 3T3 cells, and Ca2+-dependent activation of HIF-1α in colon cancer cells.{17327,17328,17329}  

     

    Brand:
    Cayman
    SKU:-
  • KN-93 (phosphate) is a potent and selective inhibitor of Ca2+/calmodulin-dependent kinase II (CaMKII) (Ki = 370 nM), inhibiting both the α- and β-subunits of CaMKII.{17325} It does not have significant effects on cAMP-dependent protein kinase, Ca2+/phospholipid-dependent protein kinase, myosin light chain kinase, or Ca2+ phosphodiesterase activity. It inhibits histamine-induced aminopyrine uptake in parietal cells (IC50 = 300 nM).{17326} KN-93 can block voltage-gated potassium (Kv) channels when applied extracellularly, independent of its CaMKII action.{33674} More recently, KN-93 has been used to implicate roles for CaMKII in Ca2+-induced Ca2+ release in cardiac myocytes, constitutive phosphorylation of 5-lipoxygenase in 3T3 cells, and Ca2+-dependent activation of HIF-1α in colon cancer cells.{17327,17328,17329}  

     

    Brand:
    Cayman
    SKU:21472 -

    Out of stock

  • KN-93 (phosphate) is a potent and selective inhibitor of Ca2+/calmodulin-dependent kinase II (CaMKII) (Ki = 370 nM), inhibiting both the α- and β-subunits of CaMKII.{17325} It does not have significant effects on cAMP-dependent protein kinase, Ca2+/phospholipid-dependent protein kinase, myosin light chain kinase, or Ca2+ phosphodiesterase activity. It inhibits histamine-induced aminopyrine uptake in parietal cells (IC50 = 300 nM).{17326} KN-93 can block voltage-gated potassium (Kv) channels when applied extracellularly, independent of its CaMKII action.{33674} More recently, KN-93 has been used to implicate roles for CaMKII in Ca2+-induced Ca2+ release in cardiac myocytes, constitutive phosphorylation of 5-lipoxygenase in 3T3 cells, and Ca2+-dependent activation of HIF-1α in colon cancer cells.{17327,17328,17329}  

     

    Brand:
    Cayman
    SKU:21472 -

    Out of stock

  • KN-93 (phosphate) is a potent and selective inhibitor of Ca2+/calmodulin-dependent kinase II (CaMKII) (Ki = 370 nM), inhibiting both the α- and β-subunits of CaMKII.{17325} It does not have significant effects on cAMP-dependent protein kinase, Ca2+/phospholipid-dependent protein kinase, myosin light chain kinase, or Ca2+ phosphodiesterase activity. It inhibits histamine-induced aminopyrine uptake in parietal cells (IC50 = 300 nM).{17326} KN-93 can block voltage-gated potassium (Kv) channels when applied extracellularly, independent of its CaMKII action.{33674} More recently, KN-93 has been used to implicate roles for CaMKII in Ca2+-induced Ca2+ release in cardiac myocytes, constitutive phosphorylation of 5-lipoxygenase in 3T3 cells, and Ca2+-dependent activation of HIF-1α in colon cancer cells.{17327,17328,17329}  

     

    Brand:
    Cayman
    SKU:21472 -

    Out of stock

  • KN-93 (phosphate) is a potent and selective inhibitor of Ca2+/calmodulin-dependent kinase II (CaMKII) (Ki = 370 nM), inhibiting both the α- and β-subunits of CaMKII.{17325} It does not have significant effects on cAMP-dependent protein kinase, Ca2+/phospholipid-dependent protein kinase, myosin light chain kinase, or Ca2+ phosphodiesterase activity. It inhibits histamine-induced aminopyrine uptake in parietal cells (IC50 = 300 nM).{17326} KN-93 can block voltage-gated potassium (Kv) channels when applied extracellularly, independent of its CaMKII action.{33674} More recently, KN-93 has been used to implicate roles for CaMKII in Ca2+-induced Ca2+ release in cardiac myocytes, constitutive phosphorylation of 5-lipoxygenase in 3T3 cells, and Ca2+-dependent activation of HIF-1α in colon cancer cells.{17327,17328,17329}  

     

    Brand:
    Cayman
    SKU:21472 -

    Out of stock

  • Breast cancer resistance protein (BCRP) is an ATP-binding cassette protein known also as ABCG2. While it normally functions as a high-capacity urate exporter in the renal system, it also acts as a xenobiotic transporter and contributes to multidrug resistance (e.g., to mitoxantrone) in certain types of cancer.{24807} BCRP is abundant at the intestinal epithelium and blood-brain barrier, potentially restricting the distribution of certain drugs.{24809,24808} Ko 143 is a potent and selective inhibitor of BCRP, preventing the export of mitoxantrone and topotecan in breast cancer cell lines (EC50s = 23 and 26 nM, respectively).{24809} It is much less effective at the transporters P-glycoprotein and multidrug resistance-associated protein 1, MRP1.{24809} Ko 143 is effective in vivo in mice.{24809,24808}  

     

    Brand:
    Cayman
    SKU:-
  • Breast cancer resistance protein (BCRP) is an ATP-binding cassette protein known also as ABCG2. While it normally functions as a high-capacity urate exporter in the renal system, it also acts as a xenobiotic transporter and contributes to multidrug resistance (e.g., to mitoxantrone) in certain types of cancer.{24807} BCRP is abundant at the intestinal epithelium and blood-brain barrier, potentially restricting the distribution of certain drugs.{24809,24808} Ko 143 is a potent and selective inhibitor of BCRP, preventing the export of mitoxantrone and topotecan in breast cancer cell lines (EC50s = 23 and 26 nM, respectively).{24809} It is much less effective at the transporters P-glycoprotein and multidrug resistance-associated protein 1, MRP1.{24809} Ko 143 is effective in vivo in mice.{24809,24808}  

     

    Brand:
    Cayman
    SKU:-
  • Breast cancer resistance protein (BCRP) is an ATP-binding cassette protein known also as ABCG2. While it normally functions as a high-capacity urate exporter in the renal system, it also acts as a xenobiotic transporter and contributes to multidrug resistance (e.g., to mitoxantrone) in certain types of cancer.{24807} BCRP is abundant at the intestinal epithelium and blood-brain barrier, potentially restricting the distribution of certain drugs.{24809,24808} Ko 143 is a potent and selective inhibitor of BCRP, preventing the export of mitoxantrone and topotecan in breast cancer cell lines (EC50s = 23 and 26 nM, respectively).{24809} It is much less effective at the transporters P-glycoprotein and multidrug resistance-associated protein 1, MRP1.{24809} Ko 143 is effective in vivo in mice.{24809,24808}  

     

    Brand:
    Cayman
    SKU:-
  • Breast cancer resistance protein (BCRP) is an ATP-binding cassette protein known also as ABCG2. While it normally functions as a high-capacity urate exporter in the renal system, it also acts as a xenobiotic transporter and contributes to multidrug resistance (e.g., to mitoxantrone) in certain types of cancer.{24807} BCRP is abundant at the intestinal epithelium and blood-brain barrier, potentially restricting the distribution of certain drugs.{24809,24808} Ko 143 is a potent and selective inhibitor of BCRP, preventing the export of mitoxantrone and topotecan in breast cancer cell lines (EC50s = 23 and 26 nM, respectively).{24809} It is much less effective at the transporters P-glycoprotein and multidrug resistance-associated protein 1, MRP1.{24809} Ko 143 is effective in vivo in mice.{24809,24808}  

     

    Brand:
    Cayman
    SKU:-
  • KO947 is an ERK inhibitor (IC50 = V600E with an IC50 value of less than 250 nM.{46896} It inhibits proliferation of A375 cells, as well as mutant K-Ras-expressing HCT116 and H358 cancer cell lines (IC50s = 50-250 nM for all).  

     

    Brand:
    Cayman
    SKU:29213 - 1 mg

    Available on backorder

  • KO947 is an ERK inhibitor (IC50 = V600E with an IC50 value of less than 250 nM.{46896} It inhibits proliferation of A375 cells, as well as mutant K-Ras-expressing HCT116 and H358 cancer cell lines (IC50s = 50-250 nM for all).  

     

    Brand:
    Cayman
    SKU:29213 - 10 mg

    Available on backorder

  • KO947 is an ERK inhibitor (IC50 = V600E with an IC50 value of less than 250 nM.{46896} It inhibits proliferation of A375 cells, as well as mutant K-Ras-expressing HCT116 and H358 cancer cell lines (IC50s = 50-250 nM for all).  

     

    Brand:
    Cayman
    SKU:29213 - 25 mg

    Available on backorder

  • KO947 is an ERK inhibitor (IC50 = V600E with an IC50 value of less than 250 nM.{46896} It inhibits proliferation of A375 cells, as well as mutant K-Ras-expressing HCT116 and H358 cancer cell lines (IC50s = 50-250 nM for all).  

     

    Brand:
    Cayman
    SKU:29213 - 5 mg

    Available on backorder

  • The Ras family of small GTPases (H-Ras, K-Ras, and N-Ras) function as molecular switches, cycling between a GTP-bound active state and a GDP-bound inactive state, to turn on downstream Raf protein kinases. This initiates complex signaling pathways involved in cell growth, differentiation, and apoptosis. Mutations leading to aberrant Ras activation are frequently associated with various human cancers. Kobe 0065 is an orally active Ras inhibitor with selectivity for H-Ras (Ki = 46 μM).{27843} It can inhibit both anchorage-dependent and -independent growth and induce apoptosis of H-RasG12V-transformed NIH 3T3 cells (IC50 = ~1.5 μM), which leads to a down-regulation of MEK/ERK, Akt, RalA, and Son of sevenless.{27843} At an oral dose of 80 mg/kg, Kobe 0065 also exhibits antitumor activity in mice bearing a xenograft of human colon cancer SW480 cells expressing K-RasG12V.{27843}  

     

    Brand:
    Cayman
    SKU:-
  • The Ras family of small GTPases (H-Ras, K-Ras, and N-Ras) function as molecular switches, cycling between a GTP-bound active state and a GDP-bound inactive state, to turn on downstream Raf protein kinases. This initiates complex signaling pathways involved in cell growth, differentiation, and apoptosis. Mutations leading to aberrant Ras activation are frequently associated with various human cancers. Kobe 0065 is an orally active Ras inhibitor with selectivity for H-Ras (Ki = 46 μM).{27843} It can inhibit both anchorage-dependent and -independent growth and induce apoptosis of H-RasG12V-transformed NIH 3T3 cells (IC50 = ~1.5 μM), which leads to a down-regulation of MEK/ERK, Akt, RalA, and Son of sevenless.{27843} At an oral dose of 80 mg/kg, Kobe 0065 also exhibits antitumor activity in mice bearing a xenograft of human colon cancer SW480 cells expressing K-RasG12V.{27843}  

     

    Brand:
    Cayman
    SKU:-
  • The Ras family of small GTPases (H-Ras, K-Ras, and N-Ras) function as molecular switches, cycling between a GTP-bound active state and a GDP-bound inactive state, to turn on downstream Raf protein kinases. This initiates complex signaling pathways involved in cell growth, differentiation, and apoptosis. Mutations leading to aberrant Ras activation are frequently associated with various human cancers. Kobe 0065 is an orally active Ras inhibitor with selectivity for H-Ras (Ki = 46 μM).{27843} It can inhibit both anchorage-dependent and -independent growth and induce apoptosis of H-RasG12V-transformed NIH 3T3 cells (IC50 = ~1.5 μM), which leads to a down-regulation of MEK/ERK, Akt, RalA, and Son of sevenless.{27843} At an oral dose of 80 mg/kg, Kobe 0065 also exhibits antitumor activity in mice bearing a xenograft of human colon cancer SW480 cells expressing K-RasG12V.{27843}  

     

    Brand:
    Cayman
    SKU:-
  • The Ras family of small GTPases (H-Ras, K-Ras, and N-Ras) function as molecular switches, cycling between a GTP-bound active state and a GDP-bound inactive state, to turn on downstream Raf protein kinases. This initiates complex signaling pathways involved in cell growth, differentiation, and apoptosis. Mutations leading to aberrant Ras activation are frequently associated with various human cancers. Kobe 0065 is an orally active Ras inhibitor with selectivity for H-Ras (Ki = 46 μM).{27843} It can inhibit both anchorage-dependent and -independent growth and induce apoptosis of H-RasG12V-transformed NIH 3T3 cells (IC50 = ~1.5 μM), which leads to a down-regulation of MEK/ERK, Akt, RalA, and Son of sevenless.{27843} At an oral dose of 80 mg/kg, Kobe 0065 also exhibits antitumor activity in mice bearing a xenograft of human colon cancer SW480 cells expressing K-RasG12V.{27843}  

     

    Brand:
    Cayman
    SKU:-
  • The Ras family of small GTPases (H-Ras, K-Ras, and N-Ras) function as molecular switches, cycling between a GTP-bound active state and a GDP-bound inactive state, to turn on downstream Raf protein kinases. This initiates complex signaling pathways involved in cell growth, differentiation, and apoptosis. Mutations leading to aberrant Ras activation are frequently associated with various human cancers. Kobe 2602 is a selective Ras inhibitor that blocks H-Ras GTP binding to c-Raf-1 (Ki = 149 µM).{27843} Kobe 2602 has been shown to inhibit both anchorage-dependent and -independent growth and to induce apoptosis of H-RasG12V-transformed NIH 3T3 cells (IC50 = 1.4-2 µM).{27843} At an oral dose of 80 mg/kg, it also exhibits antitumor activity in mice bearing a xenograft of human colon cancer SW480 cells expressing K-RasG12V.{27843}  

     

    Brand:
    Cayman
    SKU:-
  • The Ras family of small GTPases (H-Ras, K-Ras, and N-Ras) function as molecular switches, cycling between a GTP-bound active state and a GDP-bound inactive state, to turn on downstream Raf protein kinases. This initiates complex signaling pathways involved in cell growth, differentiation, and apoptosis. Mutations leading to aberrant Ras activation are frequently associated with various human cancers. Kobe 2602 is a selective Ras inhibitor that blocks H-Ras GTP binding to c-Raf-1 (Ki = 149 µM).{27843} Kobe 2602 has been shown to inhibit both anchorage-dependent and -independent growth and to induce apoptosis of H-RasG12V-transformed NIH 3T3 cells (IC50 = 1.4-2 µM).{27843} At an oral dose of 80 mg/kg, it also exhibits antitumor activity in mice bearing a xenograft of human colon cancer SW480 cells expressing K-RasG12V.{27843}  

     

    Brand:
    Cayman
    SKU:-
  • The Ras family of small GTPases (H-Ras, K-Ras, and N-Ras) function as molecular switches, cycling between a GTP-bound active state and a GDP-bound inactive state, to turn on downstream Raf protein kinases. This initiates complex signaling pathways involved in cell growth, differentiation, and apoptosis. Mutations leading to aberrant Ras activation are frequently associated with various human cancers. Kobe 2602 is a selective Ras inhibitor that blocks H-Ras GTP binding to c-Raf-1 (Ki = 149 µM).{27843} Kobe 2602 has been shown to inhibit both anchorage-dependent and -independent growth and to induce apoptosis of H-RasG12V-transformed NIH 3T3 cells (IC50 = 1.4-2 µM).{27843} At an oral dose of 80 mg/kg, it also exhibits antitumor activity in mice bearing a xenograft of human colon cancer SW480 cells expressing K-RasG12V.{27843}  

     

    Brand:
    Cayman
    SKU:-
  • The Ras family of small GTPases (H-Ras, K-Ras, and N-Ras) function as molecular switches, cycling between a GTP-bound active state and a GDP-bound inactive state, to turn on downstream Raf protein kinases. This initiates complex signaling pathways involved in cell growth, differentiation, and apoptosis. Mutations leading to aberrant Ras activation are frequently associated with various human cancers. Kobe 2602 is a selective Ras inhibitor that blocks H-Ras GTP binding to c-Raf-1 (Ki = 149 µM).{27843} Kobe 2602 has been shown to inhibit both anchorage-dependent and -independent growth and to induce apoptosis of H-RasG12V-transformed NIH 3T3 cells (IC50 = 1.4-2 µM).{27843} At an oral dose of 80 mg/kg, it also exhibits antitumor activity in mice bearing a xenograft of human colon cancer SW480 cells expressing K-RasG12V.{27843}  

     

    Brand:
    Cayman
    SKU:-
  • Kocurin is a thiazolyl peptide originally isolated from K. palustris and has antibiotic activity.{52349} It is active against methicillin-resistant S. aureus (MRSA; MIC = 0.25 µg/ml), as well as B. subtilis and E. faecium in a solid agar test when used at a concentration of 8 µg/ml. Kocurin is also active against E. faecium, E. faecalis, S. epidermidis, and clinical isolates of vancomycin-resistant enterococci (MICs = 0.004-1.025 µg/ml).{52350} In vivo, kocurin (2.5, 5, and 10 mg/ml) increases survival in a mouse model of E. faecium-induced septicemia. It decreases the number of colony forming units (CFUs) in a mouse model of MRSA lung infection.  

     

    Brand:
    Cayman
    SKU:29125 - 1 mg

    Available on backorder

  • Oxidized low-density lipoprotien (oxLDL) particles contain low molecular weight species which are cytotoxic and pro-atherogenic.{9800} Many of these substances were recently isolated and purified from oxLDL, and identified as phosphatidylcholine species containing a fragmented, oxidized short-chain fatty acid remnant at the sn-2 position.{9891} 1-(Palmitoyl)-2-(5-keto-6-octene-dioyl) phosphatidylcholine, or KOdiA-PC, is one of the most potent CD36 ligands among the oxLDL species.{9890} KOdiA-PC confers CD36 scavenger receptor binding affinity to LDL at a frequency of only 2 to 3 KOdiA-PC molecules/LDL particle, and may be one of the more important structural determinants of oxLDL.  

     

    Brand:
    Cayman
    SKU:62945 - 1 mg

    Available on backorder

  • Oxidized low-density lipoprotien (oxLDL) particles contain low molecular weight species which are cytotoxic and pro-atherogenic.{9800} Many of these substances were recently isolated and purified from oxLDL, and identified as phosphatidylcholine species containing a fragmented, oxidized short-chain fatty acid remnant at the sn-2 position.{9891} 1-(Palmitoyl)-2-(5-keto-6-octene-dioyl) phosphatidylcholine, or KOdiA-PC, is one of the most potent CD36 ligands among the oxLDL species.{9890} KOdiA-PC confers CD36 scavenger receptor binding affinity to LDL at a frequency of only 2 to 3 KOdiA-PC molecules/LDL particle, and may be one of the more important structural determinants of oxLDL.  

     

    Brand:
    Cayman
    SKU:62945 - 10 mg

    Available on backorder

  • Oxidized low-density lipoprotien (oxLDL) particles contain low molecular weight species which are cytotoxic and pro-atherogenic.{9800} Many of these substances were recently isolated and purified from oxLDL, and identified as phosphatidylcholine species containing a fragmented, oxidized short-chain fatty acid remnant at the sn-2 position.{9891} 1-(Palmitoyl)-2-(5-keto-6-octene-dioyl) phosphatidylcholine, or KOdiA-PC, is one of the most potent CD36 ligands among the oxLDL species.{9890} KOdiA-PC confers CD36 scavenger receptor binding affinity to LDL at a frequency of only 2 to 3 KOdiA-PC molecules/LDL particle, and may be one of the more important structural determinants of oxLDL.  

     

    Brand:
    Cayman
    SKU:62945 - 5 mg

    Available on backorder

  • Oxidized low-density lipoprotien (oxLDL) particles contain low molecular weight species which are cytotoxic and pro-atherogenic.{9800} Many of these substances were recently isolated and purified from oxLDL, and identified as phosphatidylcholine species containing a fragmented, oxidized short-chain fatty acid remnant at the sn-2 position.{9891} 1-(Palmitoyl)-2-(5-keto-6-octene-dioyl) phosphatidylcholine, or KOdiA-PC, is one of the most potent CD36 ligands among the oxLDL species.{9890} KOdiA-PC confers CD36 scavenger receptor binding affinity to LDL at a frequency of only 2 to 3 KOdiA-PC molecules/LDL particle, and may be one of the more important structural determinants of oxLDL.  

     

    Brand:
    Cayman
    SKU:62945 - 500 µg

    Available on backorder

  • Kojic acid is a fungal metabolite that inhibits tyrosinase, an enzyme involved in melanin synthesis, with an IC50 value of 30.6 µM for mushroom tyrosinase.{38117} It decreases growth of Leishmania parasites in vitro and in vivo, and it protects mice from damage induced by gamma irradiation.{38118,38119} Kojic acid has been used as a food additive to prevent enzymatic browning.{38116} Formulations containing kojic acid are used in the treatment of hyperpigmentation disorders.{21434}  

     

    Brand:
    Cayman
    SKU:22712 -

    Out of stock

  • Kojic acid is a fungal metabolite that inhibits tyrosinase, an enzyme involved in melanin synthesis, with an IC50 value of 30.6 µM for mushroom tyrosinase.{38117} It decreases growth of Leishmania parasites in vitro and in vivo, and it protects mice from damage induced by gamma irradiation.{38118,38119} Kojic acid has been used as a food additive to prevent enzymatic browning.{38116} Formulations containing kojic acid are used in the treatment of hyperpigmentation disorders.{21434}  

     

    Brand:
    Cayman
    SKU:22712 -

    Out of stock

  • Kojic acid is a fungal metabolite that inhibits tyrosinase, an enzyme involved in melanin synthesis, with an IC50 value of 30.6 µM for mushroom tyrosinase.{38117} It decreases growth of Leishmania parasites in vitro and in vivo, and it protects mice from damage induced by gamma irradiation.{38118,38119} Kojic acid has been used as a food additive to prevent enzymatic browning.{38116} Formulations containing kojic acid are used in the treatment of hyperpigmentation disorders.{21434}  

     

    Brand:
    Cayman
    SKU:22712 -

    Out of stock

  • Kojic acid is a fungal metabolite that inhibits tyrosinase, an enzyme involved in melanin synthesis, with an IC50 value of 30.6 µM for mushroom tyrosinase.{38117} It decreases growth of Leishmania parasites in vitro and in vivo, and it protects mice from damage induced by gamma irradiation.{38118,38119} Kojic acid has been used as a food additive to prevent enzymatic browning.{38116} Formulations containing kojic acid are used in the treatment of hyperpigmentation disorders.{21434}  

     

    Brand:
    Cayman
    SKU:22712 -

    Out of stock

  • Kotanin A is a fungal metabolite produced by A. glaucus (A. clavatus), A. alliaceus, and A. niger.{36638,36637} It is toxic to day-old chicks (LD100 = 62.5 mg/kg) but has no effect in rats.{36638}  

     

    Brand:
    Cayman
    SKU:24917 - 2.5 mg

    Available on backorder

  • Kotanin A is a fungal metabolite produced by A. glaucus (A. clavatus), A. alliaceus, and A. niger.{36638,36637} It is toxic to day-old chicks (LD100 = 62.5 mg/kg) but has no effect in rats.{36638}  

     

    Brand:
    Cayman
    SKU:24917 - 500 µg

    Available on backorder

  • KP372-1 is a specific Akt inhibitor that demonstrates at least 10-fold selectivity against a panel of additional kinase targets, including CDK1, ERK1, GSK3β, LCK, MEK1, PKA, PKC, and S6K.{26547,26546} By blocking Akt signaling, KP372-1 has been shown to inhibit proliferation and to induce apoptosis of thyroid cancer cells with an IC50 value of 30-60 nM in vitro.{26546} In acute myelogenous leukemia cells, KP372-1 is reported to inhibit the kinase activity of Akt, PDK1, and FLT3, decreasing the colony-forming ability of these cells with an IC50 value less than 200 nM.{26547}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • KP372-1 is a specific Akt inhibitor that demonstrates at least 10-fold selectivity against a panel of additional kinase targets, including CDK1, ERK1, GSK3β, LCK, MEK1, PKA, PKC, and S6K.{26547,26546} By blocking Akt signaling, KP372-1 has been shown to inhibit proliferation and to induce apoptosis of thyroid cancer cells with an IC50 value of 30-60 nM in vitro.{26546} In acute myelogenous leukemia cells, KP372-1 is reported to inhibit the kinase activity of Akt, PDK1, and FLT3, decreasing the colony-forming ability of these cells with an IC50 value less than 200 nM.{26547}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • KP372-1 is a specific Akt inhibitor that demonstrates at least 10-fold selectivity against a panel of additional kinase targets, including CDK1, ERK1, GSK3β, LCK, MEK1, PKA, PKC, and S6K.{26547,26546} By blocking Akt signaling, KP372-1 has been shown to inhibit proliferation and to induce apoptosis of thyroid cancer cells with an IC50 value of 30-60 nM in vitro.{26546} In acute myelogenous leukemia cells, KP372-1 is reported to inhibit the kinase activity of Akt, PDK1, and FLT3, decreasing the colony-forming ability of these cells with an IC50 value less than 200 nM.{26547}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • KPT-185 is an inhibitor of Exportin 1 (XPO1/CRM1) with anticancer activity.{47263,31566} It reduces proliferation in a panel of patient-derived acute myeloid leukemia cells (IC50s = 100-500 nM).{47263} KPT-185 induces cell cycle arrest in the G1 phase and apoptosis in MOLT-4 T cell acute lymphoblastic leukemia cells and in a panel of six non-small cell lung cancer (NSCLC) cell lines in a time- and dose-dependent manner.{31566,47264}  

     

    Brand:
    Cayman
    SKU:26074 - 10 mg

    Available on backorder

  • KPT-185 is an inhibitor of Exportin 1 (XPO1/CRM1) with anticancer activity.{47263,31566} It reduces proliferation in a panel of patient-derived acute myeloid leukemia cells (IC50s = 100-500 nM).{47263} KPT-185 induces cell cycle arrest in the G1 phase and apoptosis in MOLT-4 T cell acute lymphoblastic leukemia cells and in a panel of six non-small cell lung cancer (NSCLC) cell lines in a time- and dose-dependent manner.{31566,47264}  

     

    Brand:
    Cayman
    SKU:26074 - 25 mg

    Available on backorder

  • KPT-185 is an inhibitor of Exportin 1 (XPO1/CRM1) with anticancer activity.{47263,31566} It reduces proliferation in a panel of patient-derived acute myeloid leukemia cells (IC50s = 100-500 nM).{47263} KPT-185 induces cell cycle arrest in the G1 phase and apoptosis in MOLT-4 T cell acute lymphoblastic leukemia cells and in a panel of six non-small cell lung cancer (NSCLC) cell lines in a time- and dose-dependent manner.{31566,47264}  

     

    Brand:
    Cayman
    SKU:26074 - 5 mg

    Available on backorder

  • KPT-276 is an orally bioavailable inhibitor of Exportin 1 (XPO1/CRM1) with anticancer activity.{47263} In vivo, KPT-276 (150 mg/kg) increases survival and reduces spleen weight and white blood cell count in an MV4-11 acute myeloid leukemia (AML) mouse xenograft model. It also reduces tumor volume and increases survival in a BT 145 glioblastoma mouse xenograft model when administered at a dose of 75 mg/kg.{53291}  

     

    Brand:
    Cayman
    SKU:29158 - 10 mg

    Available on backorder

  • KPT-276 is an orally bioavailable inhibitor of Exportin 1 (XPO1/CRM1) with anticancer activity.{47263} In vivo, KPT-276 (150 mg/kg) increases survival and reduces spleen weight and white blood cell count in an MV4-11 acute myeloid leukemia (AML) mouse xenograft model. It also reduces tumor volume and increases survival in a BT 145 glioblastoma mouse xenograft model when administered at a dose of 75 mg/kg.{53291}  

     

    Brand:
    Cayman
    SKU:29158 - 25 mg

    Available on backorder

  • KPT-276 is an orally bioavailable inhibitor of Exportin 1 (XPO1/CRM1) with anticancer activity.{47263} In vivo, KPT-276 (150 mg/kg) increases survival and reduces spleen weight and white blood cell count in an MV4-11 acute myeloid leukemia (AML) mouse xenograft model. It also reduces tumor volume and increases survival in a BT 145 glioblastoma mouse xenograft model when administered at a dose of 75 mg/kg.{53291}  

     

    Brand:
    Cayman
    SKU:29158 - 5 mg

    Available on backorder

  • KPT-276 is an orally bioavailable inhibitor of Exportin 1 (XPO1/CRM1) with anticancer activity.{47263} In vivo, KPT-276 (150 mg/kg) increases survival and reduces spleen weight and white blood cell count in an MV4-11 acute myeloid leukemia (AML) mouse xenograft model. It also reduces tumor volume and increases survival in a BT 145 glioblastoma mouse xenograft model when administered at a dose of 75 mg/kg.{53291}  

     

    Brand:
    Cayman
    SKU:29158 - 50 mg

    Available on backorder

  • KR-32568 is an inhibitor of the sodium-hydrogen exchanger isoform-1 (NHE-1; IC50 = 230 nM).{36411} It restores cardiac contractile function ex vivo in an isolated ischemic rat heart model when used at a concentration of 10 μM. KR-32568 (0.3 mg/kg) reduces myocardial infarct size in a rat model of ischemia and reperfusion injury.  

     

    Brand:
    Cayman
    SKU:23968 - 1 mg

    Available on backorder

  • KR-32568 is an inhibitor of the sodium-hydrogen exchanger isoform-1 (NHE-1; IC50 = 230 nM).{36411} It restores cardiac contractile function ex vivo in an isolated ischemic rat heart model when used at a concentration of 10 μM. KR-32568 (0.3 mg/kg) reduces myocardial infarct size in a rat model of ischemia and reperfusion injury.  

     

    Brand:
    Cayman
    SKU:23968 - 5 mg

    Available on backorder

  • KR-33493 is an inhibitor of Fas-associated factor 1 (FAF1).{45494,45495} It inhibits chemical hypoxia-induced apoptosis in H9c2 cardiomyocytes and hydrogen peroxide-induced cell death in SH-SY5Y cells when used at a concentrations of 10 and 20 μM, respectively.{45495,45496} KR-33493 (20 mg/kg per day) reduces decreases in striatal dopamine transporter activity in a mouse model of Parkinson’s disease induced by MPTP.{45494}  

     

    Brand:
    Cayman
    SKU:22071 -

    Out of stock

  • KR-33493 is an inhibitor of Fas-associated factor 1 (FAF1).{45494,45495} It inhibits chemical hypoxia-induced apoptosis in H9c2 cardiomyocytes and hydrogen peroxide-induced cell death in SH-SY5Y cells when used at a concentrations of 10 and 20 μM, respectively.{45495,45496} KR-33493 (20 mg/kg per day) reduces decreases in striatal dopamine transporter activity in a mouse model of Parkinson’s disease induced by MPTP.{45494}  

     

    Brand:
    Cayman
    SKU:22071 -

    Out of stock

  • KR-33493 is an inhibitor of Fas-associated factor 1 (FAF1).{45494,45495} It inhibits chemical hypoxia-induced apoptosis in H9c2 cardiomyocytes and hydrogen peroxide-induced cell death in SH-SY5Y cells when used at a concentrations of 10 and 20 μM, respectively.{45495,45496} KR-33493 (20 mg/kg per day) reduces decreases in striatal dopamine transporter activity in a mouse model of Parkinson’s disease induced by MPTP.{45494}  

     

    Brand:
    Cayman
    SKU:22071 -

    Out of stock

  • KR-33493 is an inhibitor of Fas-associated factor 1 (FAF1).{45494,45495} It inhibits chemical hypoxia-induced apoptosis in H9c2 cardiomyocytes and hydrogen peroxide-induced cell death in SH-SY5Y cells when used at a concentrations of 10 and 20 μM, respectively.{45495,45496} KR-33493 (20 mg/kg per day) reduces decreases in striatal dopamine transporter activity in a mouse model of Parkinson’s disease induced by MPTP.{45494}  

     

    Brand:
    Cayman
    SKU:22071 -

    Out of stock

  • Kresoxim-methyl is a strobilurin fungicide.{48004} It inhibits conidial germination of V. inaequalis isolates from apple orchards (EC50s = 0.00033-0.0078 mg/L). Kresoxim-methyl also inhibits mycelial growth (EC50 = 0.240 mg/L) and is fungicidal against Saprolegnia (MIC = 1 mg/L).{48005} It increases intracellular calcium levels and disrupts the mitochondrial membrane potential in mouse cortical cultures in a concentration-dependent manner.{48006} Kresoxim-methyl is toxic to goldfish (C. auratus; LC50 = 0.807 mg/L).{48005}  

     

    Brand:
    Cayman
    SKU:25816 - 100 mg

    Available on backorder

  • Kresoxim-methyl is a strobilurin fungicide.{48004} It inhibits conidial germination of V. inaequalis isolates from apple orchards (EC50s = 0.00033-0.0078 mg/L). Kresoxim-methyl also inhibits mycelial growth (EC50 = 0.240 mg/L) and is fungicidal against Saprolegnia (MIC = 1 mg/L).{48005} It increases intracellular calcium levels and disrupts the mitochondrial membrane potential in mouse cortical cultures in a concentration-dependent manner.{48006} Kresoxim-methyl is toxic to goldfish (C. auratus; LC50 = 0.807 mg/L).{48005}  

     

    Brand:
    Cayman
    SKU:25816 - 25 mg

    Available on backorder

  • Kresoxim-methyl is a strobilurin fungicide.{48004} It inhibits conidial germination of V. inaequalis isolates from apple orchards (EC50s = 0.00033-0.0078 mg/L). Kresoxim-methyl also inhibits mycelial growth (EC50 = 0.240 mg/L) and is fungicidal against Saprolegnia (MIC = 1 mg/L).{48005} It increases intracellular calcium levels and disrupts the mitochondrial membrane potential in mouse cortical cultures in a concentration-dependent manner.{48006} Kresoxim-methyl is toxic to goldfish (C. auratus; LC50 = 0.807 mg/L).{48005}  

     

    Brand:
    Cayman
    SKU:25816 - 50 mg

    Available on backorder

  • KRIBB11 is an inhibitor of heat shock factor 1 (Hsf1) with an IC50 value of 1.2 μM in a luciferase reporter assay.{37149} It blocks heat shock-induced Hsp70, Hsp40, and Hsp27 mRNA expression and down-regulates protein expression of the Hsf1 target proteins Hsp70 and Hsp27 in HCT116 cells in a dose-dependent manner. KRIBB11 specifically binds to Hsf1 over other Hsf1-associated proteins, lacking activity at heat shock protein 90 (Hsp90), Hsf2, and Cdk9 in an in vitro pull-down assay. It inhibits growth of HCT116, Mia-PaCa-2, SW620, HT-29, A549, and MDA-MB-231 cancer cell lines (IC50s = 3-8 μM) via induction of cell cycle arrest at the G2/M phase and apoptosis. In vivo, administration of KRIBB11 decreases tumor growth in a mouse HCT116 xenograft model. KRIB11 administration also attenuates dengue virus progression and reduces mortality without affecting bodyweight in infected mice.{37150}  

     

    Brand:
    Cayman
    SKU:9002528 - 10 mg

    Available on backorder

  • KRIBB11 is an inhibitor of heat shock factor 1 (Hsf1) with an IC50 value of 1.2 μM in a luciferase reporter assay.{37149} It blocks heat shock-induced Hsp70, Hsp40, and Hsp27 mRNA expression and down-regulates protein expression of the Hsf1 target proteins Hsp70 and Hsp27 in HCT116 cells in a dose-dependent manner. KRIBB11 specifically binds to Hsf1 over other Hsf1-associated proteins, lacking activity at heat shock protein 90 (Hsp90), Hsf2, and Cdk9 in an in vitro pull-down assay. It inhibits growth of HCT116, Mia-PaCa-2, SW620, HT-29, A549, and MDA-MB-231 cancer cell lines (IC50s = 3-8 μM) via induction of cell cycle arrest at the G2/M phase and apoptosis. In vivo, administration of KRIBB11 decreases tumor growth in a mouse HCT116 xenograft model. KRIB11 administration also attenuates dengue virus progression and reduces mortality without affecting bodyweight in infected mice.{37150}  

     

    Brand:
    Cayman
    SKU:9002528 - 5 mg

    Available on backorder

  • KRIBB3 is an Hsp27 and microtubule inhibitor that inhibits migration and invasion of MDA-MB-231 cells in vitro in an Hsp27-dependent manner.{38667,38666} It inhibits protein kinase C (PKC) phosphorylation of Hsp27 but not phospholipase Cβ3, indicating KRIBB3 interaction with Hsp27 is preventing its phosphorylation. KRIBB3 (1-100 μM) inhibits growth of HCT116, HCT15, and MDA-MB-231 cells in an Hsp27-independent and concentration-dependent manner. It induces HCT116 cell cycle arrest in the G2/M phase via formation of the Mad2/p55CDC inhibitory complex and Bax activation of apoptosis.{38666} KRIBB3 also inhibits microtubule polymerization in HCT116 cells. In vivo, KRIBB3 (50-100 mg/kg) reduces tumor volume in an HCT116 mouse xenograft model.  

     

    Brand:
    Cayman
    SKU:23973 - 5 mg

    Available on backorder

  • KRN 633 is an ATP-competitive inhibitor of VEGFR kinase activity (IC50s = 170, 160, and 125 nM for VEGFR1, 2, and 3, respectively).{23658} At higher concentrations KRN 633 inhibits PDGFR-α and c-KIT with IC50 values of 0.97 and 4.3 μM, respectively, and is inactive towards a panel of 17 additional kinases.{23658} KRN 633 suppresses VEGF-dependent activation of MAPK and cell proliferation and demonstrates antitumor and antiangiogenic activity by inhibiting vessel formation and vascular permeability in human tumor xenograft models.{24366}  

     

    Brand:
    Cayman
    SKU:-
  • KRN 633 is an ATP-competitive inhibitor of VEGFR kinase activity (IC50s = 170, 160, and 125 nM for VEGFR1, 2, and 3, respectively).{23658} At higher concentrations KRN 633 inhibits PDGFR-α and c-KIT with IC50 values of 0.97 and 4.3 μM, respectively, and is inactive towards a panel of 17 additional kinases.{23658} KRN 633 suppresses VEGF-dependent activation of MAPK and cell proliferation and demonstrates antitumor and antiangiogenic activity by inhibiting vessel formation and vascular permeability in human tumor xenograft models.{24366}  

     

    Brand:
    Cayman
    SKU:-
  • KRN 633 is an ATP-competitive inhibitor of VEGFR kinase activity (IC50s = 170, 160, and 125 nM for VEGFR1, 2, and 3, respectively).{23658} At higher concentrations KRN 633 inhibits PDGFR-α and c-KIT with IC50 values of 0.97 and 4.3 μM, respectively, and is inactive towards a panel of 17 additional kinases.{23658} KRN 633 suppresses VEGF-dependent activation of MAPK and cell proliferation and demonstrates antitumor and antiangiogenic activity by inhibiting vessel formation and vascular permeability in human tumor xenograft models.{24366}  

     

    Brand:
    Cayman
    SKU:-
  • KRN 633 is an ATP-competitive inhibitor of VEGFR kinase activity (IC50s = 170, 160, and 125 nM for VEGFR1, 2, and 3, respectively).{23658} At higher concentrations KRN 633 inhibits PDGFR-α and c-KIT with IC50 values of 0.97 and 4.3 μM, respectively, and is inactive towards a panel of 17 additional kinases.{23658} KRN 633 suppresses VEGF-dependent activation of MAPK and cell proliferation and demonstrates antitumor and antiangiogenic activity by inhibiting vessel formation and vascular permeability in human tumor xenograft models.{24366}  

     

    Brand:
    Cayman
    SKU:-
  • KRN 7000 is a potent synthetic α-galactosylceramide, which, in association with the antigen-presenting CD1d protein, activates NKT immune cells.{20770,20769} As these cells have important roles in the rejection of malignant tumors and in the regulation of several autoimmune diseases, KRN 7000 has activity in many diseases, including cancer, lupus, diabetes, malaria, and tuberculosis.{5861,20768,20767}  

     

    Brand:
    Cayman
    SKU:11208 - 1 mg

    Available on backorder

  • KRN 7000 is a potent synthetic α-galactosylceramide, which, in association with the antigen-presenting CD1d protein, activates NKT immune cells.{20770,20769} As these cells have important roles in the rejection of malignant tumors and in the regulation of several autoimmune diseases, KRN 7000 has activity in many diseases, including cancer, lupus, diabetes, malaria, and tuberculosis.{5861,20768,20767}  

     

    Brand:
    Cayman
    SKU:11208 - 250 µg

    Available on backorder

  • KS-176 is a selective inhibitor of breast cancer resistance protein (BRCP; IC50 = 1.39 μM) with no activity against P-glycoprotein (P-gp) or multidrug resistance-associated protein 1 (MRP1).{39060} It acts as a non-competitive inhibitor whose potency is increased by imatinib binding. KS-176 does not reduce cell viability at concentrations up to 10 μM.  

     

    Brand:
    Cayman
    SKU:22201 -

    Out of stock

  • KS-176 is a selective inhibitor of breast cancer resistance protein (BRCP; IC50 = 1.39 μM) with no activity against P-glycoprotein (P-gp) or multidrug resistance-associated protein 1 (MRP1).{39060} It acts as a non-competitive inhibitor whose potency is increased by imatinib binding. KS-176 does not reduce cell viability at concentrations up to 10 μM.  

     

    Brand:
    Cayman
    SKU:22201 -

    Out of stock

  • KS-176 is a selective inhibitor of breast cancer resistance protein (BRCP; IC50 = 1.39 μM) with no activity against P-glycoprotein (P-gp) or multidrug resistance-associated protein 1 (MRP1).{39060} It acts as a non-competitive inhibitor whose potency is increased by imatinib binding. KS-176 does not reduce cell viability at concentrations up to 10 μM.  

     

    Brand:
    Cayman
    SKU:22201 -

    Out of stock

  • KS-176 is a selective inhibitor of breast cancer resistance protein (BRCP; IC50 = 1.39 μM) with no activity against P-glycoprotein (P-gp) or multidrug resistance-associated protein 1 (MRP1).{39060} It acts as a non-competitive inhibitor whose potency is increased by imatinib binding. KS-176 does not reduce cell viability at concentrations up to 10 μM.  

     

    Brand:
    Cayman
    SKU:22201 -

    Out of stock

  • Protein kinase A (PKA) regulates multiple signal transduction events via protein phosphorylation and is integral to all cellular responses involving the cyclic AMP second messenger system. KT 5720 is one of a family of compounds synthesized by the fungus Nocardiopsis sp. It blocks PKA signaling through competitive inhibition of ATP with a Ki value of 60 nM.{16598} Reported IC50 values vary widely depending upon ATP concentration tested and can range from 56 nM (low ATP) to 3 µM (physiologic ATP).{12847,16597} Non-specific effects of KT 5720 include inhibition of phosphorylase kinase, PDK1, MEK, MSK1, PKBα, and GSK3β at concentrations as effective as or more potent than that for inhibition of PKA.{12847,16597}  

     

    Brand:
    Cayman
    SKU:10011011 - 100 µg

    Available on backorder

  • Protein kinase A (PKA) regulates multiple signal transduction events via protein phosphorylation and is integral to all cellular responses involving the cyclic AMP second messenger system. KT 5720 is one of a family of compounds synthesized by the fungus Nocardiopsis sp. It blocks PKA signaling through competitive inhibition of ATP with a Ki value of 60 nM.{16598} Reported IC50 values vary widely depending upon ATP concentration tested and can range from 56 nM (low ATP) to 3 µM (physiologic ATP).{12847,16597} Non-specific effects of KT 5720 include inhibition of phosphorylase kinase, PDK1, MEK, MSK1, PKBα, and GSK3β at concentrations as effective as or more potent than that for inhibition of PKA.{12847,16597}  

     

    Brand:
    Cayman
    SKU:10011011 - 250 µg

    Available on backorder

  • Protein kinase A (PKA) regulates multiple signal transduction events via protein phosphorylation and is integral to all cellular responses involving the cyclic AMP second messenger system. KT 5720 is one of a family of compounds synthesized by the fungus Nocardiopsis sp. It blocks PKA signaling through competitive inhibition of ATP with a Ki value of 60 nM.{16598} Reported IC50 values vary widely depending upon ATP concentration tested and can range from 56 nM (low ATP) to 3 µM (physiologic ATP).{12847,16597} Non-specific effects of KT 5720 include inhibition of phosphorylase kinase, PDK1, MEK, MSK1, PKBα, and GSK3β at concentrations as effective as or more potent than that for inhibition of PKA.{12847,16597}  

     

    Brand:
    Cayman
    SKU:10011011 - 50 µg

    Available on backorder

  • Protein kinase A (PKA) regulates multiple signal transduction events via protein phosphorylation and is integral to all cellular responses involving the cyclic AMP second messenger system. KT 5720 is one of a family of compounds synthesized by the fungus Nocardiopsis sp. It blocks PKA signaling through competitive inhibition of ATP with a Ki value of 60 nM.{16598} Reported IC50 values vary widely depending upon ATP concentration tested and can range from 56 nM (low ATP) to 3 µM (physiologic ATP).{12847,16597} Non-specific effects of KT 5720 include inhibition of phosphorylase kinase, PDK1, MEK, MSK1, PKBα, and GSK3β at concentrations as effective as or more potent than that for inhibition of PKA.{12847,16597}  

     

    Brand:
    Cayman
    SKU:10011011 - 500 µg

    Available on backorder

  • The activity of cGMP-dependent protein kinase (PKG) is controlled by factors that elevate cellular cGMP, like nitric oxide (NO), and by those that reduce cGMP levels, like certain phosphodiesterases. KT 5823 is a potent, selective inhibitor of cGMP-dependent protein kinase (PKG) (in vitro IC50 = 234 nM).{16586} KT 5823 is cell-permeable and is often used in intact cells to assess the role of PKG in signaling, although there are cases where it poorly inhibits PKG in cells.{16587} KT 5823 is a weak inhibitor of PKC (Ki = 4 µM) and PKA (Ki >10 µM).{16586}  

     

    Brand:
    Cayman
    SKU:10010965 - 100 µg

    Available on backorder

  • The activity of cGMP-dependent protein kinase (PKG) is controlled by factors that elevate cellular cGMP, like nitric oxide (NO), and by those that reduce cGMP levels, like certain phosphodiesterases. KT 5823 is a potent, selective inhibitor of cGMP-dependent protein kinase (PKG) (in vitro IC50 = 234 nM).{16586} KT 5823 is cell-permeable and is often used in intact cells to assess the role of PKG in signaling, although there are cases where it poorly inhibits PKG in cells.{16587} KT 5823 is a weak inhibitor of PKC (Ki = 4 µM) and PKA (Ki >10 µM).{16586}  

     

    Brand:
    Cayman
    SKU:10010965 - 25 µg

    Available on backorder

  • The activity of cGMP-dependent protein kinase (PKG) is controlled by factors that elevate cellular cGMP, like nitric oxide (NO), and by those that reduce cGMP levels, like certain phosphodiesterases. KT 5823 is a potent, selective inhibitor of cGMP-dependent protein kinase (PKG) (in vitro IC50 = 234 nM).{16586} KT 5823 is cell-permeable and is often used in intact cells to assess the role of PKG in signaling, although there are cases where it poorly inhibits PKG in cells.{16587} KT 5823 is a weak inhibitor of PKC (Ki = 4 µM) and PKA (Ki >10 µM).{16586}  

     

    Brand:
    Cayman
    SKU:10010965 - 50 µg

    Available on backorder

  • The activity of cGMP-dependent protein kinase (PKG) is controlled by factors that elevate cellular cGMP, like nitric oxide (NO), and by those that reduce cGMP levels, like certain phosphodiesterases. KT 5823 is a potent, selective inhibitor of cGMP-dependent protein kinase (PKG) (in vitro IC50 = 234 nM).{16586} KT 5823 is cell-permeable and is often used in intact cells to assess the role of PKG in signaling, although there are cases where it poorly inhibits PKG in cells.{16587} KT 5823 is a weak inhibitor of PKC (Ki = 4 µM) and PKA (Ki >10 µM).{16586}  

     

    Brand:
    Cayman
    SKU:10010965 - 500 µg

    Available on backorder

  • In humans, two forms of diacylglycerol lipase, DAGLα and DAGLβ, generate the endocannabinoid 2-arachidonoyl glycerol (2-AG; Item No. 62160) by attacking DAG at the sn-1 position. KT109 is a selective inhibitor of DAGLβ with an IC50 value of 42 nM.{30430} It demonstrates ~60-fold selectivity for DAGLβ over DAGLα, and negligible activity against other key enzymes involved in endocannabinoid signaling, including FAAH, MAGL, and ABHD11.{30430} KT109 has been shown to disrupt the lipid network involved in macrophage inflammatory responses, lowering 2-AG, as well as arachidonic acid (Item No. 90010) and eicosanoids, in mouse peritoneal macrophages.{30430}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • In humans, two forms of diacylglycerol lipase, DAGLα and DAGLβ, generate the endocannabinoid 2-arachidonoyl glycerol (2-AG; Item No. 62160) by attacking DAG at the sn-1 position. KT109 is a selective inhibitor of DAGLβ with an IC50 value of 42 nM.{30430} It demonstrates ~60-fold selectivity for DAGLβ over DAGLα, and negligible activity against other key enzymes involved in endocannabinoid signaling, including FAAH, MAGL, and ABHD11.{30430} KT109 has been shown to disrupt the lipid network involved in macrophage inflammatory responses, lowering 2-AG, as well as arachidonic acid (Item No. 90010) and eicosanoids, in mouse peritoneal macrophages.{30430}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • In humans, two forms of diacylglycerol lipase, DAGLα and DAGLβ, generate the endocannabinoid 2-arachidonoyl glycerol (2-AG; Item No. 62160) by attacking DAG at the sn-1 position. KT109 is a selective inhibitor of DAGLβ with an IC50 value of 42 nM.{30430} It demonstrates ~60-fold selectivity for DAGLβ over DAGLα, and negligible activity against other key enzymes involved in endocannabinoid signaling, including FAAH, MAGL, and ABHD11.{30430} KT109 has been shown to disrupt the lipid network involved in macrophage inflammatory responses, lowering 2-AG, as well as arachidonic acid (Item No. 90010) and eicosanoids, in mouse peritoneal macrophages.{30430}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • KT172 is a non-selective inhibitor of diacylglycerol lipase α (DAGLα) and DAGLβ.{30430} It inhibits DAGL-mediated hydrolysis of 1-stearoyl-2-arachidonoylglycerol (Item No. 10008650) in HEK293T cell membranes expressing recombinant DAGLα or DAGLβ (IC50s = 140 and 60 nM, respectively). KT172 also inhibits α/β-hydrolase 6 (ABHD6; IC50 = 5 nM) and weakly inhibits monoacylglycerol lipase (MAGL; IC50 = 5,000 nM) in a panel of 47 mouse serine hydrolases. It restores nicotine-stimulated GABA release in isolated ventral tegmental area (VTA) dopamine neurons from rats chronically exposed to nicotine when used at a concentration of 1 µM.{51209} KT172 decreases production of 2-arachidonoyl glycerol (Item No. 62160) and subsequently reduces arachidonic acid (Item Nos. 90010 | 90010.1 | 10006607), prostaglandin E2 (PGE2; Item No. 14010), and PGD2 (Item No. 12010) in thioglycolate-stimulated peritoneal macrophages when administered at a dose of 5 mg/kg in mice.{30430}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • KT172 is a non-selective inhibitor of diacylglycerol lipase α (DAGLα) and DAGLβ.{30430} It inhibits DAGL-mediated hydrolysis of 1-stearoyl-2-arachidonoylglycerol (Item No. 10008650) in HEK293T cell membranes expressing recombinant DAGLα or DAGLβ (IC50s = 140 and 60 nM, respectively). KT172 also inhibits α/β-hydrolase 6 (ABHD6; IC50 = 5 nM) and weakly inhibits monoacylglycerol lipase (MAGL; IC50 = 5,000 nM) in a panel of 47 mouse serine hydrolases. It restores nicotine-stimulated GABA release in isolated ventral tegmental area (VTA) dopamine neurons from rats chronically exposed to nicotine when used at a concentration of 1 µM.{51209} KT172 decreases production of 2-arachidonoyl glycerol (Item No. 62160) and subsequently reduces arachidonic acid (Item Nos. 90010 | 90010.1 | 10006607), prostaglandin E2 (PGE2; Item No. 14010), and PGD2 (Item No. 12010) in thioglycolate-stimulated peritoneal macrophages when administered at a dose of 5 mg/kg in mice.{30430}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • KT172 is a non-selective inhibitor of diacylglycerol lipase α (DAGLα) and DAGLβ.{30430} It inhibits DAGL-mediated hydrolysis of 1-stearoyl-2-arachidonoylglycerol (Item No. 10008650) in HEK293T cell membranes expressing recombinant DAGLα or DAGLβ (IC50s = 140 and 60 nM, respectively). KT172 also inhibits α/β-hydrolase 6 (ABHD6; IC50 = 5 nM) and weakly inhibits monoacylglycerol lipase (MAGL; IC50 = 5,000 nM) in a panel of 47 mouse serine hydrolases. It restores nicotine-stimulated GABA release in isolated ventral tegmental area (VTA) dopamine neurons from rats chronically exposed to nicotine when used at a concentration of 1 µM.{51209} KT172 decreases production of 2-arachidonoyl glycerol (Item No. 62160) and subsequently reduces arachidonic acid (Item Nos. 90010 | 90010.1 | 10006607), prostaglandin E2 (PGE2; Item No. 14010), and PGD2 (Item No. 12010) in thioglycolate-stimulated peritoneal macrophages when administered at a dose of 5 mg/kg in mice.{30430}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • KT172 is a non-selective inhibitor of diacylglycerol lipase α (DAGLα) and DAGLβ.{30430} It inhibits DAGL-mediated hydrolysis of 1-stearoyl-2-arachidonoylglycerol (Item No. 10008650) in HEK293T cell membranes expressing recombinant DAGLα or DAGLβ (IC50s = 140 and 60 nM, respectively). KT172 also inhibits α/β-hydrolase 6 (ABHD6; IC50 = 5 nM) and weakly inhibits monoacylglycerol lipase (MAGL; IC50 = 5,000 nM) in a panel of 47 mouse serine hydrolases. It restores nicotine-stimulated GABA release in isolated ventral tegmental area (VTA) dopamine neurons from rats chronically exposed to nicotine when used at a concentration of 1 µM.{51209} KT172 decreases production of 2-arachidonoyl glycerol (Item No. 62160) and subsequently reduces arachidonic acid (Item Nos. 90010 | 90010.1 | 10006607), prostaglandin E2 (PGE2; Item No. 14010), and PGD2 (Item No. 12010) in thioglycolate-stimulated peritoneal macrophages when administered at a dose of 5 mg/kg in mice.{30430}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • KT182 is a potent inhibitor of α/β-hydrolase domain-containing protein 6 (ABHD6) with IC50 values of 1.7, 15.1, and 0.24 nM using Neuro2a membrane proteomes, recombinant ABHD6 in HEK293T cells, and Neuro2a cells in situ, respectively.{24855} Following administration of KT182 (1 mg/kg, i.p.) in mice, ABHD6 is inactivated in liver and brain extracts, suggesting that it is brain-penetrant, unlike the closely related compound KT203 (Item No. 14819).  

     

    Brand:
    Cayman
    SKU:-
  • KT182 is a potent inhibitor of α/β-hydrolase domain-containing protein 6 (ABHD6) with IC50 values of 1.7, 15.1, and 0.24 nM using Neuro2a membrane proteomes, recombinant ABHD6 in HEK293T cells, and Neuro2a cells in situ, respectively.{24855} Following administration of KT182 (1 mg/kg, i.p.) in mice, ABHD6 is inactivated in liver and brain extracts, suggesting that it is brain-penetrant, unlike the closely related compound KT203 (Item No. 14819).  

     

    Brand:
    Cayman
    SKU:-
  • KT182 is a potent inhibitor of α/β-hydrolase domain-containing protein 6 (ABHD6) with IC50 values of 1.7, 15.1, and 0.24 nM using Neuro2a membrane proteomes, recombinant ABHD6 in HEK293T cells, and Neuro2a cells in situ, respectively.{24855} Following administration of KT182 (1 mg/kg, i.p.) in mice, ABHD6 is inactivated in liver and brain extracts, suggesting that it is brain-penetrant, unlike the closely related compound KT203 (Item No. 14819).  

     

    Brand:
    Cayman
    SKU:-
  • KT182 is a potent inhibitor of α/β-hydrolase domain-containing protein 6 (ABHD6) with IC50 values of 1.7, 15.1, and 0.24 nM using Neuro2a membrane proteomes, recombinant ABHD6 in HEK293T cells, and Neuro2a cells in situ, respectively.{24855} Following administration of KT182 (1 mg/kg, i.p.) in mice, ABHD6 is inactivated in liver and brain extracts, suggesting that it is brain-penetrant, unlike the closely related compound KT203 (Item No. 14819).  

     

    Brand:
    Cayman
    SKU:-
  • KT185 is an orally bioavailable inhibitor of α/β-hydrolase domain-containing protein 6 (ABHD6) with an IC50 value of 0.21 nM in a competitive activity-based protein profiling assay using Neuro2A membranes.{24855} It inhibits ABHD6 in a 2-arachidonoyl glycerol (2-AG; Item No. 62160) hydrolysis assay (IC50 = 13.6 nM for the mouse recombinant enzyme expressed in HEK293T cells). KT185 is selective for ABHD6 over diacylglycerol lipase β (DAGLβ) at 1 µM but inhibits lysophospholipase 1 (LYPLA1) and LYPLA2 at 10 µM. It inhibits ABHD6 activity in mouse liver and brain in vivo when administered at doses of 5-10 and approximately 40 mg/kg, respectively, without inhibiting fatty acid amide hydrolase (FAAH) in the brain. KT185 inhibits increases in the frequency of spontaneous inhibitory post-synaptic currents (sIPSCs) induced by nicotine (Item No. 29138) in the rat ventral tegmental area (VTA) but does not reduce nicotine self-administration in rats when administered intracerebroventricularly at a dose of 200 µg.{51209} It has been used as a negative control for the off-target effect of the DAGL inhibitor KT172 (Item No. 19112) on ABHD6.  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • KT185 is an orally bioavailable inhibitor of α/β-hydrolase domain-containing protein 6 (ABHD6) with an IC50 value of 0.21 nM in a competitive activity-based protein profiling assay using Neuro2A membranes.{24855} It inhibits ABHD6 in a 2-arachidonoyl glycerol (2-AG; Item No. 62160) hydrolysis assay (IC50 = 13.6 nM for the mouse recombinant enzyme expressed in HEK293T cells). KT185 is selective for ABHD6 over diacylglycerol lipase β (DAGLβ) at 1 µM but inhibits lysophospholipase 1 (LYPLA1) and LYPLA2 at 10 µM. It inhibits ABHD6 activity in mouse liver and brain in vivo when administered at doses of 5-10 and approximately 40 mg/kg, respectively, without inhibiting fatty acid amide hydrolase (FAAH) in the brain. KT185 inhibits increases in the frequency of spontaneous inhibitory post-synaptic currents (sIPSCs) induced by nicotine (Item No. 29138) in the rat ventral tegmental area (VTA) but does not reduce nicotine self-administration in rats when administered intracerebroventricularly at a dose of 200 µg.{51209} It has been used as a negative control for the off-target effect of the DAGL inhibitor KT172 (Item No. 19112) on ABHD6.  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • KT185 is an orally bioavailable inhibitor of α/β-hydrolase domain-containing protein 6 (ABHD6) with an IC50 value of 0.21 nM in a competitive activity-based protein profiling assay using Neuro2A membranes.{24855} It inhibits ABHD6 in a 2-arachidonoyl glycerol (2-AG; Item No. 62160) hydrolysis assay (IC50 = 13.6 nM for the mouse recombinant enzyme expressed in HEK293T cells). KT185 is selective for ABHD6 over diacylglycerol lipase β (DAGLβ) at 1 µM but inhibits lysophospholipase 1 (LYPLA1) and LYPLA2 at 10 µM. It inhibits ABHD6 activity in mouse liver and brain in vivo when administered at doses of 5-10 and approximately 40 mg/kg, respectively, without inhibiting fatty acid amide hydrolase (FAAH) in the brain. KT185 inhibits increases in the frequency of spontaneous inhibitory post-synaptic currents (sIPSCs) induced by nicotine (Item No. 29138) in the rat ventral tegmental area (VTA) but does not reduce nicotine self-administration in rats when administered intracerebroventricularly at a dose of 200 µg.{51209} It has been used as a negative control for the off-target effect of the DAGL inhibitor KT172 (Item No. 19112) on ABHD6.  

     

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    Cayman
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    Available on backorder

  • KT185 is an orally bioavailable inhibitor of α/β-hydrolase domain-containing protein 6 (ABHD6) with an IC50 value of 0.21 nM in a competitive activity-based protein profiling assay using Neuro2A membranes.{24855} It inhibits ABHD6 in a 2-arachidonoyl glycerol (2-AG; Item No. 62160) hydrolysis assay (IC50 = 13.6 nM for the mouse recombinant enzyme expressed in HEK293T cells). KT185 is selective for ABHD6 over diacylglycerol lipase β (DAGLβ) at 1 µM but inhibits lysophospholipase 1 (LYPLA1) and LYPLA2 at 10 µM. It inhibits ABHD6 activity in mouse liver and brain in vivo when administered at doses of 5-10 and approximately 40 mg/kg, respectively, without inhibiting fatty acid amide hydrolase (FAAH) in the brain. KT185 inhibits increases in the frequency of spontaneous inhibitory post-synaptic currents (sIPSCs) induced by nicotine (Item No. 29138) in the rat ventral tegmental area (VTA) but does not reduce nicotine self-administration in rats when administered intracerebroventricularly at a dose of 200 µg.{51209} It has been used as a negative control for the off-target effect of the DAGL inhibitor KT172 (Item No. 19112) on ABHD6.  

     

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    Cayman
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    Available on backorder

  • The serine hydrolase known as α/β-hydrolase domain-containing protein 6 (ABHD6) hydrolyzes 2-arachidonoyl glycerol (2-AG; Item No. 62160) to regulate its availability at cannabinoid receptors. KT195 is a selective inhibitor of ABHD6 (IC50 = 10 nM) with negligible activity against other serine hydrolases such as DAGLβ.{30430,30418} While it can be used as a probe to study ABHD6, it also has use as a negative control for studies of DAGLβ.{30430} By inactivating ABHD6, KT195 has been shown to induce a significant accumulation of 2-AG in Neuro2a cells.{30430} KT195 is also reported to reduce IL-1β secretion from lipopolysaccharide-treated macrophages.{30430}  

     

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    Cayman
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  • The serine hydrolase known as α/β-hydrolase domain-containing protein 6 (ABHD6) hydrolyzes 2-arachidonoyl glycerol (2-AG; Item No. 62160) to regulate its availability at cannabinoid receptors. KT195 is a selective inhibitor of ABHD6 (IC50 = 10 nM) with negligible activity against other serine hydrolases such as DAGLβ.{30430,30418} While it can be used as a probe to study ABHD6, it also has use as a negative control for studies of DAGLβ.{30430} By inactivating ABHD6, KT195 has been shown to induce a significant accumulation of 2-AG in Neuro2a cells.{30430} KT195 is also reported to reduce IL-1β secretion from lipopolysaccharide-treated macrophages.{30430}  

     

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    Cayman
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  • The serine hydrolase known as α/β-hydrolase domain-containing protein 6 (ABHD6) hydrolyzes 2-arachidonoyl glycerol (2-AG; Item No. 62160) to regulate its availability at cannabinoid receptors. KT195 is a selective inhibitor of ABHD6 (IC50 = 10 nM) with negligible activity against other serine hydrolases such as DAGLβ.{30430,30418} While it can be used as a probe to study ABHD6, it also has use as a negative control for studies of DAGLβ.{30430} By inactivating ABHD6, KT195 has been shown to induce a significant accumulation of 2-AG in Neuro2a cells.{30430} KT195 is also reported to reduce IL-1β secretion from lipopolysaccharide-treated macrophages.{30430}  

     

    Brand:
    Cayman
    SKU:-
  • The serine hydrolase known as α/β-hydrolase domain-containing protein 6 (ABHD6) hydrolyzes 2-arachidonoyl glycerol (2-AG; Item No. 62160) to regulate its availability at cannabinoid receptors. KT195 is a selective inhibitor of ABHD6 (IC50 = 10 nM) with negligible activity against other serine hydrolases such as DAGLβ.{30430,30418} While it can be used as a probe to study ABHD6, it also has use as a negative control for studies of DAGLβ.{30430} By inactivating ABHD6, KT195 has been shown to induce a significant accumulation of 2-AG in Neuro2a cells.{30430} KT195 is also reported to reduce IL-1β secretion from lipopolysaccharide-treated macrophages.{30430}  

     

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    Cayman
    SKU:-
  • KT203 is a potent inhibitor of α/β-hydrolase domain-containing protein 6 (ABHD6) with IC50 values of 0.82, 3.9, and 0.31 nM using Neuro2A membrane proteomes, recombinant ABHD6 in HEK293T cells, and Neuro2A cells in situ, respectively.{24855} Following administration of KT203 (1 mg/kg, i.p.) in mice, ABHD6 is inactivated in liver but not brain extracts, suggesting that KT203 is not brain-penetrant.  

     

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    Cayman
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  • KT203 is a potent inhibitor of α/β-hydrolase domain-containing protein 6 (ABHD6) with IC50 values of 0.82, 3.9, and 0.31 nM using Neuro2A membrane proteomes, recombinant ABHD6 in HEK293T cells, and Neuro2A cells in situ, respectively.{24855} Following administration of KT203 (1 mg/kg, i.p.) in mice, ABHD6 is inactivated in liver but not brain extracts, suggesting that KT203 is not brain-penetrant.  

     

    Brand:
    Cayman
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  • KT203 is a potent inhibitor of α/β-hydrolase domain-containing protein 6 (ABHD6) with IC50 values of 0.82, 3.9, and 0.31 nM using Neuro2A membrane proteomes, recombinant ABHD6 in HEK293T cells, and Neuro2A cells in situ, respectively.{24855} Following administration of KT203 (1 mg/kg, i.p.) in mice, ABHD6 is inactivated in liver but not brain extracts, suggesting that KT203 is not brain-penetrant.  

     

    Brand:
    Cayman
    SKU:-
  • KT203 is a potent inhibitor of α/β-hydrolase domain-containing protein 6 (ABHD6) with IC50 values of 0.82, 3.9, and 0.31 nM using Neuro2A membrane proteomes, recombinant ABHD6 in HEK293T cells, and Neuro2A cells in situ, respectively.{24855} Following administration of KT203 (1 mg/kg, i.p.) in mice, ABHD6 is inactivated in liver but not brain extracts, suggesting that KT203 is not brain-penetrant.  

     

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    Cayman
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  • Ku-0060648 is an ATP-competitive inhibitor of DNA-dependent protein kinase (DNA-PK) and an inhibitor of PI3K. In a cell-free assay, it has IC50s of 5, 4, 0.5, 50s of 19 and 39 nM, for DNA-PK and PI3K, respectively, while in SW620 cells, it has an IC50 of 170 nM for DNA-PK but >10,000 nM for PI3K.{34167} Ku-0060648 is useful for Cas9 editing due to its DNA-PK inhibition, which reduces the frequency of non-homologous end joining and increases homology-directed recombination.{34168} It also shows promise in cancer research in vitro and in vivo.{34165,34166}  

     

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    Cayman
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  • Ku-0060648 is an ATP-competitive inhibitor of DNA-dependent protein kinase (DNA-PK) and an inhibitor of PI3K. In a cell-free assay, it has IC50s of 5, 4, 0.5, 50s of 19 and 39 nM, for DNA-PK and PI3K, respectively, while in SW620 cells, it has an IC50 of 170 nM for DNA-PK but >10,000 nM for PI3K.{34167} Ku-0060648 is useful for Cas9 editing due to its DNA-PK inhibition, which reduces the frequency of non-homologous end joining and increases homology-directed recombination.{34168} It also shows promise in cancer research in vitro and in vivo.{34165,34166}  

     

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    Cayman
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  • Ku-0060648 is an ATP-competitive inhibitor of DNA-dependent protein kinase (DNA-PK) and an inhibitor of PI3K. In a cell-free assay, it has IC50s of 5, 4, 0.5, 50s of 19 and 39 nM, for DNA-PK and PI3K, respectively, while in SW620 cells, it has an IC50 of 170 nM for DNA-PK but >10,000 nM for PI3K.{34167} Ku-0060648 is useful for Cas9 editing due to its DNA-PK inhibition, which reduces the frequency of non-homologous end joining and increases homology-directed recombination.{34168} It also shows promise in cancer research in vitro and in vivo.{34165,34166}  

     

    Brand:
    Cayman
    SKU:-
  • Ku-0060648 is an ATP-competitive inhibitor of DNA-dependent protein kinase (DNA-PK) and an inhibitor of PI3K. In a cell-free assay, it has IC50s of 5, 4, 0.5, 50s of 19 and 39 nM, for DNA-PK and PI3K, respectively, while in SW620 cells, it has an IC50 of 170 nM for DNA-PK but >10,000 nM for PI3K.{34167} Ku-0060648 is useful for Cas9 editing due to its DNA-PK inhibition, which reduces the frequency of non-homologous end joining and increases homology-directed recombination.{34168} It also shows promise in cancer research in vitro and in vivo.{34165,34166}  

     

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    Cayman
    SKU:-
  • The mammalian target of rapamycin (mTOR) is a serine-threonine kinase which acts as part of two distinct complexes, TORC1 and TORC2. Both complexes (TORC1/2) play central roles in cell growth, gene expression, angiogenesis, and cell survival.{16931} Ku-0063794 is a cell-permeable, selective dual inhibitor of mTORC1 and mTORC2 (IC50 = 10 nM).{17538} It does not affect the activity of 76 other protein kinases or seven lipid kinases, including PI3Ks.{17538} Ku-0063794 inhibits cell growth by inducing G1-cell cycle arrest and autophagy, but not apoptosis, and inhibits tumor growth in a xenograft model of renal cell carcinoma (8 mg/kg for 46 days).{17538,23552,23551}  

     

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    Cayman
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  • The mammalian target of rapamycin (mTOR) is a serine-threonine kinase which acts as part of two distinct complexes, TORC1 and TORC2. Both complexes (TORC1/2) play central roles in cell growth, gene expression, angiogenesis, and cell survival.{16931} Ku-0063794 is a cell-permeable, selective dual inhibitor of mTORC1 and mTORC2 (IC50 = 10 nM).{17538} It does not affect the activity of 76 other protein kinases or seven lipid kinases, including PI3Ks.{17538} Ku-0063794 inhibits cell growth by inducing G1-cell cycle arrest and autophagy, but not apoptosis, and inhibits tumor growth in a xenograft model of renal cell carcinoma (8 mg/kg for 46 days).{17538,23552,23551}  

     

    Brand:
    Cayman
    SKU:-
  • The mammalian target of rapamycin (mTOR) is a serine-threonine kinase which acts as part of two distinct complexes, TORC1 and TORC2. Both complexes (TORC1/2) play central roles in cell growth, gene expression, angiogenesis, and cell survival.{16931} Ku-0063794 is a cell-permeable, selective dual inhibitor of mTORC1 and mTORC2 (IC50 = 10 nM).{17538} It does not affect the activity of 76 other protein kinases or seven lipid kinases, including PI3Ks.{17538} Ku-0063794 inhibits cell growth by inducing G1-cell cycle arrest and autophagy, but not apoptosis, and inhibits tumor growth in a xenograft model of renal cell carcinoma (8 mg/kg for 46 days).{17538,23552,23551}  

     

    Brand:
    Cayman
    SKU:-
  • The mammalian target of rapamycin (mTOR) is a serine-threonine kinase which acts as part of two distinct complexes, TORC1 and TORC2. Both complexes (TORC1/2) play central roles in cell growth, gene expression, angiogenesis, and cell survival.{16931} Ku-0063794 is a cell-permeable, selective dual inhibitor of mTORC1 and mTORC2 (IC50 = 10 nM).{17538} It does not affect the activity of 76 other protein kinases or seven lipid kinases, including PI3Ks.{17538} Ku-0063794 inhibits cell growth by inducing G1-cell cycle arrest and autophagy, but not apoptosis, and inhibits tumor growth in a xenograft model of renal cell carcinoma (8 mg/kg for 46 days).{17538,23552,23551}  

     

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    Cayman
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  • Ku-55933 is a potent ATP-competitive inhibitor of the ataxia-telangiectasia mutated (ATM) kinase (IC50 = 13 nM; Ki = 2.2 nM).{26647} Inhibition of ATM by Ku-55933 blocks radiation-induced phosphorylation of downstream cellular targets and sensitizes cells to the cytotoxic effects of both ionizing radiation and chemotherapeutic agents.{26647} Ku-55933 induces senescent breast, lung, and colon carcinoma cells to undergo cell death.{26648} It also inhibits HIV-1 replication in C8166 human T-lymophocyte cells with an IC50 value of 2.4 µM.{26649}  

     

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    Cayman
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    Out of stock

  • Ku-55933 is a potent ATP-competitive inhibitor of the ataxia-telangiectasia mutated (ATM) kinase (IC50 = 13 nM; Ki = 2.2 nM).{26647} Inhibition of ATM by Ku-55933 blocks radiation-induced phosphorylation of downstream cellular targets and sensitizes cells to the cytotoxic effects of both ionizing radiation and chemotherapeutic agents.{26647} Ku-55933 induces senescent breast, lung, and colon carcinoma cells to undergo cell death.{26648} It also inhibits HIV-1 replication in C8166 human T-lymophocyte cells with an IC50 value of 2.4 µM.{26649}  

     

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    Cayman
    SKU:-

    Out of stock

  • Ku-55933 is a potent ATP-competitive inhibitor of the ataxia-telangiectasia mutated (ATM) kinase (IC50 = 13 nM; Ki = 2.2 nM).{26647} Inhibition of ATM by Ku-55933 blocks radiation-induced phosphorylation of downstream cellular targets and sensitizes cells to the cytotoxic effects of both ionizing radiation and chemotherapeutic agents.{26647} Ku-55933 induces senescent breast, lung, and colon carcinoma cells to undergo cell death.{26648} It also inhibits HIV-1 replication in C8166 human T-lymophocyte cells with an IC50 value of 2.4 µM.{26649}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • Ku-55933 is a potent ATP-competitive inhibitor of the ataxia-telangiectasia mutated (ATM) kinase (IC50 = 13 nM; Ki = 2.2 nM).{26647} Inhibition of ATM by Ku-55933 blocks radiation-induced phosphorylation of downstream cellular targets and sensitizes cells to the cytotoxic effects of both ionizing radiation and chemotherapeutic agents.{26647} Ku-55933 induces senescent breast, lung, and colon carcinoma cells to undergo cell death.{26648} It also inhibits HIV-1 replication in C8166 human T-lymophocyte cells with an IC50 value of 2.4 µM.{26649}  

     

    Brand:
    Cayman
    SKU:-

    Out of stock

  • Ataxia-telangiectasia mutated (ATM) is a serine/threonine kinase that activates checkpoint signaling following double strand DNA breaks and genotoxic stress. Ku-60019 is a potent, reversible inhibitor of ATM kinase (IC50 = 6.3 nM), blocking the phosphorylation of ATM substrate proteins.{28729,28730} It is much less effective or without effect against a panel of 229 other kinases.{28729} Ku-60019 sensitizes glioma cells to radiation and inhibits migration and invasion of glioma cells in vitro.{28729,28730} It produces radiosensitization and increases survival in vivo when administered intra-tumorally in orthotopic xenograft models of glioblastoma multiforme.{28728} Ku-60019 is particularly effective in producing lethality in cells with mutant p53 or that are deficient in PTEN.{28728,28731}  

     

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    Cayman
    SKU:-

    Available on backorder

  • Ataxia-telangiectasia mutated (ATM) is a serine/threonine kinase that activates checkpoint signaling following double strand DNA breaks and genotoxic stress. Ku-60019 is a potent, reversible inhibitor of ATM kinase (IC50 = 6.3 nM), blocking the phosphorylation of ATM substrate proteins.{28729,28730} It is much less effective or without effect against a panel of 229 other kinases.{28729} Ku-60019 sensitizes glioma cells to radiation and inhibits migration and invasion of glioma cells in vitro.{28729,28730} It produces radiosensitization and increases survival in vivo when administered intra-tumorally in orthotopic xenograft models of glioblastoma multiforme.{28728} Ku-60019 is particularly effective in producing lethality in cells with mutant p53 or that are deficient in PTEN.{28728,28731}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder

  • Ataxia-telangiectasia mutated (ATM) is a serine/threonine kinase that activates checkpoint signaling following double strand DNA breaks and genotoxic stress. Ku-60019 is a potent, reversible inhibitor of ATM kinase (IC50 = 6.3 nM), blocking the phosphorylation of ATM substrate proteins.{28729,28730} It is much less effective or without effect against a panel of 229 other kinases.{28729} Ku-60019 sensitizes glioma cells to radiation and inhibits migration and invasion of glioma cells in vitro.{28729,28730} It produces radiosensitization and increases survival in vivo when administered intra-tumorally in orthotopic xenograft models of glioblastoma multiforme.{28728} Ku-60019 is particularly effective in producing lethality in cells with mutant p53 or that are deficient in PTEN.{28728,28731}  

     

    Brand:
    Cayman
    SKU:-

    Available on backorder