Chemicals
Showing 27301–27450 of 41137 results
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ML-346 is an activator of the heat shock response that induces the expression of the heat shock proteins HSP70, HSP40, and HSP27.{38557} It induces the expression of the oxidative stress response genes HO1, GCLM, and BiP in mouse embryonic fibroblasts (MEFs) and pretreatment protects cells from severe heat shock-induced death and H2O2-induced apoptosis. It promotes folding of metastable proteins in models of conformational disease, including cellular models of Huntingtin aggregation and cystic fibrosis. It reduces aggregate formation in PC12 cells expressing human Huntingtin exon 1 containing a 74 glutamine expansion when used at a concentration of 10 µM. It also corrects trafficking of cystic fibrosis transmembrane conductance regulator proteins bearing the F508 deletion (ΔF508-CFTR) mutation carried by the majority of cystic fibrosis patients, leading to increased cell surface expression.
Brand:CaymanSKU:23844 - 10 mgAvailable on backorder
ML-346 is an activator of the heat shock response that induces the expression of the heat shock proteins HSP70, HSP40, and HSP27.{38557} It induces the expression of the oxidative stress response genes HO1, GCLM, and BiP in mouse embryonic fibroblasts (MEFs) and pretreatment protects cells from severe heat shock-induced death and H2O2-induced apoptosis. It promotes folding of metastable proteins in models of conformational disease, including cellular models of Huntingtin aggregation and cystic fibrosis. It reduces aggregate formation in PC12 cells expressing human Huntingtin exon 1 containing a 74 glutamine expansion when used at a concentration of 10 µM. It also corrects trafficking of cystic fibrosis transmembrane conductance regulator proteins bearing the F508 deletion (ΔF508-CFTR) mutation carried by the majority of cystic fibrosis patients, leading to increased cell surface expression.
Brand:CaymanSKU:23844 - 25 mgAvailable on backorder
ML-346 is an activator of the heat shock response that induces the expression of the heat shock proteins HSP70, HSP40, and HSP27.{38557} It induces the expression of the oxidative stress response genes HO1, GCLM, and BiP in mouse embryonic fibroblasts (MEFs) and pretreatment protects cells from severe heat shock-induced death and H2O2-induced apoptosis. It promotes folding of metastable proteins in models of conformational disease, including cellular models of Huntingtin aggregation and cystic fibrosis. It reduces aggregate formation in PC12 cells expressing human Huntingtin exon 1 containing a 74 glutamine expansion when used at a concentration of 10 µM. It also corrects trafficking of cystic fibrosis transmembrane conductance regulator proteins bearing the F508 deletion (ΔF508-CFTR) mutation carried by the majority of cystic fibrosis patients, leading to increased cell surface expression.
Brand:CaymanSKU:23844 - 5 mgAvailable on backorder
Activation of bone morphogenetic protein (BMP) type I receptors, also known as activin receptor-like kinases (ALK1-7), leads to the assembly of SMAD complexes, which translocate to the nucleus to induce transcriptional activation important for normal development and tissue repair.{9612} ML-347 is a 5-quinoline compound that inhibits ALK1 and ALK2 with IC50 values of 46 and 32 nM, respectively.{28723} It demonstrates >300-fold selectivity for ALK2 over ALK3, ALK6, and VEGF type 2 receptor (IC50s = 10.8, 9.8, and 19.7 µM, respectively) and is inactive at ALK4, ALK5, BMP type 2 receptors, TGF-β type 2 receptor, and AMPK.{28723} In a functional assay, ML-347 was shown to inhibit BMP4 signaling with an IC50 value of 152 nM.{28723}
Brand:CaymanSKU:-Available on backorder
Activation of bone morphogenetic protein (BMP) type I receptors, also known as activin receptor-like kinases (ALK1-7), leads to the assembly of SMAD complexes, which translocate to the nucleus to induce transcriptional activation important for normal development and tissue repair.{9612} ML-347 is a 5-quinoline compound that inhibits ALK1 and ALK2 with IC50 values of 46 and 32 nM, respectively.{28723} It demonstrates >300-fold selectivity for ALK2 over ALK3, ALK6, and VEGF type 2 receptor (IC50s = 10.8, 9.8, and 19.7 µM, respectively) and is inactive at ALK4, ALK5, BMP type 2 receptors, TGF-β type 2 receptor, and AMPK.{28723} In a functional assay, ML-347 was shown to inhibit BMP4 signaling with an IC50 value of 152 nM.{28723}
Brand:CaymanSKU:-Available on backorder
Activation of bone morphogenetic protein (BMP) type I receptors, also known as activin receptor-like kinases (ALK1-7), leads to the assembly of SMAD complexes, which translocate to the nucleus to induce transcriptional activation important for normal development and tissue repair.{9612} ML-347 is a 5-quinoline compound that inhibits ALK1 and ALK2 with IC50 values of 46 and 32 nM, respectively.{28723} It demonstrates >300-fold selectivity for ALK2 over ALK3, ALK6, and VEGF type 2 receptor (IC50s = 10.8, 9.8, and 19.7 µM, respectively) and is inactive at ALK4, ALK5, BMP type 2 receptors, TGF-β type 2 receptor, and AMPK.{28723} In a functional assay, ML-347 was shown to inhibit BMP4 signaling with an IC50 value of 152 nM.{28723}
Brand:CaymanSKU:-Available on backorder
Activation of bone morphogenetic protein (BMP) type I receptors, also known as activin receptor-like kinases (ALK1-7), leads to the assembly of SMAD complexes, which translocate to the nucleus to induce transcriptional activation important for normal development and tissue repair.{9612} ML-347 is a 5-quinoline compound that inhibits ALK1 and ALK2 with IC50 values of 46 and 32 nM, respectively.{28723} It demonstrates >300-fold selectivity for ALK2 over ALK3, ALK6, and VEGF type 2 receptor (IC50s = 10.8, 9.8, and 19.7 µM, respectively) and is inactive at ALK4, ALK5, BMP type 2 receptors, TGF-β type 2 receptor, and AMPK.{28723} In a functional assay, ML-347 was shown to inhibit BMP4 signaling with an IC50 value of 152 nM.{28723}
Brand:CaymanSKU:-Available on backorder
Lysophospholipase 1 (LYPLA1) is a protein palmitoyl thioesterase responsible for depalmitoylation of the oncogene HRas.{17771,28661} Palmitoylation of such oncogenes is thought to be required for trafficking and malignant transformation, making LYPLA1 a target for downregulating oncogenic signaling.{17771,28661} ML-348 is a reversible LYPLA1 inhibitor with an IC50 value of 210 nM.{29760} It is 14-fold selective for LYPLA1 over LYPLA2 (IC50 = >3,000) and demonstrates little activity against a panel of more than 20 other serine hydrolases (IC50s = >10,000).{29760}
Brand:CaymanSKU:-Available on backorder
Lysophospholipase 1 (LYPLA1) is a protein palmitoyl thioesterase responsible for depalmitoylation of the oncogene HRas.{17771,28661} Palmitoylation of such oncogenes is thought to be required for trafficking and malignant transformation, making LYPLA1 a target for downregulating oncogenic signaling.{17771,28661} ML-348 is a reversible LYPLA1 inhibitor with an IC50 value of 210 nM.{29760} It is 14-fold selective for LYPLA1 over LYPLA2 (IC50 = >3,000) and demonstrates little activity against a panel of more than 20 other serine hydrolases (IC50s = >10,000).{29760}
Brand:CaymanSKU:-Available on backorder
Lysophospholipase 1 (LYPLA1) is a protein palmitoyl thioesterase responsible for depalmitoylation of the oncogene HRas.{17771,28661} Palmitoylation of such oncogenes is thought to be required for trafficking and malignant transformation, making LYPLA1 a target for downregulating oncogenic signaling.{17771,28661} ML-348 is a reversible LYPLA1 inhibitor with an IC50 value of 210 nM.{29760} It is 14-fold selective for LYPLA1 over LYPLA2 (IC50 = >3,000) and demonstrates little activity against a panel of more than 20 other serine hydrolases (IC50s = >10,000).{29760}
Brand:CaymanSKU:-Available on backorder
Lysophospholipase 1 (LYPLA1) is a protein palmitoyl thioesterase responsible for depalmitoylation of the oncogene HRas.{17771,28661} Palmitoylation of such oncogenes is thought to be required for trafficking and malignant transformation, making LYPLA1 a target for downregulating oncogenic signaling.{17771,28661} ML-348 is a reversible LYPLA1 inhibitor with an IC50 value of 210 nM.{29760} It is 14-fold selective for LYPLA1 over LYPLA2 (IC50 = >3,000) and demonstrates little activity against a panel of more than 20 other serine hydrolases (IC50s = >10,000).{29760}
Brand:CaymanSKU:-Available on backorder
ML-349 is a selective and reversible inhibitor of lysophospholipase 2 (LYPLA2; Kis = 230 and >10,000 nM for human recombinant LYPLA2 and LYPLA1, respectively).{41062} Treatment with ML-349 results in >95% inhibition of LYPLA2 with no change in the activity of 25 other serine hydrolases in BW5147 murine T cell hybridoma cells. ML-349 almost completely inhibits LYPLA2 in HEK293T and mouse T cells and in vivo in murine lung, heart, and kidneys. It partially inhibits LYPLA2 in murine brain.
Brand:CaymanSKU:20923 -Out of stock
ML-349 is a selective and reversible inhibitor of lysophospholipase 2 (LYPLA2; Kis = 230 and >10,000 nM for human recombinant LYPLA2 and LYPLA1, respectively).{41062} Treatment with ML-349 results in >95% inhibition of LYPLA2 with no change in the activity of 25 other serine hydrolases in BW5147 murine T cell hybridoma cells. ML-349 almost completely inhibits LYPLA2 in HEK293T and mouse T cells and in vivo in murine lung, heart, and kidneys. It partially inhibits LYPLA2 in murine brain.
Brand:CaymanSKU:20923 -Out of stock
ML-349 is a selective and reversible inhibitor of lysophospholipase 2 (LYPLA2; Kis = 230 and >10,000 nM for human recombinant LYPLA2 and LYPLA1, respectively).{41062} Treatment with ML-349 results in >95% inhibition of LYPLA2 with no change in the activity of 25 other serine hydrolases in BW5147 murine T cell hybridoma cells. ML-349 almost completely inhibits LYPLA2 in HEK293T and mouse T cells and in vivo in murine lung, heart, and kidneys. It partially inhibits LYPLA2 in murine brain.
Brand:CaymanSKU:20923 -Out of stock
ML-352 is a noncompetitive inhibitor of the presynaptic choline transporter (CHT) with Ki values of 92 and 166 nM for HEK293 cells expressing human CHT and mouse forebrain synaptosomes, respectively.{42276} It is selective for CHT over dopamine, norepinephrine, and serotonin transporters in HEK293 cells expressing human transporters when used at a concentration of 5 μM as well as a panel of 68 G protein-coupled receptors, ion channels, and transporters when used at a concentration of 10 μM. ML-352 (5 μM) increases cell surface expression of CHT without affecting total protein levels.
Brand:CaymanSKU:21878 -Out of stock
ML-352 is a noncompetitive inhibitor of the presynaptic choline transporter (CHT) with Ki values of 92 and 166 nM for HEK293 cells expressing human CHT and mouse forebrain synaptosomes, respectively.{42276} It is selective for CHT over dopamine, norepinephrine, and serotonin transporters in HEK293 cells expressing human transporters when used at a concentration of 5 μM as well as a panel of 68 G protein-coupled receptors, ion channels, and transporters when used at a concentration of 10 μM. ML-352 (5 μM) increases cell surface expression of CHT without affecting total protein levels.
Brand:CaymanSKU:21878 -Out of stock
ML-352 is a noncompetitive inhibitor of the presynaptic choline transporter (CHT) with Ki values of 92 and 166 nM for HEK293 cells expressing human CHT and mouse forebrain synaptosomes, respectively.{42276} It is selective for CHT over dopamine, norepinephrine, and serotonin transporters in HEK293 cells expressing human transporters when used at a concentration of 5 μM as well as a panel of 68 G protein-coupled receptors, ion channels, and transporters when used at a concentration of 10 μM. ML-352 (5 μM) increases cell surface expression of CHT without affecting total protein levels.
Brand:CaymanSKU:21878 -Out of stock
ML-354 is an indole-based, proteinase-activated receptor 4 (PAR4) antagonist (IC50 = 140 nM) that exhibits 71-fold selectivity for PAR4 over PAR1 (IC50 = 10 μM) in isolated human platelets.{31126}
Brand:CaymanSKU:-Available on backorder
ML-354 is an indole-based, proteinase-activated receptor 4 (PAR4) antagonist (IC50 = 140 nM) that exhibits 71-fold selectivity for PAR4 over PAR1 (IC50 = 10 μM) in isolated human platelets.{31126}
Brand:CaymanSKU:-Available on backorder
ML-354 is an indole-based, proteinase-activated receptor 4 (PAR4) antagonist (IC50 = 140 nM) that exhibits 71-fold selectivity for PAR4 over PAR1 (IC50 = 10 μM) in isolated human platelets.{31126}
Brand:CaymanSKU:-Available on backorder
ML-354 is an indole-based, proteinase-activated receptor 4 (PAR4) antagonist (IC50 = 140 nM) that exhibits 71-fold selectivity for PAR4 over PAR1 (IC50 = 10 μM) in isolated human platelets.{31126}
Brand:CaymanSKU:-Available on backorder
ML-356 is an inhibitor of the thioesterase domain of fatty acid synthase (FASN-TE; IC50 = 334 nM).{32731} It is selective for FASN over a number of other human thioesterases expressed in tumor cells, and selective for FASN-TE over its most closely related human homolog, ACOT4.{32731} In cells, ML-356 has been shown to block the biosynthesis of palmitate, the end product of FASN.{32731}
Brand:CaymanSKU:20940 -Out of stock
ML-356 is an inhibitor of the thioesterase domain of fatty acid synthase (FASN-TE; IC50 = 334 nM).{32731} It is selective for FASN over a number of other human thioesterases expressed in tumor cells, and selective for FASN-TE over its most closely related human homolog, ACOT4.{32731} In cells, ML-356 has been shown to block the biosynthesis of palmitate, the end product of FASN.{32731}
Brand:CaymanSKU:20940 -Out of stock
ML-356 is an inhibitor of the thioesterase domain of fatty acid synthase (FASN-TE; IC50 = 334 nM).{32731} It is selective for FASN over a number of other human thioesterases expressed in tumor cells, and selective for FASN-TE over its most closely related human homolog, ACOT4.{32731} In cells, ML-356 has been shown to block the biosynthesis of palmitate, the end product of FASN.{32731}
Brand:CaymanSKU:20940 -Out of stock
ML-364 is a reversible inhibitor of ubiquitin-specific protease 2 (USP2), a deubiquitinase, that has an IC50 value of 1.1 µM in a fluorescence-based assay using di-ubiquitin substrates.{39305} It inhibits USP8, which is closely related to USP2, with an IC50 value of 0.95 µM in the same assay. It has no activity at the proteases caspase-6, caspase-7, MMP-1, MMP-9, and USP15 or at 102 kinases in a panel including cell cycle regulators. ML-364 increases cyclin D1 degradation (IC50 = 0.97 µM) in HCT116 colorectal carcinoma cells. It induces arrest of the cell cycle at the G1 phase in Mino mantle cell lymphoma and HCT116 cells and inhibits proliferation of HCT116 cells (IC50 = 3.6 µM). It also decreases homologous recombination-mediated DNA repair in DR-GFP U2OS cells.
Brand:CaymanSKU:21774 -Out of stock
ML-364 is a reversible inhibitor of ubiquitin-specific protease 2 (USP2), a deubiquitinase, that has an IC50 value of 1.1 µM in a fluorescence-based assay using di-ubiquitin substrates.{39305} It inhibits USP8, which is closely related to USP2, with an IC50 value of 0.95 µM in the same assay. It has no activity at the proteases caspase-6, caspase-7, MMP-1, MMP-9, and USP15 or at 102 kinases in a panel including cell cycle regulators. ML-364 increases cyclin D1 degradation (IC50 = 0.97 µM) in HCT116 colorectal carcinoma cells. It induces arrest of the cell cycle at the G1 phase in Mino mantle cell lymphoma and HCT116 cells and inhibits proliferation of HCT116 cells (IC50 = 3.6 µM). It also decreases homologous recombination-mediated DNA repair in DR-GFP U2OS cells.
Brand:CaymanSKU:21774 -Out of stock
ML-364 is a reversible inhibitor of ubiquitin-specific protease 2 (USP2), a deubiquitinase, that has an IC50 value of 1.1 µM in a fluorescence-based assay using di-ubiquitin substrates.{39305} It inhibits USP8, which is closely related to USP2, with an IC50 value of 0.95 µM in the same assay. It has no activity at the proteases caspase-6, caspase-7, MMP-1, MMP-9, and USP15 or at 102 kinases in a panel including cell cycle regulators. ML-364 increases cyclin D1 degradation (IC50 = 0.97 µM) in HCT116 colorectal carcinoma cells. It induces arrest of the cell cycle at the G1 phase in Mino mantle cell lymphoma and HCT116 cells and inhibits proliferation of HCT116 cells (IC50 = 3.6 µM). It also decreases homologous recombination-mediated DNA repair in DR-GFP U2OS cells.
Brand:CaymanSKU:21774 -Out of stock
ML-364 is a reversible inhibitor of ubiquitin-specific protease 2 (USP2), a deubiquitinase, that has an IC50 value of 1.1 µM in a fluorescence-based assay using di-ubiquitin substrates.{39305} It inhibits USP8, which is closely related to USP2, with an IC50 value of 0.95 µM in the same assay. It has no activity at the proteases caspase-6, caspase-7, MMP-1, MMP-9, and USP15 or at 102 kinases in a panel including cell cycle regulators. ML-364 increases cyclin D1 degradation (IC50 = 0.97 µM) in HCT116 colorectal carcinoma cells. It induces arrest of the cell cycle at the G1 phase in Mino mantle cell lymphoma and HCT116 cells and inhibits proliferation of HCT116 cells (IC50 = 3.6 µM). It also decreases homologous recombination-mediated DNA repair in DR-GFP U2OS cells.
Brand:CaymanSKU:21774 -Out of stock
ML-365 is a bis-amide TASK-1 potassium channel blocker (IC50 = 16 nM).{42066} It is selective for TASK-1 over TASK-3 channels in a QPatch assay (IC50 = 990 nM). It also acts as an antagonist of the metabotropic glutamate receptor mGluR5 (IC50 = 1.35 μM).{42067}
Brand:CaymanSKU:24666 - 1 mgAvailable on backorder
ML-365 is a bis-amide TASK-1 potassium channel blocker (IC50 = 16 nM).{42066} It is selective for TASK-1 over TASK-3 channels in a QPatch assay (IC50 = 990 nM). It also acts as an antagonist of the metabotropic glutamate receptor mGluR5 (IC50 = 1.35 μM).{42067}
Brand:CaymanSKU:24666 - 10 mgAvailable on backorder
ML-365 is a bis-amide TASK-1 potassium channel blocker (IC50 = 16 nM).{42066} It is selective for TASK-1 over TASK-3 channels in a QPatch assay (IC50 = 990 nM). It also acts as an antagonist of the metabotropic glutamate receptor mGluR5 (IC50 = 1.35 μM).{42067}
Brand:CaymanSKU:24666 - 25 mgAvailable on backorder
ML-365 is a bis-amide TASK-1 potassium channel blocker (IC50 = 16 nM).{42066} It is selective for TASK-1 over TASK-3 channels in a QPatch assay (IC50 = 990 nM). It also acts as an antagonist of the metabotropic glutamate receptor mGluR5 (IC50 = 1.35 μM).{42067}
Brand:CaymanSKU:24666 - 5 mgAvailable on backorder
ML-385 is an inhibitor of nuclear factor erythroid 2-related factor 2 (Nrf2; IC50 = 1.9 µM) that blocks downstream target gene expression.{32646} It substantially enhances cytotoxicity in non-small cell lung cancer (NSCLC) cells treated with platinum-based drugs.{32646} ML-385 shows specificity and selectivity for NSCLC cells with KEAP1 mutation, which leads to gain of Nrf2 function.{32646}
Brand:CaymanSKU:21114 -Out of stock
ML-385 is an inhibitor of nuclear factor erythroid 2-related factor 2 (Nrf2; IC50 = 1.9 µM) that blocks downstream target gene expression.{32646} It substantially enhances cytotoxicity in non-small cell lung cancer (NSCLC) cells treated with platinum-based drugs.{32646} ML-385 shows specificity and selectivity for NSCLC cells with KEAP1 mutation, which leads to gain of Nrf2 function.{32646}
Brand:CaymanSKU:21114 -Out of stock
ML-385 is an inhibitor of nuclear factor erythroid 2-related factor 2 (Nrf2; IC50 = 1.9 µM) that blocks downstream target gene expression.{32646} It substantially enhances cytotoxicity in non-small cell lung cancer (NSCLC) cells treated with platinum-based drugs.{32646} ML-385 shows specificity and selectivity for NSCLC cells with KEAP1 mutation, which leads to gain of Nrf2 function.{32646}
Brand:CaymanSKU:21114 -Out of stock
ML-390 is an inhibitor of dihydroorotate dehydrogenase (DHODH), the enzyme that converts dihydroorotate to orotate during de novo pyrimidine synthesis.{39048} In acute myeloid leukemia, leukemic myeloblast development is halted at an immature stage leading to perpetual self-renewal rather than differentiation. ML-390 induces differentiation in the acute myeloid leukemia cell lines U937 (murine) and THP-1 (human) cell lines with an EC50 value of approximately 2 µM.
Brand:CaymanSKU:21395 -Out of stock
ML-390 is an inhibitor of dihydroorotate dehydrogenase (DHODH), the enzyme that converts dihydroorotate to orotate during de novo pyrimidine synthesis.{39048} In acute myeloid leukemia, leukemic myeloblast development is halted at an immature stage leading to perpetual self-renewal rather than differentiation. ML-390 induces differentiation in the acute myeloid leukemia cell lines U937 (murine) and THP-1 (human) cell lines with an EC50 value of approximately 2 µM.
Brand:CaymanSKU:21395 -Out of stock
ML-390 is an inhibitor of dihydroorotate dehydrogenase (DHODH), the enzyme that converts dihydroorotate to orotate during de novo pyrimidine synthesis.{39048} In acute myeloid leukemia, leukemic myeloblast development is halted at an immature stage leading to perpetual self-renewal rather than differentiation. ML-390 induces differentiation in the acute myeloid leukemia cell lines U937 (murine) and THP-1 (human) cell lines with an EC50 value of approximately 2 µM.
Brand:CaymanSKU:21395 -Out of stock
ML-390 is an inhibitor of dihydroorotate dehydrogenase (DHODH), the enzyme that converts dihydroorotate to orotate during de novo pyrimidine synthesis.{39048} In acute myeloid leukemia, leukemic myeloblast development is halted at an immature stage leading to perpetual self-renewal rather than differentiation. ML-390 induces differentiation in the acute myeloid leukemia cell lines U937 (murine) and THP-1 (human) cell lines with an EC50 value of approximately 2 µM.
Brand:CaymanSKU:21395 -Out of stock
ML-396 is a positive allosteric modulator of group III metabotropic glutamate receptors (mGluRs) with EC50 values of 108, 146, and 128 nM for mGluR4, mGluR7, and mGluR8, respectively, in calcium mobilization assays.{46721} ML-396 potentiates LSP4-2022-induced reductions in paired-pulse field excitatory post synaptic potential (fEPSP) slopes in mouse hippocampal slices. In vivo, ML-396 (30 mg/kg) restores hippocampal long-term potentiation, improves novel object recognition, contextual fear learning, and social memory, and decreases sleep apneas in the Mecp2-/- mouse model of Rett syndrome.{46722}
Brand:CaymanSKU:29167 - 1 mgAvailable on backorder
ML-396 is a positive allosteric modulator of group III metabotropic glutamate receptors (mGluRs) with EC50 values of 108, 146, and 128 nM for mGluR4, mGluR7, and mGluR8, respectively, in calcium mobilization assays.{46721} ML-396 potentiates LSP4-2022-induced reductions in paired-pulse field excitatory post synaptic potential (fEPSP) slopes in mouse hippocampal slices. In vivo, ML-396 (30 mg/kg) restores hippocampal long-term potentiation, improves novel object recognition, contextual fear learning, and social memory, and decreases sleep apneas in the Mecp2-/- mouse model of Rett syndrome.{46722}
Brand:CaymanSKU:29167 - 10 mgAvailable on backorder
ML-396 is a positive allosteric modulator of group III metabotropic glutamate receptors (mGluRs) with EC50 values of 108, 146, and 128 nM for mGluR4, mGluR7, and mGluR8, respectively, in calcium mobilization assays.{46721} ML-396 potentiates LSP4-2022-induced reductions in paired-pulse field excitatory post synaptic potential (fEPSP) slopes in mouse hippocampal slices. In vivo, ML-396 (30 mg/kg) restores hippocampal long-term potentiation, improves novel object recognition, contextual fear learning, and social memory, and decreases sleep apneas in the Mecp2-/- mouse model of Rett syndrome.{46722}
Brand:CaymanSKU:29167 - 25 mgAvailable on backorder
ML-396 is a positive allosteric modulator of group III metabotropic glutamate receptors (mGluRs) with EC50 values of 108, 146, and 128 nM for mGluR4, mGluR7, and mGluR8, respectively, in calcium mobilization assays.{46721} ML-396 potentiates LSP4-2022-induced reductions in paired-pulse field excitatory post synaptic potential (fEPSP) slopes in mouse hippocampal slices. In vivo, ML-396 (30 mg/kg) restores hippocampal long-term potentiation, improves novel object recognition, contextual fear learning, and social memory, and decreases sleep apneas in the Mecp2-/- mouse model of Rett syndrome.{46722}
Brand:CaymanSKU:29167 - 5 mgAvailable on backorder
ML-7 inhibits smooth muscle myosin light chain kinase (MLCK) with a Ki value of 0.3 µM and displays reversible, ATP-competitive inhibition of Ca2+-calmodulin-dependent and -independent smooth muscle MLCKs.{22134,14995} It exhibits a 10-fold more potent inhibition of MLCK than its parent compound ML-9 (Item No. 10010236).{22134,14995}
Brand:CaymanSKU:11801 - 1 mgAvailable on backorder
ML-7 inhibits smooth muscle myosin light chain kinase (MLCK) with a Ki value of 0.3 µM and displays reversible, ATP-competitive inhibition of Ca2+-calmodulin-dependent and -independent smooth muscle MLCKs.{22134,14995} It exhibits a 10-fold more potent inhibition of MLCK than its parent compound ML-9 (Item No. 10010236).{22134,14995}
Brand:CaymanSKU:11801 - 10 mgAvailable on backorder
ML-7 inhibits smooth muscle myosin light chain kinase (MLCK) with a Ki value of 0.3 µM and displays reversible, ATP-competitive inhibition of Ca2+-calmodulin-dependent and -independent smooth muscle MLCKs.{22134,14995} It exhibits a 10-fold more potent inhibition of MLCK than its parent compound ML-9 (Item No. 10010236).{22134,14995}
Brand:CaymanSKU:11801 - 5 mgAvailable on backorder
ML-7 inhibits smooth muscle myosin light chain kinase (MLCK) with a Ki value of 0.3 µM and displays reversible, ATP-competitive inhibition of Ca2+-calmodulin-dependent and -independent smooth muscle MLCKs.{22134,14995} It exhibits a 10-fold more potent inhibition of MLCK than its parent compound ML-9 (Item No. 10010236).{22134,14995}
Brand:CaymanSKU:11801 - 50 mgAvailable on backorder
ML-9 was originally identified as a selective Ca2+-calmodulin-dependent myosin light chain kinase inhibitor. Concentrations from 10-100 µM are effective at inhibiting vascular smooth muscle tension and reducing intracellular Ca2+ concentrations.{15194} ML-9 also inhibits PKB/Akt activity with an IC50 range of 10-50 µM in rat primary adipocytes. This results in a specific inhibition of insulin-stimulated glucose transport and GLUT4/IGF II receptor translocation to the plasma membrane yet does not interfere with the antilipolytic effect of insulin.{15239} Additionally, ML-9 inhibits other serine/threonine kinases including PKA (IC50 = ~20 µM), p90 S6 (IC50 = ~50 µM), and MAP kinase (IC50 = ~35 µM).{15239}
Brand:CaymanSKU:10010236 - 10 mgAvailable on backorder
ML-9 was originally identified as a selective Ca2+-calmodulin-dependent myosin light chain kinase inhibitor. Concentrations from 10-100 µM are effective at inhibiting vascular smooth muscle tension and reducing intracellular Ca2+ concentrations.{15194} ML-9 also inhibits PKB/Akt activity with an IC50 range of 10-50 µM in rat primary adipocytes. This results in a specific inhibition of insulin-stimulated glucose transport and GLUT4/IGF II receptor translocation to the plasma membrane yet does not interfere with the antilipolytic effect of insulin.{15239} Additionally, ML-9 inhibits other serine/threonine kinases including PKA (IC50 = ~20 µM), p90 S6 (IC50 = ~50 µM), and MAP kinase (IC50 = ~35 µM).{15239}
Brand:CaymanSKU:- ML-9 was originally identified as a selective Ca2+-calmodulin-dependent myosin light chain kinase inhibitor. Concentrations from 10-100 µM are effective at inhibiting vascular smooth muscle tension and reducing intracellular Ca2+ concentrations.{15194} ML-9 also inhibits PKB/Akt activity with an IC50 range of 10-50 µM in rat primary adipocytes. This results in a specific inhibition of insulin-stimulated glucose transport and GLUT4/IGF II receptor translocation to the plasma membrane yet does not interfere with the antilipolytic effect of insulin.{15239} Additionally, ML-9 inhibits other serine/threonine kinases including PKA (IC50 = ~20 µM), p90 S6 (IC50 = ~50 µM), and MAP kinase (IC50 = ~35 µM).{15239}
Brand:CaymanSKU:10010236 - 100 mgAvailable on backorder
ML-9 was originally identified as a selective Ca2+-calmodulin-dependent myosin light chain kinase inhibitor. Concentrations from 10-100 µM are effective at inhibiting vascular smooth muscle tension and reducing intracellular Ca2+ concentrations.{15194} ML-9 also inhibits PKB/Akt activity with an IC50 range of 10-50 µM in rat primary adipocytes. This results in a specific inhibition of insulin-stimulated glucose transport and GLUT4/IGF II receptor translocation to the plasma membrane yet does not interfere with the antilipolytic effect of insulin.{15239} Additionally, ML-9 inhibits other serine/threonine kinases including PKA (IC50 = ~20 µM), p90 S6 (IC50 = ~50 µM), and MAP kinase (IC50 = ~35 µM).{15239}
Brand:CaymanSKU:- ML-9 was originally identified as a selective Ca2+-calmodulin-dependent myosin light chain kinase inhibitor. Concentrations from 10-100 µM are effective at inhibiting vascular smooth muscle tension and reducing intracellular Ca2+ concentrations.{15194} ML-9 also inhibits PKB/Akt activity with an IC50 range of 10-50 µM in rat primary adipocytes. This results in a specific inhibition of insulin-stimulated glucose transport and GLUT4/IGF II receptor translocation to the plasma membrane yet does not interfere with the antilipolytic effect of insulin.{15239} Additionally, ML-9 inhibits other serine/threonine kinases including PKA (IC50 = ~20 µM), p90 S6 (IC50 = ~50 µM), and MAP kinase (IC50 = ~35 µM).{15239}
Brand:CaymanSKU:10010236 - 250 mgAvailable on backorder
ML-9 was originally identified as a selective Ca2+-calmodulin-dependent myosin light chain kinase inhibitor. Concentrations from 10-100 µM are effective at inhibiting vascular smooth muscle tension and reducing intracellular Ca2+ concentrations.{15194} ML-9 also inhibits PKB/Akt activity with an IC50 range of 10-50 µM in rat primary adipocytes. This results in a specific inhibition of insulin-stimulated glucose transport and GLUT4/IGF II receptor translocation to the plasma membrane yet does not interfere with the antilipolytic effect of insulin.{15239} Additionally, ML-9 inhibits other serine/threonine kinases including PKA (IC50 = ~20 µM), p90 S6 (IC50 = ~50 µM), and MAP kinase (IC50 = ~35 µM).{15239}
Brand:CaymanSKU:- ML-9 was originally identified as a selective Ca2+-calmodulin-dependent myosin light chain kinase inhibitor. Concentrations from 10-100 µM are effective at inhibiting vascular smooth muscle tension and reducing intracellular Ca2+ concentrations.{15194} ML-9 also inhibits PKB/Akt activity with an IC50 range of 10-50 µM in rat primary adipocytes. This results in a specific inhibition of insulin-stimulated glucose transport and GLUT4/IGF II receptor translocation to the plasma membrane yet does not interfere with the antilipolytic effect of insulin.{15239} Additionally, ML-9 inhibits other serine/threonine kinases including PKA (IC50 = ~20 µM), p90 S6 (IC50 = ~50 µM), and MAP kinase (IC50 = ~35 µM).{15239}
Brand:CaymanSKU:10010236 - 50 mgAvailable on backorder
ML-SA1 is an agonist of transient receptor potential mucolipin 1 (TRPML1).{46901} It induces cytosolic calcium increases in HEK293T cells expressing surface-expressed mutant TRPML1 channels when used at a concentration of 10 µM. ML-SA1 activates TRPML1-mediated current (IML1) in isolated vacuoles that were enlarged by vacuolin-1 (Item No. 20425) prior to isolation from HEK293 cells expressing TRPML1. It also activates whole-endolysosome IML1 in primary murine macrophages.
Brand:CaymanSKU:29958 - 10 mgAvailable on backorder
ML-SA1 is an agonist of transient receptor potential mucolipin 1 (TRPML1).{46901} It induces cytosolic calcium increases in HEK293T cells expressing surface-expressed mutant TRPML1 channels when used at a concentration of 10 µM. ML-SA1 activates TRPML1-mediated current (IML1) in isolated vacuoles that were enlarged by vacuolin-1 (Item No. 20425) prior to isolation from HEK293 cells expressing TRPML1. It also activates whole-endolysosome IML1 in primary murine macrophages.
Brand:CaymanSKU:29958 - 100 mgAvailable on backorder
ML-SA1 is an agonist of transient receptor potential mucolipin 1 (TRPML1).{46901} It induces cytosolic calcium increases in HEK293T cells expressing surface-expressed mutant TRPML1 channels when used at a concentration of 10 µM. ML-SA1 activates TRPML1-mediated current (IML1) in isolated vacuoles that were enlarged by vacuolin-1 (Item No. 20425) prior to isolation from HEK293 cells expressing TRPML1. It also activates whole-endolysosome IML1 in primary murine macrophages.
Brand:CaymanSKU:29958 - 250 mgAvailable on backorder
ML-SA1 is an agonist of transient receptor potential mucolipin 1 (TRPML1).{46901} It induces cytosolic calcium increases in HEK293T cells expressing surface-expressed mutant TRPML1 channels when used at a concentration of 10 µM. ML-SA1 activates TRPML1-mediated current (IML1) in isolated vacuoles that were enlarged by vacuolin-1 (Item No. 20425) prior to isolation from HEK293 cells expressing TRPML1. It also activates whole-endolysosome IML1 in primary murine macrophages.
Brand:CaymanSKU:29958 - 50 mgAvailable on backorder
Signal transducer and activator of transcription 3 (STAT3) is a cytokine-inducible transcription factor with roles in inflammation and cancer.{7286,11981} ML115 is an isoxazole carboxamide that acts as a cell-permeable STAT3 activator (EC50 = 2 nM) and is more than 28,000-fold selective for STAT3 over STAT1 and NF-κB.{29820} It shows no cytotoxicity against HT-1080 or NIH-3T3 cells. ML115 increases the expression of BCL3, a known STAT3-dependent oncogene, and enhances STAT3 activation by the pro-inflammatory cytokine IL-6.{29820} As the maintenance of pluripotency in mouse embryonic stem cells requires continued activation of STAT3, ML115 may be useful in maintaining embryonic stem cells in an undifferentiated state.{29820}
Brand:CaymanSKU:- Signal transducer and activator of transcription 3 (STAT3) is a cytokine-inducible transcription factor with roles in inflammation and cancer.{7286,11981} ML115 is an isoxazole carboxamide that acts as a cell-permeable STAT3 activator (EC50 = 2 nM) and is more than 28,000-fold selective for STAT3 over STAT1 and NF-κB.{29820} It shows no cytotoxicity against HT-1080 or NIH-3T3 cells. ML115 increases the expression of BCL3, a known STAT3-dependent oncogene, and enhances STAT3 activation by the pro-inflammatory cytokine IL-6.{29820} As the maintenance of pluripotency in mouse embryonic stem cells requires continued activation of STAT3, ML115 may be useful in maintaining embryonic stem cells in an undifferentiated state.{29820}
Brand:CaymanSKU:- Signal transducer and activator of transcription 3 (STAT3) is a cytokine-inducible transcription factor with roles in inflammation and cancer.{7286,11981} ML115 is an isoxazole carboxamide that acts as a cell-permeable STAT3 activator (EC50 = 2 nM) and is more than 28,000-fold selective for STAT3 over STAT1 and NF-κB.{29820} It shows no cytotoxicity against HT-1080 or NIH-3T3 cells. ML115 increases the expression of BCL3, a known STAT3-dependent oncogene, and enhances STAT3 activation by the pro-inflammatory cytokine IL-6.{29820} As the maintenance of pluripotency in mouse embryonic stem cells requires continued activation of STAT3, ML115 may be useful in maintaining embryonic stem cells in an undifferentiated state.{29820}
Brand:CaymanSKU:-
ML154 is an antagonist of the neuropeptide S receptor (NPSR; IC50 = 3.5 nM).{46808} It is selective for NPSR over arginine vasopressin (AVP) receptor V1B, as well as a panel of 55 receptors, channels, and transporters at 10 µM.{46809,46808} ML154 reduces NPS-induced calcium mobilization, cAMP formation, and ERK activation with IC50 values of 0.96, 45, and 1.3 nM, respectively, in CHO cells expressing NPSR.{46808} It reduces alcohol self-administration and the progressive ratio breakpoint, but not cue- or stress-induced reinstatement of alcohol-seeking behavior, in rats when administered intraperitoneally at a dose of 1 mg/kg.{46809} ML154 (10 µg, i.c.v.) inhibits decreases in food intake induced by intracerebroventricular administration of NPS in rats.{46808}
Brand:CaymanSKU:30200 - 1 mgAvailable on backorder
ML154 is an antagonist of the neuropeptide S receptor (NPSR; IC50 = 3.5 nM).{46808} It is selective for NPSR over arginine vasopressin (AVP) receptor V1B, as well as a panel of 55 receptors, channels, and transporters at 10 µM.{46809,46808} ML154 reduces NPS-induced calcium mobilization, cAMP formation, and ERK activation with IC50 values of 0.96, 45, and 1.3 nM, respectively, in CHO cells expressing NPSR.{46808} It reduces alcohol self-administration and the progressive ratio breakpoint, but not cue- or stress-induced reinstatement of alcohol-seeking behavior, in rats when administered intraperitoneally at a dose of 1 mg/kg.{46809} ML154 (10 µg, i.c.v.) inhibits decreases in food intake induced by intracerebroventricular administration of NPS in rats.{46808}
Brand:CaymanSKU:30200 - 10 mgAvailable on backorder
ML154 is an antagonist of the neuropeptide S receptor (NPSR; IC50 = 3.5 nM).{46808} It is selective for NPSR over arginine vasopressin (AVP) receptor V1B, as well as a panel of 55 receptors, channels, and transporters at 10 µM.{46809,46808} ML154 reduces NPS-induced calcium mobilization, cAMP formation, and ERK activation with IC50 values of 0.96, 45, and 1.3 nM, respectively, in CHO cells expressing NPSR.{46808} It reduces alcohol self-administration and the progressive ratio breakpoint, but not cue- or stress-induced reinstatement of alcohol-seeking behavior, in rats when administered intraperitoneally at a dose of 1 mg/kg.{46809} ML154 (10 µg, i.c.v.) inhibits decreases in food intake induced by intracerebroventricular administration of NPS in rats.{46808}
Brand:CaymanSKU:30200 - 5 mgAvailable on backorder
The Cdc2-like kinases (Clks) and the dual-specificity tyrosine phosphorylation-regulated kinases (DYRKs) are involved in regulating gene splicing. Clks phosphorylate serine/arginine-rich proteins, which are a major component of the spliceosome, whereas DYRKs interact with and activate splicing factors. ML167 is a selective, ATP-competitive inhibitor of Clk4 with an IC50 value of 136 nM.{29292} It is more than 10-fold less active against the closely related kinases Clk1-3, DYRK1A, and DYRK1B (IC50s = 1.5, 1.6, >10, >10, and 4.4 µM, respectively), and minimally active against a panel of other kinases.{29292}
Brand:CaymanSKU:-Available on backorder
The Cdc2-like kinases (Clks) and the dual-specificity tyrosine phosphorylation-regulated kinases (DYRKs) are involved in regulating gene splicing. Clks phosphorylate serine/arginine-rich proteins, which are a major component of the spliceosome, whereas DYRKs interact with and activate splicing factors. ML167 is a selective, ATP-competitive inhibitor of Clk4 with an IC50 value of 136 nM.{29292} It is more than 10-fold less active against the closely related kinases Clk1-3, DYRK1A, and DYRK1B (IC50s = 1.5, 1.6, >10, >10, and 4.4 µM, respectively), and minimally active against a panel of other kinases.{29292}
Brand:CaymanSKU:-Available on backorder
The Cdc2-like kinases (Clks) and the dual-specificity tyrosine phosphorylation-regulated kinases (DYRKs) are involved in regulating gene splicing. Clks phosphorylate serine/arginine-rich proteins, which are a major component of the spliceosome, whereas DYRKs interact with and activate splicing factors. ML167 is a selective, ATP-competitive inhibitor of Clk4 with an IC50 value of 136 nM.{29292} It is more than 10-fold less active against the closely related kinases Clk1-3, DYRK1A, and DYRK1B (IC50s = 1.5, 1.6, >10, >10, and 4.4 µM, respectively), and minimally active against a panel of other kinases.{29292}
Brand:CaymanSKU:-Available on backorder
ML314 is a neurotensin-1 receptor (NTS1) agonist.{43308,43309} It is selective for NTS1 over NTS2 in a cell-based assay of receptor/β-arrestin complex formation (EC50s = 2 and >80 μM, respectively) but is inactive in an NTS1 calcium flux assay (EC50 = >80 μM) indicating that, in contrast to other NTS1 agonists, it does not signal through the traditional Gq-coupled pathway.{43309} ML314 is also a positive allosteric modulator of NTS1 that increases binding of radiolabeled neurotensin (Item No. 24717) to NTS1 in a concentration-dependent manner.{43308} It reduces locomotion in dopamine transporter knockout mice and methamphetamine-exposed mice when administered at doses of 20 and 10 to 30 mg/kg, respectively.{43308} ML314 (30 mg/kg) also reduces methamphetamine self-administration in rats.
Brand:CaymanSKU:-Available on backorder
ML314 is a neurotensin-1 receptor (NTS1) agonist.{43308,43309} It is selective for NTS1 over NTS2 in a cell-based assay of receptor/β-arrestin complex formation (EC50s = 2 and >80 μM, respectively) but is inactive in an NTS1 calcium flux assay (EC50 = >80 μM) indicating that, in contrast to other NTS1 agonists, it does not signal through the traditional Gq-coupled pathway.{43309} ML314 is also a positive allosteric modulator of NTS1 that increases binding of radiolabeled neurotensin (Item No. 24717) to NTS1 in a concentration-dependent manner.{43308} It reduces locomotion in dopamine transporter knockout mice and methamphetamine-exposed mice when administered at doses of 20 and 10 to 30 mg/kg, respectively.{43308} ML314 (30 mg/kg) also reduces methamphetamine self-administration in rats.
Brand:CaymanSKU:-Available on backorder
ML314 is a neurotensin-1 receptor (NTS1) agonist.{43308,43309} It is selective for NTS1 over NTS2 in a cell-based assay of receptor/β-arrestin complex formation (EC50s = 2 and >80 μM, respectively) but is inactive in an NTS1 calcium flux assay (EC50 = >80 μM) indicating that, in contrast to other NTS1 agonists, it does not signal through the traditional Gq-coupled pathway.{43309} ML314 is also a positive allosteric modulator of NTS1 that increases binding of radiolabeled neurotensin (Item No. 24717) to NTS1 in a concentration-dependent manner.{43308} It reduces locomotion in dopamine transporter knockout mice and methamphetamine-exposed mice when administered at doses of 20 and 10 to 30 mg/kg, respectively.{43308} ML314 (30 mg/kg) also reduces methamphetamine self-administration in rats.
Brand:CaymanSKU:-Available on backorder
ML314 is a neurotensin-1 receptor (NTS1) agonist.{43308,43309} It is selective for NTS1 over NTS2 in a cell-based assay of receptor/β-arrestin complex formation (EC50s = 2 and >80 μM, respectively) but is inactive in an NTS1 calcium flux assay (EC50 = >80 μM) indicating that, in contrast to other NTS1 agonists, it does not signal through the traditional Gq-coupled pathway.{43309} ML314 is also a positive allosteric modulator of NTS1 that increases binding of radiolabeled neurotensin (Item No. 24717) to NTS1 in a concentration-dependent manner.{43308} It reduces locomotion in dopamine transporter knockout mice and methamphetamine-exposed mice when administered at doses of 20 and 10 to 30 mg/kg, respectively.{43308} ML314 (30 mg/kg) also reduces methamphetamine self-administration in rats.
Brand:CaymanSKU:-Available on backorder
ML335 is an activator of the two-pore domain potassium channels K2P2.1/TREK1 and K2P10.1/TREK2 (EC50s = 14.3 and 5.2 µM, respectively, in Xenopus oocytes).{47628} It is selective for K2P2.1/TREK1 and K2P10.1/TREK2 channels over K2P4.1/TRAAK channels. ML335 activates K2P2.1/TREK1 by binding to the C-type gate, which is the active site of TREK channels.
Brand:CaymanSKU:27635 - 10 mgAvailable on backorder
ML335 is an activator of the two-pore domain potassium channels K2P2.1/TREK1 and K2P10.1/TREK2 (EC50s = 14.3 and 5.2 µM, respectively, in Xenopus oocytes).{47628} It is selective for K2P2.1/TREK1 and K2P10.1/TREK2 channels over K2P4.1/TRAAK channels. ML335 activates K2P2.1/TREK1 by binding to the C-type gate, which is the active site of TREK channels.
Brand:CaymanSKU:27635 - 25 mgAvailable on backorder
ML335 is an activator of the two-pore domain potassium channels K2P2.1/TREK1 and K2P10.1/TREK2 (EC50s = 14.3 and 5.2 µM, respectively, in Xenopus oocytes).{47628} It is selective for K2P2.1/TREK1 and K2P10.1/TREK2 channels over K2P4.1/TRAAK channels. ML335 activates K2P2.1/TREK1 by binding to the C-type gate, which is the active site of TREK channels.
Brand:CaymanSKU:27635 - 5 mgAvailable on backorder
ML335 is an activator of the two-pore domain potassium channels K2P2.1/TREK1 and K2P10.1/TREK2 (EC50s = 14.3 and 5.2 µM, respectively, in Xenopus oocytes).{47628} It is selective for K2P2.1/TREK1 and K2P10.1/TREK2 channels over K2P4.1/TRAAK channels. ML335 activates K2P2.1/TREK1 by binding to the C-type gate, which is the active site of TREK channels.
Brand:CaymanSKU:27635 - 50 mgAvailable on backorder
Lipoxygenases (LOs) are non-heme iron-containing dioxygenases that catalyze the oxidation of polyunsaturated fatty acids to generate unsaturated fatty acid hydroperoxides.{3140} The immediate products of 15-LO fatty acid oxidation act as mediators in inflammation, thrombosis, and cancer.{12192} ML351 is an inhibitor of human reticulocyte 15-LO-1 (IC50 = 200 nM) with >250-fold selectivity over the related enzymes 5-LO, platelet 12-LO, 15-LO-2, ovine COX-1, and human COX-2.{29406,26085} ML351 was shown to be protective against oxidative glutamate toxicity in mouse neuronal HT-22 cells and significantly reduced infarct size in an in vivo mouse model for ischemic stroke.{29406,26085}
Brand:CaymanSKU:- Lipoxygenases (LOs) are non-heme iron-containing dioxygenases that catalyze the oxidation of polyunsaturated fatty acids to generate unsaturated fatty acid hydroperoxides.{3140} The immediate products of 15-LO fatty acid oxidation act as mediators in inflammation, thrombosis, and cancer.{12192} ML351 is an inhibitor of human reticulocyte 15-LO-1 (IC50 = 200 nM) with >250-fold selectivity over the related enzymes 5-LO, platelet 12-LO, 15-LO-2, ovine COX-1, and human COX-2.{29406,26085} ML351 was shown to be protective against oxidative glutamate toxicity in mouse neuronal HT-22 cells and significantly reduced infarct size in an in vivo mouse model for ischemic stroke.{29406,26085}
Brand:CaymanSKU:-
Platelet-type 12-lipoxygenase (12-LO; Item No. 10341) catalyzes the formation of 12-HpETE (Item No. 44570) from arachidonic acid (Item No. 90010).{3606} It has been found to be expressed in various tumor cells as well as pancreatic islets and can be activated by inflammatory cytokines.{25127} It has also been implicated in the modulation of hemostasis and thrombosis through its role in regulating platelet function.{25127} ML355 is a selective inhibitor of 12-LO with an IC50 value of 0.34 µM.{25127} It demonstrates greatly reduced potency for 15-LO-1, 15-LO-2, and 5-LO (IC50s = 9.7, >100, and >100 µM) and no inhibition of COX-1 and -2.{25127} In cell-based assays, ML355 has been shown to decrease calcium mobilization and thrombin receptor PAR4-induced platelet aggregation in patient-derived human platelets and to significantly inhibit arachidonic acid and calcium- ionophore-induced 12-HpETE synthesis in mouse BTC3 cells and human islets.{25127}
Brand:CaymanSKU:-Available on backorder
Platelet-type 12-lipoxygenase (12-LO; Item No. 10341) catalyzes the formation of 12-HpETE (Item No. 44570) from arachidonic acid (Item No. 90010).{3606} It has been found to be expressed in various tumor cells as well as pancreatic islets and can be activated by inflammatory cytokines.{25127} It has also been implicated in the modulation of hemostasis and thrombosis through its role in regulating platelet function.{25127} ML355 is a selective inhibitor of 12-LO with an IC50 value of 0.34 µM.{25127} It demonstrates greatly reduced potency for 15-LO-1, 15-LO-2, and 5-LO (IC50s = 9.7, >100, and >100 µM) and no inhibition of COX-1 and -2.{25127} In cell-based assays, ML355 has been shown to decrease calcium mobilization and thrombin receptor PAR4-induced platelet aggregation in patient-derived human platelets and to significantly inhibit arachidonic acid and calcium- ionophore-induced 12-HpETE synthesis in mouse BTC3 cells and human islets.{25127}
Brand:CaymanSKU:-Available on backorder
Platelet-type 12-lipoxygenase (12-LO; Item No. 10341) catalyzes the formation of 12-HpETE (Item No. 44570) from arachidonic acid (Item No. 90010).{3606} It has been found to be expressed in various tumor cells as well as pancreatic islets and can be activated by inflammatory cytokines.{25127} It has also been implicated in the modulation of hemostasis and thrombosis through its role in regulating platelet function.{25127} ML355 is a selective inhibitor of 12-LO with an IC50 value of 0.34 µM.{25127} It demonstrates greatly reduced potency for 15-LO-1, 15-LO-2, and 5-LO (IC50s = 9.7, >100, and >100 µM) and no inhibition of COX-1 and -2.{25127} In cell-based assays, ML355 has been shown to decrease calcium mobilization and thrombin receptor PAR4-induced platelet aggregation in patient-derived human platelets and to significantly inhibit arachidonic acid and calcium- ionophore-induced 12-HpETE synthesis in mouse BTC3 cells and human islets.{25127}
Brand:CaymanSKU:-Available on backorder
Platelet-type 12-lipoxygenase (12-LO; Item No. 10341) catalyzes the formation of 12-HpETE (Item No. 44570) from arachidonic acid (Item No. 90010).{3606} It has been found to be expressed in various tumor cells as well as pancreatic islets and can be activated by inflammatory cytokines.{25127} It has also been implicated in the modulation of hemostasis and thrombosis through its role in regulating platelet function.{25127} ML355 is a selective inhibitor of 12-LO with an IC50 value of 0.34 µM.{25127} It demonstrates greatly reduced potency for 15-LO-1, 15-LO-2, and 5-LO (IC50s = 9.7, >100, and >100 µM) and no inhibition of COX-1 and -2.{25127} In cell-based assays, ML355 has been shown to decrease calcium mobilization and thrombin receptor PAR4-induced platelet aggregation in patient-derived human platelets and to significantly inhibit arachidonic acid and calcium- ionophore-induced 12-HpETE synthesis in mouse BTC3 cells and human islets.{25127}
Brand:CaymanSKU:-Available on backorder