Chemicals
Showing 24151–24300 of 41137 results
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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:CaymanSKU: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:CaymanSKU: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:CaymanSKU: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:CaymanSKU: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:CaymanSKU:10011011 - 100 µgAvailable 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:CaymanSKU:10011011 - 250 µgAvailable 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:CaymanSKU:10011011 - 50 µgAvailable 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:CaymanSKU:10011011 - 500 µgAvailable 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:CaymanSKU:10010965 - 100 µgAvailable 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:CaymanSKU:10010965 - 25 µgAvailable 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:CaymanSKU:10010965 - 50 µgAvailable 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:CaymanSKU:10010965 - 500 µgAvailable 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:CaymanSKU:-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:CaymanSKU:-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:CaymanSKU:-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:CaymanSKU:-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:CaymanSKU:-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:CaymanSKU:-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:CaymanSKU:-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:CaymanSKU:- 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:CaymanSKU:- 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:CaymanSKU:- 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:CaymanSKU:-
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:CaymanSKU:-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:CaymanSKU:-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:CaymanSKU:-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:CaymanSKU:-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}
Brand:CaymanSKU:- 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:CaymanSKU:- 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:CaymanSKU:- 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:CaymanSKU:-
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:CaymanSKU:- 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:CaymanSKU:- 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:CaymanSKU:- 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:CaymanSKU:-
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:CaymanSKU:- 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:CaymanSKU:- 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:CaymanSKU:- 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:CaymanSKU:-
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:CaymanSKU:- 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:CaymanSKU:- 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:CaymanSKU:- 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:CaymanSKU:-
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:CaymanSKU:-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:CaymanSKU:-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:CaymanSKU:-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:CaymanSKU:-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}
Brand:CaymanSKU:-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:CaymanSKU:-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:CaymanSKU:-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:CaymanSKU:-Available on backorder
Kukoamine A is a spermine alkaloid originally isolated from L. chinense that has diverse biological activities, including anticancer, neuroprotective, and anti-inflammatory properties.{47073} Kukoamine A (5-20 µg/ml) inhibits colony formation of U251 and WJ1 glioblastoma cells in a concentration-dependent manner.{47074} It halts the cell cycle at the G0/G1 phase and induces apoptosis when used at concentrations of 60 and 80 µg/ml. Kukoamine A (20 and 40 µM) induces autophagy and increases cell viability in an SH-SY5Y cell model of MPP-induced injury.{47075} It increases the number of dopamine neurons in the substantia nigra and striatum, decreases α-synuclein expression, and improves motor function in an MPTP mouse model of Parkinson’s disease when administered at a dose of 20 mg/kg per day. Kukoamine A (10 and 20 mg/kg) decreases IL-1β, TNF-α, and COX-2 protein levels in the hippocampus and increases hippocampal neurogenesis in a rat model of radiation injury.{47076} It also selectively inhibits trypanothione reductase (Ki = 1.8 µM), an enzyme that protects certain parasites from oxidative stress, over human glutathione reductase (Ki = >10 mM).{47077}
Brand:CaymanSKU:25139 - 1 mgAvailable on backorder
Kukoamine A is a spermine alkaloid originally isolated from L. chinense that has diverse biological activities, including anticancer, neuroprotective, and anti-inflammatory properties.{47073} Kukoamine A (5-20 µg/ml) inhibits colony formation of U251 and WJ1 glioblastoma cells in a concentration-dependent manner.{47074} It halts the cell cycle at the G0/G1 phase and induces apoptosis when used at concentrations of 60 and 80 µg/ml. Kukoamine A (20 and 40 µM) induces autophagy and increases cell viability in an SH-SY5Y cell model of MPP-induced injury.{47075} It increases the number of dopamine neurons in the substantia nigra and striatum, decreases α-synuclein expression, and improves motor function in an MPTP mouse model of Parkinson’s disease when administered at a dose of 20 mg/kg per day. Kukoamine A (10 and 20 mg/kg) decreases IL-1β, TNF-α, and COX-2 protein levels in the hippocampus and increases hippocampal neurogenesis in a rat model of radiation injury.{47076} It also selectively inhibits trypanothione reductase (Ki = 1.8 µM), an enzyme that protects certain parasites from oxidative stress, over human glutathione reductase (Ki = >10 mM).{47077}
Brand:CaymanSKU:25139 - 10 mgAvailable on backorder
Kukoamine A is a spermine alkaloid originally isolated from L. chinense that has diverse biological activities, including anticancer, neuroprotective, and anti-inflammatory properties.{47073} Kukoamine A (5-20 µg/ml) inhibits colony formation of U251 and WJ1 glioblastoma cells in a concentration-dependent manner.{47074} It halts the cell cycle at the G0/G1 phase and induces apoptosis when used at concentrations of 60 and 80 µg/ml. Kukoamine A (20 and 40 µM) induces autophagy and increases cell viability in an SH-SY5Y cell model of MPP-induced injury.{47075} It increases the number of dopamine neurons in the substantia nigra and striatum, decreases α-synuclein expression, and improves motor function in an MPTP mouse model of Parkinson’s disease when administered at a dose of 20 mg/kg per day. Kukoamine A (10 and 20 mg/kg) decreases IL-1β, TNF-α, and COX-2 protein levels in the hippocampus and increases hippocampal neurogenesis in a rat model of radiation injury.{47076} It also selectively inhibits trypanothione reductase (Ki = 1.8 µM), an enzyme that protects certain parasites from oxidative stress, over human glutathione reductase (Ki = >10 mM).{47077}
Brand:CaymanSKU:25139 - 5 mgAvailable on backorder
Kukoamine B is a spermine alkaloid first isolated from a traditional Chinese herb L. chinense that inhibits both lipopolysaccharides (LPS) and oligodeoxynucleotides containing CpG motifs (CpG DNA).{33457} It is reported to inhibit proinflammatory signal transduction and cytokine expression induced by LPS and CpG DNA (Kds = 1.24 and 0.66 µM).{33457} LPS and CpG DNA are two well-recognized pathogen-associated molecular patterns (PAMPs) that play a role in triggering sepsis, thus sepsis may be attenuated by simultaneously neutralizing LPS and CpG DNA.{33457}
Brand:CaymanSKU:21091 -Out of stock
Kukoamine B is a spermine alkaloid first isolated from a traditional Chinese herb L. chinense that inhibits both lipopolysaccharides (LPS) and oligodeoxynucleotides containing CpG motifs (CpG DNA).{33457} It is reported to inhibit proinflammatory signal transduction and cytokine expression induced by LPS and CpG DNA (Kds = 1.24 and 0.66 µM).{33457} LPS and CpG DNA are two well-recognized pathogen-associated molecular patterns (PAMPs) that play a role in triggering sepsis, thus sepsis may be attenuated by simultaneously neutralizing LPS and CpG DNA.{33457}
Brand:CaymanSKU:21091 -Out of stock
Kukoamine B is a spermine alkaloid first isolated from a traditional Chinese herb L. chinense that inhibits both lipopolysaccharides (LPS) and oligodeoxynucleotides containing CpG motifs (CpG DNA).{33457} It is reported to inhibit proinflammatory signal transduction and cytokine expression induced by LPS and CpG DNA (Kds = 1.24 and 0.66 µM).{33457} LPS and CpG DNA are two well-recognized pathogen-associated molecular patterns (PAMPs) that play a role in triggering sepsis, thus sepsis may be attenuated by simultaneously neutralizing LPS and CpG DNA.{33457}
Brand:CaymanSKU:21091 -Out of stock
Kukoamine B is a spermine alkaloid first isolated from a traditional Chinese herb L. chinense that inhibits both lipopolysaccharides (LPS) and oligodeoxynucleotides containing CpG motifs (CpG DNA).{33457} It is reported to inhibit proinflammatory signal transduction and cytokine expression induced by LPS and CpG DNA (Kds = 1.24 and 0.66 µM).{33457} LPS and CpG DNA are two well-recognized pathogen-associated molecular patterns (PAMPs) that play a role in triggering sepsis, thus sepsis may be attenuated by simultaneously neutralizing LPS and CpG DNA.{33457}
Brand:CaymanSKU:21091 -Out of stock
Kumbicin C is a bis-indolyl benzenoid fungal metabolite produced by A. kumbius FRR6049.{39715} It inhibits the growth of NS-1 mouse myeloma cells (IC50 = 0.74 μg/ml). Kumbicin C also inhibits the growth of the Gram-positive bacteria B. subtilis (MIC = 1.6 μg/ml).
Brand:CaymanSKU:25015 - 1 mgAvailable on backorder
Kumbicin C is a bis-indolyl benzenoid fungal metabolite produced by A. kumbius FRR6049.{39715} It inhibits the growth of NS-1 mouse myeloma cells (IC50 = 0.74 μg/ml). Kumbicin C also inhibits the growth of the Gram-positive bacteria B. subtilis (MIC = 1.6 μg/ml).
Brand:CaymanSKU:25015 - 250 µgAvailable on backorder
KUS121 is a valosin-containing protein (VCP) modulator that inhibits VCP ATPase activity (IC50 = 330 nM).{56033} It inhibits cell death, ATP depletion, and upregulation of C/EBP-homologous protein (CHOP) induced by tunicamycin, an inducer of ER stress, in HeLa cells when used at concentrations of 20, 50, and 50 μM, respectively. KUS121 (100 μM) inhibits ATP depletion and cell death induced by oxygen-glucose deprivation (OGD) in rat primary cortical neurons in an in vitro model of cerebral ischemia.{45805} It reduces infarction volume and increases the latency to fall in an accelerating rotarod test in a mouse model of focal cerebral ischemia induced by transient distal middle cerebral artery occlusion (MCAO) when administered at a dose of 100 mg/kg immediately following occlusion and again at 50 mg/kg following reperfusion. KUS121 (50 mg/kg) inhibits thinning of the retinal outer nuclear layer and preserves visual function in an rd10 mouse model of retinitis pigmentosa.{56033}
Brand:CaymanSKU:30297 - 1 mgAvailable on backorder
KUS121 is a valosin-containing protein (VCP) modulator that inhibits VCP ATPase activity (IC50 = 330 nM).{56033} It inhibits cell death, ATP depletion, and upregulation of C/EBP-homologous protein (CHOP) induced by tunicamycin, an inducer of ER stress, in HeLa cells when used at concentrations of 20, 50, and 50 μM, respectively. KUS121 (100 μM) inhibits ATP depletion and cell death induced by oxygen-glucose deprivation (OGD) in rat primary cortical neurons in an in vitro model of cerebral ischemia.{45805} It reduces infarction volume and increases the latency to fall in an accelerating rotarod test in a mouse model of focal cerebral ischemia induced by transient distal middle cerebral artery occlusion (MCAO) when administered at a dose of 100 mg/kg immediately following occlusion and again at 50 mg/kg following reperfusion. KUS121 (50 mg/kg) inhibits thinning of the retinal outer nuclear layer and preserves visual function in an rd10 mouse model of retinitis pigmentosa.{56033}
Brand:CaymanSKU:30297 - 10 mgAvailable on backorder
KUS121 is a valosin-containing protein (VCP) modulator that inhibits VCP ATPase activity (IC50 = 330 nM).{56033} It inhibits cell death, ATP depletion, and upregulation of C/EBP-homologous protein (CHOP) induced by tunicamycin, an inducer of ER stress, in HeLa cells when used at concentrations of 20, 50, and 50 μM, respectively. KUS121 (100 μM) inhibits ATP depletion and cell death induced by oxygen-glucose deprivation (OGD) in rat primary cortical neurons in an in vitro model of cerebral ischemia.{45805} It reduces infarction volume and increases the latency to fall in an accelerating rotarod test in a mouse model of focal cerebral ischemia induced by transient distal middle cerebral artery occlusion (MCAO) when administered at a dose of 100 mg/kg immediately following occlusion and again at 50 mg/kg following reperfusion. KUS121 (50 mg/kg) inhibits thinning of the retinal outer nuclear layer and preserves visual function in an rd10 mouse model of retinitis pigmentosa.{56033}
Brand:CaymanSKU:30297 - 5 mgAvailable on backorder
KW 2449 is a potent multi-kinase inhibitor of fml-like tyrosine kinase 3 (FLT3), Abelson tyrosine-protein kinase 1 (ABL), ABL-T315I, and Aurora kinase (IC50s = 6.6, 14, 4, and 48 nM, respectively).{40201} It has growth inhibitory activity against leukemia cells expressing FLT3 with activating mutations (GI50s = 11-46 nM) and suppresses phosphorylation of FLT3 and STAT5 in MOLM-13 cells in a dose-dependent manner in vitro. KW 2499 (100 nM) inhibits colony formation of human primary acute myeloid leukemia (AML) cells with wild-type or activated mutant FLT3. It also induces MOLM-13 xenograft regression in a dose-dependent manner in vivo. Formulations containing KW 2499 are being investigated in clinical trials for treatment of relapsed or refractory AML.
Brand:CaymanSKU:22207 -Out of stock
KW 2449 is a potent multi-kinase inhibitor of fml-like tyrosine kinase 3 (FLT3), Abelson tyrosine-protein kinase 1 (ABL), ABL-T315I, and Aurora kinase (IC50s = 6.6, 14, 4, and 48 nM, respectively).{40201} It has growth inhibitory activity against leukemia cells expressing FLT3 with activating mutations (GI50s = 11-46 nM) and suppresses phosphorylation of FLT3 and STAT5 in MOLM-13 cells in a dose-dependent manner in vitro. KW 2499 (100 nM) inhibits colony formation of human primary acute myeloid leukemia (AML) cells with wild-type or activated mutant FLT3. It also induces MOLM-13 xenograft regression in a dose-dependent manner in vivo. Formulations containing KW 2499 are being investigated in clinical trials for treatment of relapsed or refractory AML.
Brand:CaymanSKU:22207 -Out of stock
KW 2449 is a potent multi-kinase inhibitor of fml-like tyrosine kinase 3 (FLT3), Abelson tyrosine-protein kinase 1 (ABL), ABL-T315I, and Aurora kinase (IC50s = 6.6, 14, 4, and 48 nM, respectively).{40201} It has growth inhibitory activity against leukemia cells expressing FLT3 with activating mutations (GI50s = 11-46 nM) and suppresses phosphorylation of FLT3 and STAT5 in MOLM-13 cells in a dose-dependent manner in vitro. KW 2499 (100 nM) inhibits colony formation of human primary acute myeloid leukemia (AML) cells with wild-type or activated mutant FLT3. It also induces MOLM-13 xenograft regression in a dose-dependent manner in vivo. Formulations containing KW 2499 are being investigated in clinical trials for treatment of relapsed or refractory AML.
Brand:CaymanSKU:22207 -Out of stock
KW 2449 is a potent multi-kinase inhibitor of fml-like tyrosine kinase 3 (FLT3), Abelson tyrosine-protein kinase 1 (ABL), ABL-T315I, and Aurora kinase (IC50s = 6.6, 14, 4, and 48 nM, respectively).{40201} It has growth inhibitory activity against leukemia cells expressing FLT3 with activating mutations (GI50s = 11-46 nM) and suppresses phosphorylation of FLT3 and STAT5 in MOLM-13 cells in a dose-dependent manner in vitro. KW 2499 (100 nM) inhibits colony formation of human primary acute myeloid leukemia (AML) cells with wild-type or activated mutant FLT3. It also induces MOLM-13 xenograft regression in a dose-dependent manner in vivo. Formulations containing KW 2499 are being investigated in clinical trials for treatment of relapsed or refractory AML.
Brand:CaymanSKU:22207 -Out of stock
KW 2478 is an inhibitor of heat shock protein 90 (Hsp90; IC50 = 3.8 nM for Hsp90α).{42521} It inhibits the growth of OPM-2/GFP, KMS011, RPMI 8226, and NCI-H929 multiple myeloma cells (GI50s = 0.3, 0.34, 0.39, and 0.12 μM, respectively) and Raji, SR, and SC-1 non-Hodgkin’s lymphoma cells (GI50s = 0.39, 0.098, and 0.33 μM, respectively). KW 2478 decreases expression of the Hsp90 client proteins IGF-IRβ and c-RAF-1 and induces apoptosis in OPM-2/GFP and NCI-H929 cells. In vivo, KW 2478 (100 mg/kg) reduces IGF-IRβ, c-RAF-1, Cdk9, and phosphorylated ERK1/2 protein levels in tumor tissue and decreases tumor growth in an NCI-H929 mouse xenograft model.
Brand:CaymanSKU:22418 -Out of stock
KW 2478 is an inhibitor of heat shock protein 90 (Hsp90; IC50 = 3.8 nM for Hsp90α).{42521} It inhibits the growth of OPM-2/GFP, KMS011, RPMI 8226, and NCI-H929 multiple myeloma cells (GI50s = 0.3, 0.34, 0.39, and 0.12 μM, respectively) and Raji, SR, and SC-1 non-Hodgkin’s lymphoma cells (GI50s = 0.39, 0.098, and 0.33 μM, respectively). KW 2478 decreases expression of the Hsp90 client proteins IGF-IRβ and c-RAF-1 and induces apoptosis in OPM-2/GFP and NCI-H929 cells. In vivo, KW 2478 (100 mg/kg) reduces IGF-IRβ, c-RAF-1, Cdk9, and phosphorylated ERK1/2 protein levels in tumor tissue and decreases tumor growth in an NCI-H929 mouse xenograft model.
Brand:CaymanSKU:22418 -Out of stock
KW 2478 is an inhibitor of heat shock protein 90 (Hsp90; IC50 = 3.8 nM for Hsp90α).{42521} It inhibits the growth of OPM-2/GFP, KMS011, RPMI 8226, and NCI-H929 multiple myeloma cells (GI50s = 0.3, 0.34, 0.39, and 0.12 μM, respectively) and Raji, SR, and SC-1 non-Hodgkin’s lymphoma cells (GI50s = 0.39, 0.098, and 0.33 μM, respectively). KW 2478 decreases expression of the Hsp90 client proteins IGF-IRβ and c-RAF-1 and induces apoptosis in OPM-2/GFP and NCI-H929 cells. In vivo, KW 2478 (100 mg/kg) reduces IGF-IRβ, c-RAF-1, Cdk9, and phosphorylated ERK1/2 protein levels in tumor tissue and decreases tumor growth in an NCI-H929 mouse xenograft model.
Brand:CaymanSKU:22418 -Out of stock
KW 2478 is an inhibitor of heat shock protein 90 (Hsp90; IC50 = 3.8 nM for Hsp90α).{42521} It inhibits the growth of OPM-2/GFP, KMS011, RPMI 8226, and NCI-H929 multiple myeloma cells (GI50s = 0.3, 0.34, 0.39, and 0.12 μM, respectively) and Raji, SR, and SC-1 non-Hodgkin’s lymphoma cells (GI50s = 0.39, 0.098, and 0.33 μM, respectively). KW 2478 decreases expression of the Hsp90 client proteins IGF-IRβ and c-RAF-1 and induces apoptosis in OPM-2/GFP and NCI-H929 cells. In vivo, KW 2478 (100 mg/kg) reduces IGF-IRβ, c-RAF-1, Cdk9, and phosphorylated ERK1/2 protein levels in tumor tissue and decreases tumor growth in an NCI-H929 mouse xenograft model.
Brand:CaymanSKU:22418 -Out of stock
KW 3902 is an antagonist of the adenosine A1 receptor (Ki = 0.19 nM).{34380,34379} It displays 890-fold selectivity for A1 receptors over A2A receptors and has no activity at A3 receptors. KW 3902 less potently inhibits human organic anion transporter 1 (OAT1; Ki = 7.82 µM).{23931} KW 3902 exhibits renal protective effects during hypoxemia in rabbits.{34378}
Brand:CaymanSKU:11940 - 1 mgAvailable on backorder
KW 3902 is an antagonist of the adenosine A1 receptor (Ki = 0.19 nM).{34380,34379} It displays 890-fold selectivity for A1 receptors over A2A receptors and has no activity at A3 receptors. KW 3902 less potently inhibits human organic anion transporter 1 (OAT1; Ki = 7.82 µM).{23931} KW 3902 exhibits renal protective effects during hypoxemia in rabbits.{34378}
Brand:CaymanSKU:11940 - 10 mgAvailable on backorder
KW 3902 is an antagonist of the adenosine A1 receptor (Ki = 0.19 nM).{34380,34379} It displays 890-fold selectivity for A1 receptors over A2A receptors and has no activity at A3 receptors. KW 3902 less potently inhibits human organic anion transporter 1 (OAT1; Ki = 7.82 µM).{23931} KW 3902 exhibits renal protective effects during hypoxemia in rabbits.{34378}
Brand:CaymanSKU:11940 - 25 mgAvailable on backorder
KW 3902 is an antagonist of the adenosine A1 receptor (Ki = 0.19 nM).{34380,34379} It displays 890-fold selectivity for A1 receptors over A2A receptors and has no activity at A3 receptors. KW 3902 less potently inhibits human organic anion transporter 1 (OAT1; Ki = 7.82 µM).{23931} KW 3902 exhibits renal protective effects during hypoxemia in rabbits.{34378}
Brand:CaymanSKU:11940 - 5 mgAvailable on backorder
KX1-004 is a non-ATP competitive inhibitor of Src protein tyrosine kinase (Src-PTK; IC50 = 40 µM).{41235} It protects against a permanent threshold shift in the auditory threshold and against outer hair cell loss in chinchillas following noise exposure at 106 dB when used at 30, 50, or 100 µM on the round window membrane of the ear. KX1-004 (50 mg/kg) is also effective against chronic noise exposure when administered systemically in chinchillas.{41234}
Brand:CaymanSKU:22198 -Out of stock
KX1-004 is a non-ATP competitive inhibitor of Src protein tyrosine kinase (Src-PTK; IC50 = 40 µM).{41235} It protects against a permanent threshold shift in the auditory threshold and against outer hair cell loss in chinchillas following noise exposure at 106 dB when used at 30, 50, or 100 µM on the round window membrane of the ear. KX1-004 (50 mg/kg) is also effective against chronic noise exposure when administered systemically in chinchillas.{41234}
Brand:CaymanSKU:22198 -Out of stock
KX1-004 is a non-ATP competitive inhibitor of Src protein tyrosine kinase (Src-PTK; IC50 = 40 µM).{41235} It protects against a permanent threshold shift in the auditory threshold and against outer hair cell loss in chinchillas following noise exposure at 106 dB when used at 30, 50, or 100 µM on the round window membrane of the ear. KX1-004 (50 mg/kg) is also effective against chronic noise exposure when administered systemically in chinchillas.{41234}
Brand:CaymanSKU:22198 -Out of stock
KX1-004 is a non-ATP competitive inhibitor of Src protein tyrosine kinase (Src-PTK; IC50 = 40 µM).{41235} It protects against a permanent threshold shift in the auditory threshold and against outer hair cell loss in chinchillas following noise exposure at 106 dB when used at 30, 50, or 100 µM on the round window membrane of the ear. KX1-004 (50 mg/kg) is also effective against chronic noise exposure when administered systemically in chinchillas.{41234}
Brand:CaymanSKU:22198 -Out of stock
KX2-391 is a highly selective and potent Src kinase inhibitor with strong anticancer properties that binds specifically to the substrate binding site of Src kinase (IC50 = 20 nM for Src kinase autophosphorylation; IC50 = 100 nM and 25 nM in human tumor cells in the presence and absence of human plasma, respectively; GI50 = 9, 13, 26, and 60 nM in HuH7, PLC/PRF/5, Hep 3B, and Hep G2 hepatocellular carcinoma cell lines, respectively).{33784,33783,33781} It does not affect PDGFR, EGFR, JAK1, JAK2, Lck, or ZAP-70.{33780,33782} In ERα positive breast cancer cells, KX2-391 induced apoptosis through activation of caspases 6, 7, 8, and 9.{33780} It can also induce p53 expression and stimulate caspase-3 and PARP cleavage in vitro.{33784} KX2-391 has been through Phase I and Phase II clinical trials for patients with acute myeloid leukemia, solid tumors, prostate cancers, and lymphoma.{33784,33781} A Phase II clinical trial is ongoing for a formulation of KX2-391 in ointment form for patients with actinic keratosis, a disorder of the skin that can lead to squamous cell carcinoma.
Brand:CaymanSKU:21429 -Out of stock
KX2-391 is a highly selective and potent Src kinase inhibitor with strong anticancer properties that binds specifically to the substrate binding site of Src kinase (IC50 = 20 nM for Src kinase autophosphorylation; IC50 = 100 nM and 25 nM in human tumor cells in the presence and absence of human plasma, respectively; GI50 = 9, 13, 26, and 60 nM in HuH7, PLC/PRF/5, Hep 3B, and Hep G2 hepatocellular carcinoma cell lines, respectively).{33784,33783,33781} It does not affect PDGFR, EGFR, JAK1, JAK2, Lck, or ZAP-70.{33780,33782} In ERα positive breast cancer cells, KX2-391 induced apoptosis through activation of caspases 6, 7, 8, and 9.{33780} It can also induce p53 expression and stimulate caspase-3 and PARP cleavage in vitro.{33784} KX2-391 has been through Phase I and Phase II clinical trials for patients with acute myeloid leukemia, solid tumors, prostate cancers, and lymphoma.{33784,33781} A Phase II clinical trial is ongoing for a formulation of KX2-391 in ointment form for patients with actinic keratosis, a disorder of the skin that can lead to squamous cell carcinoma.
Brand:CaymanSKU:21429 -Out of stock