Cayman
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Glutamate, the major excitatory neurotransmitter in the brain, acts on both ionotropic and metabotropic glutamate receptors. Excessive metabotropic glutamate receptor (mGluR) transmission has been linked to epilepsy, ischemia, pain, anxiety, and depression. Eight subtypes (1-8) and multiple splice variants of the mGluR have been identified and grouped based on their pharmacological properties. Group I mGluRs (subtypes 1 and 5) activate the phosphatidyl inositol pathway, while Group II (2 and 3) and Group III (4, 6, 7 and 8) inhibit adenylyl cyclase. MPEP is a potent, highly selective non-competitive antagonist at the mGlu5a receptor subtype (IC50 = 36 nM) while having no agonist or antagonist activities at the mGlu1b receptor at concentrations up to 30 μM.{22822} MPEP is centrally active following systemic administration in vivo, inducing anxiolytic-like effects in rodent models of anxiety and depression when administered at 1-30 mg/kg.{22822} MPEP has also been reported as a positive allosteric modulator of mGluR4 at μM concentrations.{22823}
Brand:CaymanSKU:- Glutamate, the major excitatory neurotransmitter in the brain, acts on both ionotropic and metabotropic glutamate receptors. Excessive metabotropic glutamate receptor (mGluR) transmission has been linked to epilepsy, ischemia, pain, anxiety, and depression. Eight subtypes (1-8) and multiple splice variants of the mGluR have been identified and grouped based on their pharmacological properties. Group I mGluRs (subtypes 1 and 5) activate the phosphatidyl inositol pathway, while Group II (2 and 3) and Group III (4, 6, 7 and 8) inhibit adenylyl cyclase. MPEP is a potent, highly selective non-competitive antagonist at the mGlu5a receptor subtype (IC50 = 36 nM) while having no agonist or antagonist activities at the mGlu1b receptor at concentrations up to 30 μM.{22822} MPEP is centrally active following systemic administration in vivo, inducing anxiolytic-like effects in rodent models of anxiety and depression when administered at 1-30 mg/kg.{22822} MPEP has also been reported as a positive allosteric modulator of mGluR4 at μM concentrations.{22823}
Brand:CaymanSKU:-
MPI-0441138 is a potent inducer of apoptosis and growth inhibition (EC50 = 2 nM for both processes, based on caspase-3 activation and total cellular ATP, respectively) in T47D and HCT116 cells.{16623,32891} MPI-0441138 has excellent blood brain barrier penetration and is effective in mouse xenograft cancer models.{16623,32891}
Brand:CaymanSKU:- MPI-0441138 is a potent inducer of apoptosis and growth inhibition (EC50 = 2 nM for both processes, based on caspase-3 activation and total cellular ATP, respectively) in T47D and HCT116 cells.{16623,32891} MPI-0441138 has excellent blood brain barrier penetration and is effective in mouse xenograft cancer models.{16623,32891}
Brand:CaymanSKU:- MPI-0441138 is a potent inducer of apoptosis and growth inhibition (EC50 = 2 nM for both processes, based on caspase-3 activation and total cellular ATP, respectively) in T47D and HCT116 cells.{16623,32891} MPI-0441138 has excellent blood brain barrier penetration and is effective in mouse xenograft cancer models.{16623,32891}
Brand:CaymanSKU:- MPI-0441138 is a potent inducer of apoptosis and growth inhibition (EC50 = 2 nM for both processes, based on caspase-3 activation and total cellular ATP, respectively) in T47D and HCT116 cells.{16623,32891} MPI-0441138 has excellent blood brain barrier penetration and is effective in mouse xenograft cancer models.{16623,32891}
Brand:CaymanSKU:-
MPI-0479605 is a potent and ATP-competitive inhibitor of the mitotic kinase MPS1 (IC50 = 1.8 nM).{38558} It is selective for MPS1 over a panel of 79 kinases at a concentration of 500 nM. MPI-0479605 induces time-dependent degradation of cyclin B and securin and decreases phosphorylation of BUBR1 resulting in failed cytokinesis in HeLa cells arrested by nocodazole (Item No. 13857). It also causes misalignment of chromosomes at the anaphase plate and aneuploidy in A549 cells and slows cell cycle progression of HCT116 and COLO 205 cells irrespective of p53 activity. MPI-0479605 (30-150 mg/kg) reduces tumor volume in an HCT116 mouse colon cancer xenograft model in a dose-dependent manner.
Brand:CaymanSKU:22136 -Out of stock
MPI-0479605 is a potent and ATP-competitive inhibitor of the mitotic kinase MPS1 (IC50 = 1.8 nM).{38558} It is selective for MPS1 over a panel of 79 kinases at a concentration of 500 nM. MPI-0479605 induces time-dependent degradation of cyclin B and securin and decreases phosphorylation of BUBR1 resulting in failed cytokinesis in HeLa cells arrested by nocodazole (Item No. 13857). It also causes misalignment of chromosomes at the anaphase plate and aneuploidy in A549 cells and slows cell cycle progression of HCT116 and COLO 205 cells irrespective of p53 activity. MPI-0479605 (30-150 mg/kg) reduces tumor volume in an HCT116 mouse colon cancer xenograft model in a dose-dependent manner.
Brand:CaymanSKU:22136 -Out of stock
MPI-0479605 is a potent and ATP-competitive inhibitor of the mitotic kinase MPS1 (IC50 = 1.8 nM).{38558} It is selective for MPS1 over a panel of 79 kinases at a concentration of 500 nM. MPI-0479605 induces time-dependent degradation of cyclin B and securin and decreases phosphorylation of BUBR1 resulting in failed cytokinesis in HeLa cells arrested by nocodazole (Item No. 13857). It also causes misalignment of chromosomes at the anaphase plate and aneuploidy in A549 cells and slows cell cycle progression of HCT116 and COLO 205 cells irrespective of p53 activity. MPI-0479605 (30-150 mg/kg) reduces tumor volume in an HCT116 mouse colon cancer xenograft model in a dose-dependent manner.
Brand:CaymanSKU:22136 -Out of stock
MPI-0479605 is a potent and ATP-competitive inhibitor of the mitotic kinase MPS1 (IC50 = 1.8 nM).{38558} It is selective for MPS1 over a panel of 79 kinases at a concentration of 500 nM. MPI-0479605 induces time-dependent degradation of cyclin B and securin and decreases phosphorylation of BUBR1 resulting in failed cytokinesis in HeLa cells arrested by nocodazole (Item No. 13857). It also causes misalignment of chromosomes at the anaphase plate and aneuploidy in A549 cells and slows cell cycle progression of HCT116 and COLO 205 cells irrespective of p53 activity. MPI-0479605 (30-150 mg/kg) reduces tumor volume in an HCT116 mouse colon cancer xenograft model in a dose-dependent manner.
Brand:CaymanSKU:22136 -Out of stock
Brand:CaymanSKU:700164 - 1 eaAvailable on backorder
MPP+ is an active metabolite of MPTP, a neurotoxin used to cause selective destruction of dopaminergic neurons in animal models of parkinsonism.{31390,31391,31393,31392} MPP+ induces neurotoxicity primarily by inhibiting complex I of the mitochondrial electron transport chain, resulting in ATP depletion and increased oxidative stress.{31394} The key features of different neurotoxic models of Parkinson’s disease, including the MPTP model, have been detailed.{31394}
Brand:CaymanSKU:-Out of stock
MPP+ is an active metabolite of MPTP, a neurotoxin used to cause selective destruction of dopaminergic neurons in animal models of parkinsonism.{31390,31391,31393,31392} MPP+ induces neurotoxicity primarily by inhibiting complex I of the mitochondrial electron transport chain, resulting in ATP depletion and increased oxidative stress.{31394} The key features of different neurotoxic models of Parkinson’s disease, including the MPTP model, have been detailed.{31394}
Brand:CaymanSKU:-Out of stock
MPP+ is an active metabolite of MPTP, a neurotoxin used to cause selective destruction of dopaminergic neurons in animal models of parkinsonism.{31390,31391,31393,31392} MPP+ induces neurotoxicity primarily by inhibiting complex I of the mitochondrial electron transport chain, resulting in ATP depletion and increased oxidative stress.{31394} The key features of different neurotoxic models of Parkinson’s disease, including the MPTP model, have been detailed.{31394}
Brand:CaymanSKU:-Out of stock
MPro inhibitor 11a is an inhibitor of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) main protease (MPro; IC50 = 0.053 µM in a TR-FRET assay).{59192} It reduces viral yield in the culture supernatant of SARS-CoV-2-infected Vero E6 cells (EC50 = 0.53 µM). MPro inhibitor 11a also reduces viral RNA copy numbers in the same model when used at concentrations ranging from 1.85 to 50 µM.
Brand:CaymanSKU:31344 - 1 mgAvailable on backorder
MPro inhibitor 11a is an inhibitor of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) main protease (MPro; IC50 = 0.053 µM in a TR-FRET assay).{59192} It reduces viral yield in the culture supernatant of SARS-CoV-2-infected Vero E6 cells (EC50 = 0.53 µM). MPro inhibitor 11a also reduces viral RNA copy numbers in the same model when used at concentrations ranging from 1.85 to 50 µM.
Brand:CaymanSKU:31344 - 10 mgAvailable on backorder
MPro inhibitor 11a is an inhibitor of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) main protease (MPro; IC50 = 0.053 µM in a TR-FRET assay).{59192} It reduces viral yield in the culture supernatant of SARS-CoV-2-infected Vero E6 cells (EC50 = 0.53 µM). MPro inhibitor 11a also reduces viral RNA copy numbers in the same model when used at concentrations ranging from 1.85 to 50 µM.
Brand:CaymanSKU:31344 - 5 mgAvailable on backorder
MPro inhibitor 11b is an inhibitor of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) main protease (MPro; IC50 = 0.04 µM in a TR-FRET assay).{59192} It reduces viral yield in the culture supernatant of SARS-CoV-2-infected Vero E6 cells (EC50 = 0.72 µM). MPro inhibitor 11b also reduces viral RNA copy numbers in the same model when used at concentrations ranging from 1.85 to 50 µM.
Brand:CaymanSKU:31345 - 1 mgAvailable on backorder
MPro inhibitor 11b is an inhibitor of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) main protease (MPro; IC50 = 0.04 µM in a TR-FRET assay).{59192} It reduces viral yield in the culture supernatant of SARS-CoV-2-infected Vero E6 cells (EC50 = 0.72 µM). MPro inhibitor 11b also reduces viral RNA copy numbers in the same model when used at concentrations ranging from 1.85 to 50 µM.
Brand:CaymanSKU:31345 - 10 mgAvailable on backorder
MPro inhibitor 11b is an inhibitor of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) main protease (MPro; IC50 = 0.04 µM in a TR-FRET assay).{59192} It reduces viral yield in the culture supernatant of SARS-CoV-2-infected Vero E6 cells (EC50 = 0.72 µM). MPro inhibitor 11b also reduces viral RNA copy numbers in the same model when used at concentrations ranging from 1.85 to 50 µM.
Brand:CaymanSKU:31345 - 5 mgAvailable on backorder
Mps1-IN-1 is a selective inhibitor of monopolar spindle 1 (Mps1) kinase (IC50 = 367 nM), a dual-specificity kinase involved in spindle assembly checkpoint and the maintenance of chromosomal stability.{31848} It exhibits greater than 1,000-fold selectivity against a panel of 352 kinases.{31848} Mps1-IN-1 has been shown to disrupt the recruitment of Mad2 to kinetochores and to increase the frequency of multipolar mitosis in U2OS cells.{31848}
Brand:CaymanSKU:-Available on backorder
Mps1-IN-1 is a selective inhibitor of monopolar spindle 1 (Mps1) kinase (IC50 = 367 nM), a dual-specificity kinase involved in spindle assembly checkpoint and the maintenance of chromosomal stability.{31848} It exhibits greater than 1,000-fold selectivity against a panel of 352 kinases.{31848} Mps1-IN-1 has been shown to disrupt the recruitment of Mad2 to kinetochores and to increase the frequency of multipolar mitosis in U2OS cells.{31848}
Brand:CaymanSKU:-Available on backorder
Mps1-IN-1 is a selective inhibitor of monopolar spindle 1 (Mps1) kinase (IC50 = 367 nM), a dual-specificity kinase involved in spindle assembly checkpoint and the maintenance of chromosomal stability.{31848} It exhibits greater than 1,000-fold selectivity against a panel of 352 kinases.{31848} Mps1-IN-1 has been shown to disrupt the recruitment of Mad2 to kinetochores and to increase the frequency of multipolar mitosis in U2OS cells.{31848}
Brand:CaymanSKU:-Available on backorder
Mps1-IN-1 is a selective inhibitor of monopolar spindle 1 (Mps1) kinase (IC50 = 367 nM), a dual-specificity kinase involved in spindle assembly checkpoint and the maintenance of chromosomal stability.{31848} It exhibits greater than 1,000-fold selectivity against a panel of 352 kinases.{31848} Mps1-IN-1 has been shown to disrupt the recruitment of Mad2 to kinetochores and to increase the frequency of multipolar mitosis in U2OS cells.{31848}
Brand:CaymanSKU:-Available on backorder
Mps1-IN-2 is an ATP-competitive inhibitor of the checkpoint kinase Mps1 (IC50 = 145 nM).{31848} It is 1,000-fold selective for Mps1 over a panel of 352 kinases at 10 μM, but does inhibit Plk1 (Kd = 61 nM).
Brand:CaymanSKU:-Available on backorder
Mps1-IN-2 is an ATP-competitive inhibitor of the checkpoint kinase Mps1 (IC50 = 145 nM).{31848} It is 1,000-fold selective for Mps1 over a panel of 352 kinases at 10 μM, but does inhibit Plk1 (Kd = 61 nM).
Brand:CaymanSKU:-Available on backorder
Mps1-IN-2 is an ATP-competitive inhibitor of the checkpoint kinase Mps1 (IC50 = 145 nM).{31848} It is 1,000-fold selective for Mps1 over a panel of 352 kinases at 10 μM, but does inhibit Plk1 (Kd = 61 nM).
Brand:CaymanSKU:-Available on backorder
Mps1-IN-2 is an ATP-competitive inhibitor of the checkpoint kinase Mps1 (IC50 = 145 nM).{31848} It is 1,000-fold selective for Mps1 over a panel of 352 kinases at 10 μM, but does inhibit Plk1 (Kd = 61 nM).
Brand:CaymanSKU:-Available on backorder
MPS1/TTK inhibitor is an inhibitor of monopolar spindle 1 (MPS1/TTK; IC50 = 5.8 nM), a kinase involved in mitotic spindle checkpoint signaling that is overexpressed in certain cancerous tumors.{37673,37672} It inhibits MPS1 phosphorylation of kinetochore scaffold 1 (KNL1) and increases the rate of mitosis and the number of cells entering anaphase within 15 minutes, indicating MPS1 checkpoint inhibition, when used at a concentration of 100 nM.{37673} MPS1/TTK inhibitor (50 and 100 nM) increases the number of missegregated chromosomes, with an increased number of errors at 100 nM compared with 50 nM. It also inhibits colony formation of DLD1, HCT116, and U2OS cells (IC50s = 24.6, 20.1, and 20.6 nM, respectively).
Brand:CaymanSKU:25554 - 1 mgAvailable on backorder
MPS1/TTK inhibitor is an inhibitor of monopolar spindle 1 (MPS1/TTK; IC50 = 5.8 nM), a kinase involved in mitotic spindle checkpoint signaling that is overexpressed in certain cancerous tumors.{37673,37672} It inhibits MPS1 phosphorylation of kinetochore scaffold 1 (KNL1) and increases the rate of mitosis and the number of cells entering anaphase within 15 minutes, indicating MPS1 checkpoint inhibition, when used at a concentration of 100 nM.{37673} MPS1/TTK inhibitor (50 and 100 nM) increases the number of missegregated chromosomes, with an increased number of errors at 100 nM compared with 50 nM. It also inhibits colony formation of DLD1, HCT116, and U2OS cells (IC50s = 24.6, 20.1, and 20.6 nM, respectively).
Brand:CaymanSKU:25554 - 10 mgAvailable on backorder
MPS1/TTK inhibitor is an inhibitor of monopolar spindle 1 (MPS1/TTK; IC50 = 5.8 nM), a kinase involved in mitotic spindle checkpoint signaling that is overexpressed in certain cancerous tumors.{37673,37672} It inhibits MPS1 phosphorylation of kinetochore scaffold 1 (KNL1) and increases the rate of mitosis and the number of cells entering anaphase within 15 minutes, indicating MPS1 checkpoint inhibition, when used at a concentration of 100 nM.{37673} MPS1/TTK inhibitor (50 and 100 nM) increases the number of missegregated chromosomes, with an increased number of errors at 100 nM compared with 50 nM. It also inhibits colony formation of DLD1, HCT116, and U2OS cells (IC50s = 24.6, 20.1, and 20.6 nM, respectively).
Brand:CaymanSKU:25554 - 25 mgAvailable on backorder
MPS1/TTK inhibitor is an inhibitor of monopolar spindle 1 (MPS1/TTK; IC50 = 5.8 nM), a kinase involved in mitotic spindle checkpoint signaling that is overexpressed in certain cancerous tumors.{37673,37672} It inhibits MPS1 phosphorylation of kinetochore scaffold 1 (KNL1) and increases the rate of mitosis and the number of cells entering anaphase within 15 minutes, indicating MPS1 checkpoint inhibition, when used at a concentration of 100 nM.{37673} MPS1/TTK inhibitor (50 and 100 nM) increases the number of missegregated chromosomes, with an increased number of errors at 100 nM compared with 50 nM. It also inhibits colony formation of DLD1, HCT116, and U2OS cells (IC50s = 24.6, 20.1, and 20.6 nM, respectively).
Brand:CaymanSKU:25554 - 5 mgAvailable on backorder
MPT0B014 is an inhibitor of tubulin polymerization.{53719} It inhibits proliferation of A549, H1299, and H226 human non-small cell lung cancer (NSCLC) cells (IC50s = 0.041, 0.046, and 0.041 µM, respectively), as well as adriamycin-resistant NCI/ADR cells that overexpress P-glycoprotein (IC50 = ~0.03 µM). MPT0B014 (0.3 µM) induces cell cycle arrest at the G2/M phase and apoptosis in A549 cells. It reduces tumor growth in an A549 mouse xenograft model when administered in combination with the EGFR tyrosine kinase inhibitor erlotinib (Item No. 10483).
Brand:CaymanSKU:21718 -Out of stock
MPT0B014 is an inhibitor of tubulin polymerization.{53719} It inhibits proliferation of A549, H1299, and H226 human non-small cell lung cancer (NSCLC) cells (IC50s = 0.041, 0.046, and 0.041 µM, respectively), as well as adriamycin-resistant NCI/ADR cells that overexpress P-glycoprotein (IC50 = ~0.03 µM). MPT0B014 (0.3 µM) induces cell cycle arrest at the G2/M phase and apoptosis in A549 cells. It reduces tumor growth in an A549 mouse xenograft model when administered in combination with the EGFR tyrosine kinase inhibitor erlotinib (Item No. 10483).
Brand:CaymanSKU:21718 -Out of stock
MPT0B014 is an inhibitor of tubulin polymerization.{53719} It inhibits proliferation of A549, H1299, and H226 human non-small cell lung cancer (NSCLC) cells (IC50s = 0.041, 0.046, and 0.041 µM, respectively), as well as adriamycin-resistant NCI/ADR cells that overexpress P-glycoprotein (IC50 = ~0.03 µM). MPT0B014 (0.3 µM) induces cell cycle arrest at the G2/M phase and apoptosis in A549 cells. It reduces tumor growth in an A549 mouse xenograft model when administered in combination with the EGFR tyrosine kinase inhibitor erlotinib (Item No. 10483).
Brand:CaymanSKU:21718 -Out of stock
MPT0B014 is an inhibitor of tubulin polymerization.{53719} It inhibits proliferation of A549, H1299, and H226 human non-small cell lung cancer (NSCLC) cells (IC50s = 0.041, 0.046, and 0.041 µM, respectively), as well as adriamycin-resistant NCI/ADR cells that overexpress P-glycoprotein (IC50 = ~0.03 µM). MPT0B014 (0.3 µM) induces cell cycle arrest at the G2/M phase and apoptosis in A549 cells. It reduces tumor growth in an A549 mouse xenograft model when administered in combination with the EGFR tyrosine kinase inhibitor erlotinib (Item No. 10483).
Brand:CaymanSKU:21718 -Out of stock
Prostacyclin (PGI2) is a potent vasorelaxant and inhibitor of platelet aggregation. It mediates its actions by binding to a specific G protein-coupled receptor, the IP receptor, on the surface of endothelial cells, arterial smooth muscle, and platelets.{4375} The IP receptor also participates in signal transduction of the pain response, cardioprotection, and inflammation.{5018,9805,8508,5466} MRE-269 is the active form of the prodrug NS-304. It is a potent and selective agonist for the human IP receptor with a Ki value of 20 nM.{14998} In contrast to PGI2, which has a half-life of 30 seconds to a few minutes in vivo, plasma concentrations of MRE-269 remain near peak levels for more than eight hours in rats and dogs.{14998} Unlike the PGI2 analogues, beraprost and iloprost, MRE-269 lacks high affinity for the EP3 receptor.{16443} As a result, MRE-269 induces vasodilation equally in large and small pulmonary arteries, whereas vasodilation of small arteries by beraprost and iloprost is reduced via EP3-mediated vasoconstriction.{16443}
Brand:CaymanSKU:10010412 - 1 mgAvailable on backorder
Prostacyclin (PGI2) is a potent vasorelaxant and inhibitor of platelet aggregation. It mediates its actions by binding to a specific G protein-coupled receptor, the IP receptor, on the surface of endothelial cells, arterial smooth muscle, and platelets.{4375} The IP receptor also participates in signal transduction of the pain response, cardioprotection, and inflammation.{5018,9805,8508,5466} MRE-269 is the active form of the prodrug NS-304. It is a potent and selective agonist for the human IP receptor with a Ki value of 20 nM.{14998} In contrast to PGI2, which has a half-life of 30 seconds to a few minutes in vivo, plasma concentrations of MRE-269 remain near peak levels for more than eight hours in rats and dogs.{14998} Unlike the PGI2 analogues, beraprost and iloprost, MRE-269 lacks high affinity for the EP3 receptor.{16443} As a result, MRE-269 induces vasodilation equally in large and small pulmonary arteries, whereas vasodilation of small arteries by beraprost and iloprost is reduced via EP3-mediated vasoconstriction.{16443}
Brand:CaymanSKU:10010412 - 10 mgAvailable on backorder
Prostacyclin (PGI2) is a potent vasorelaxant and inhibitor of platelet aggregation. It mediates its actions by binding to a specific G protein-coupled receptor, the IP receptor, on the surface of endothelial cells, arterial smooth muscle, and platelets.{4375} The IP receptor also participates in signal transduction of the pain response, cardioprotection, and inflammation.{5018,9805,8508,5466} MRE-269 is the active form of the prodrug NS-304. It is a potent and selective agonist for the human IP receptor with a Ki value of 20 nM.{14998} In contrast to PGI2, which has a half-life of 30 seconds to a few minutes in vivo, plasma concentrations of MRE-269 remain near peak levels for more than eight hours in rats and dogs.{14998} Unlike the PGI2 analogues, beraprost and iloprost, MRE-269 lacks high affinity for the EP3 receptor.{16443} As a result, MRE-269 induces vasodilation equally in large and small pulmonary arteries, whereas vasodilation of small arteries by beraprost and iloprost is reduced via EP3-mediated vasoconstriction.{16443}
Brand:CaymanSKU:10010412 - 5 mgAvailable on backorder
Prostacyclin (PGI2) is a potent vasorelaxant and inhibitor of platelet aggregation. It mediates its actions by binding to a specific G protein-coupled receptor, the IP receptor, on the surface of endothelial cells, arterial smooth muscle, and platelets.{4375} The IP receptor also participates in signal transduction of the pain response, cardioprotection, and inflammation.{5018,9805,8508,5466} MRE-269 is the active form of the prodrug NS-304. It is a potent and selective agonist for the human IP receptor with a Ki value of 20 nM.{14998} In contrast to PGI2, which has a half-life of 30 seconds to a few minutes in vivo, plasma concentrations of MRE-269 remain near peak levels for more than eight hours in rats and dogs.{14998} Unlike the PGI2 analogues, beraprost and iloprost, MRE-269 lacks high affinity for the EP3 receptor.{16443} As a result, MRE-269 induces vasodilation equally in large and small pulmonary arteries, whereas vasodilation of small arteries by beraprost and iloprost is reduced via EP3-mediated vasoconstriction.{16443}
Brand:CaymanSKU:10010412 - 50 mgAvailable on backorder
MreB is an actin-like protein expressed in bacteria.{25735} It determines the rod shape of cells and has critical roles in cell division, chromosome segregation, and cell polarity.{25734} MreB perturbing compound A22 is a benzylisothiourea compound that interacts with the ATP binding site of MreB rapidly and reversibly.{25730} It blocks normal rod shape formation and inhibits chromosome partitioning in E. coli, inhibiting growth (MIC = 3.1 µg/ml).{25731} It interferes with chromosome segregation in C. crescentus by preventing MreB binding to chromosomes.{25730} In V. cholerae, A22 prevents the development of normal cell shape and alters nucleoid morphology.{25733}
Brand:CaymanSKU:- MreB is an actin-like protein expressed in bacteria.{25735} It determines the rod shape of cells and has critical roles in cell division, chromosome segregation, and cell polarity.{25734} MreB perturbing compound A22 is a benzylisothiourea compound that interacts with the ATP binding site of MreB rapidly and reversibly.{25730} It blocks normal rod shape formation and inhibits chromosome partitioning in E. coli, inhibiting growth (MIC = 3.1 µg/ml).{25731} It interferes with chromosome segregation in C. crescentus by preventing MreB binding to chromosomes.{25730} In V. cholerae, A22 prevents the development of normal cell shape and alters nucleoid morphology.{25733}
Brand:CaymanSKU:- MreB is an actin-like protein expressed in bacteria.{25735} It determines the rod shape of cells and has critical roles in cell division, chromosome segregation, and cell polarity.{25734} MreB perturbing compound A22 is a benzylisothiourea compound that interacts with the ATP binding site of MreB rapidly and reversibly.{25730} It blocks normal rod shape formation and inhibits chromosome partitioning in E. coli, inhibiting growth (MIC = 3.1 µg/ml).{25731} It interferes with chromosome segregation in C. crescentus by preventing MreB binding to chromosomes.{25730} In V. cholerae, A22 prevents the development of normal cell shape and alters nucleoid morphology.{25733}
Brand:CaymanSKU:-
MRK-560 is a potent inhibitor of γ-secretase (IC50 = 0.65 nM).{48318} In vivo, MRK-560 (1-10 mg/kg) reduces diethanolamine-soluble amyloid-β (1-40) (Aβ40) levels in APP-YAC transgenic mouse brain. MRK-560 reduces brain and cerebrospinal fluid Aβ40 levels in rats (ED50s = 6 and 10 mg/kg, respectively).{48319} It also decreases brain-soluble Aβ40 and Aβ42 levels and recovers hippocampal long-term potentiation in the Tg2576 transgenic mouse model of Alzheimer’s disease.{48320}
Brand:CaymanSKU:27599 - 1 mgAvailable on backorder
MRK-560 is a potent inhibitor of γ-secretase (IC50 = 0.65 nM).{48318} In vivo, MRK-560 (1-10 mg/kg) reduces diethanolamine-soluble amyloid-β (1-40) (Aβ40) levels in APP-YAC transgenic mouse brain. MRK-560 reduces brain and cerebrospinal fluid Aβ40 levels in rats (ED50s = 6 and 10 mg/kg, respectively).{48319} It also decreases brain-soluble Aβ40 and Aβ42 levels and recovers hippocampal long-term potentiation in the Tg2576 transgenic mouse model of Alzheimer’s disease.{48320}
Brand:CaymanSKU:27599 - 5 mgAvailable on backorder
MRS1523 is a selective adenosine A3 receptor antagonist (Kis = 18.9 and 113 nM for human and rat A3 receptors, respectively, versus Kis = 15.6 and 2.05 µM for rat A1 and A2A receptors, respectively).{27829} As activation of the A3 receptor is linked to several second messenger systems for signaling pathways involving inflammatory, asthmatic, and ischemic responses, this selective antagonist may be useful in characterizing the various functions of the receptor.
Brand:CaymanSKU:-Out of stock
MRS1523 is a selective adenosine A3 receptor antagonist (Kis = 18.9 and 113 nM for human and rat A3 receptors, respectively, versus Kis = 15.6 and 2.05 µM for rat A1 and A2A receptors, respectively).{27829} As activation of the A3 receptor is linked to several second messenger systems for signaling pathways involving inflammatory, asthmatic, and ischemic responses, this selective antagonist may be useful in characterizing the various functions of the receptor.
Brand:CaymanSKU:-Out of stock
MRS1523 is a selective adenosine A3 receptor antagonist (Kis = 18.9 and 113 nM for human and rat A3 receptors, respectively, versus Kis = 15.6 and 2.05 µM for rat A1 and A2A receptors, respectively).{27829} As activation of the A3 receptor is linked to several second messenger systems for signaling pathways involving inflammatory, asthmatic, and ischemic responses, this selective antagonist may be useful in characterizing the various functions of the receptor.
Brand:CaymanSKU:-Out of stock
MRS1523 is a selective adenosine A3 receptor antagonist (Kis = 18.9 and 113 nM for human and rat A3 receptors, respectively, versus Kis = 15.6 and 2.05 µM for rat A1 and A2A receptors, respectively).{27829} As activation of the A3 receptor is linked to several second messenger systems for signaling pathways involving inflammatory, asthmatic, and ischemic responses, this selective antagonist may be useful in characterizing the various functions of the receptor.
Brand:CaymanSKU:-Out of stock
MRS1706 is a selective adenosine A2B receptor inverse agonist with Ki values of 1.39, 157, 112, and 230 nM for human A2B, A1, A2A, and A3 receptors, respectively.{32640,32641}
Brand:CaymanSKU:-Available on backorder
MRS1706 is a selective adenosine A2B receptor inverse agonist with Ki values of 1.39, 157, 112, and 230 nM for human A2B, A1, A2A, and A3 receptors, respectively.{32640,32641}
Brand:CaymanSKU:-Available on backorder
MRS1706 is a selective adenosine A2B receptor inverse agonist with Ki values of 1.39, 157, 112, and 230 nM for human A2B, A1, A2A, and A3 receptors, respectively.{32640,32641}
Brand:CaymanSKU:-Available on backorder
MRS1706 is a selective adenosine A2B receptor inverse agonist with Ki values of 1.39, 157, 112, and 230 nM for human A2B, A1, A2A, and A3 receptors, respectively.{32640,32641}
Brand:CaymanSKU:-Available on backorder
MRS2179 is a competitive purinergic P2Y1 receptor antagonist (Kb = 102 nM).{53657} It is selective for P2Y1 over P2Y2, P2Y4, P2Y6, P2Y12, and P2Y13, as well as P2X1-4, receptors at 10 µM.{19258,53658} MRS2179 reduces phospholipase C (PLC) activity induced by the P2Y receptor agonist 2-methylthioadenosine diphosphate (2-MeSADP; Item No. 21230) with an IC50 value of 331 nM in turkey erythrocyte membranes that endogenously express high levels of the P2Y1 receptor.{53657} It inhibits platelet shape change and aggregation induced by ADP (Item No. 21121) in washed isolated human platelets when used at a concentration of 10 µM.{33272} MRS2179 (50 mg/kg, i.v.) prolongs the length of tail bleeding time in mice, as well as decreases platelet thrombus formation in a mouse model of iron chloride-induced arterial thrombosis.{33272,53659}
Brand:CaymanSKU:10011450 - 1 mgAvailable on backorder
MRS2179 is a competitive purinergic P2Y1 receptor antagonist (Kb = 102 nM).{53657} It is selective for P2Y1 over P2Y2, P2Y4, P2Y6, P2Y12, and P2Y13, as well as P2X1-4, receptors at 10 µM.{19258,53658} MRS2179 reduces phospholipase C (PLC) activity induced by the P2Y receptor agonist 2-methylthioadenosine diphosphate (2-MeSADP; Item No. 21230) with an IC50 value of 331 nM in turkey erythrocyte membranes that endogenously express high levels of the P2Y1 receptor.{53657} It inhibits platelet shape change and aggregation induced by ADP (Item No. 21121) in washed isolated human platelets when used at a concentration of 10 µM.{33272} MRS2179 (50 mg/kg, i.v.) prolongs the length of tail bleeding time in mice, as well as decreases platelet thrombus formation in a mouse model of iron chloride-induced arterial thrombosis.{33272,53659}
Brand:CaymanSKU:10011450 - 10 mgAvailable on backorder
MRS2179 is a competitive purinergic P2Y1 receptor antagonist (Kb = 102 nM).{53657} It is selective for P2Y1 over P2Y2, P2Y4, P2Y6, P2Y12, and P2Y13, as well as P2X1-4, receptors at 10 µM.{19258,53658} MRS2179 reduces phospholipase C (PLC) activity induced by the P2Y receptor agonist 2-methylthioadenosine diphosphate (2-MeSADP; Item No. 21230) with an IC50 value of 331 nM in turkey erythrocyte membranes that endogenously express high levels of the P2Y1 receptor.{53657} It inhibits platelet shape change and aggregation induced by ADP (Item No. 21121) in washed isolated human platelets when used at a concentration of 10 µM.{33272} MRS2179 (50 mg/kg, i.v.) prolongs the length of tail bleeding time in mice, as well as decreases platelet thrombus formation in a mouse model of iron chloride-induced arterial thrombosis.{33272,53659}
Brand:CaymanSKU:10011450 - 5 mgAvailable on backorder
MRS2578 is an antagonist of the purinergic P2Y6 receptor (IC50s = 37 and 98 nM for human and rat receptors, respectively).{33101} It is without effect at other purinergic receptors. MRS2578 is used to study the cellular and physiological roles of P2Y6.{33098,33099,33100,33102}
Brand:CaymanSKU:19704 -Available on backorder
MRS2578 is an antagonist of the purinergic P2Y6 receptor (IC50s = 37 and 98 nM for human and rat receptors, respectively).{33101} It is without effect at other purinergic receptors. MRS2578 is used to study the cellular and physiological roles of P2Y6.{33098,33099,33100,33102}
Brand:CaymanSKU:19704 -Available on backorder
MRS2578 is an antagonist of the purinergic P2Y6 receptor (IC50s = 37 and 98 nM for human and rat receptors, respectively).{33101} It is without effect at other purinergic receptors. MRS2578 is used to study the cellular and physiological roles of P2Y6.{33098,33099,33100,33102}
Brand:CaymanSKU:19704 -Available on backorder
MRS2578 is an antagonist of the purinergic P2Y6 receptor (IC50s = 37 and 98 nM for human and rat receptors, respectively).{33101} It is without effect at other purinergic receptors. MRS2578 is used to study the cellular and physiological roles of P2Y6.{33098,33099,33100,33102}
Brand:CaymanSKU:19704 -Available on backorder
MRT10 is an antagonist of the Smoothened (Smo) receptor with an IC50 value of 0.64 μM in a luciferase reporter assay.{24331,38182} It also inhibits bodipy-cyclopamine binding to the murine Smo receptor (IC50 = 0.5 μM) when expressed in HEK293 cells.{24331}
Brand:CaymanSKU:22138 -Out of stock
MRT10 is an antagonist of the Smoothened (Smo) receptor with an IC50 value of 0.64 μM in a luciferase reporter assay.{24331,38182} It also inhibits bodipy-cyclopamine binding to the murine Smo receptor (IC50 = 0.5 μM) when expressed in HEK293 cells.{24331}
Brand:CaymanSKU:22138 -Out of stock
MRT10 is an antagonist of the Smoothened (Smo) receptor with an IC50 value of 0.64 μM in a luciferase reporter assay.{24331,38182} It also inhibits bodipy-cyclopamine binding to the murine Smo receptor (IC50 = 0.5 μM) when expressed in HEK293 cells.{24331}
Brand:CaymanSKU:22138 -Out of stock
MRT10 is an antagonist of the Smoothened (Smo) receptor with an IC50 value of 0.64 μM in a luciferase reporter assay.{24331,38182} It also inhibits bodipy-cyclopamine binding to the murine Smo receptor (IC50 = 0.5 μM) when expressed in HEK293 cells.{24331}
Brand:CaymanSKU:22138 -Out of stock
MRT67307 is a kinase inhibitor that has been shown to inhibit TBK1, MARK1-4, IKKε, and NUAK1 (IC50 values are 19, 27-52, 160, and 230 nM, respectively), the salt-inducible kinases (SIKs; IC50s = 250, 67, and 430 nM for SIK1, SIK2, and SIK3, respectively) and ULK1 and ULK2 (IC50s = 45 and 38 nM, respectively).{32502,32503,30901,32504} MRT67307 prevents the phosphorylation of IRF3 and the production of IFN-β and increases toll-like receptor-induced IL-10 and IL-1ra secretion in macrophages.{32502,30901} Through its effects on ULK1 and ULK2, MRT67307 blocks autophagy.{32504}
Brand:CaymanSKU:19916 -Available on backorder
MRT67307 is a kinase inhibitor that has been shown to inhibit TBK1, MARK1-4, IKKε, and NUAK1 (IC50 values are 19, 27-52, 160, and 230 nM, respectively), the salt-inducible kinases (SIKs; IC50s = 250, 67, and 430 nM for SIK1, SIK2, and SIK3, respectively) and ULK1 and ULK2 (IC50s = 45 and 38 nM, respectively).{32502,32503,30901,32504} MRT67307 prevents the phosphorylation of IRF3 and the production of IFN-β and increases toll-like receptor-induced IL-10 and IL-1ra secretion in macrophages.{32502,30901} Through its effects on ULK1 and ULK2, MRT67307 blocks autophagy.{32504}
Brand:CaymanSKU:19916 -Available on backorder
MRT67307 is a kinase inhibitor that has been shown to inhibit TBK1, MARK1-4, IKKε, and NUAK1 (IC50 values are 19, 27-52, 160, and 230 nM, respectively), the salt-inducible kinases (SIKs; IC50s = 250, 67, and 430 nM for SIK1, SIK2, and SIK3, respectively) and ULK1 and ULK2 (IC50s = 45 and 38 nM, respectively).{32502,32503,30901,32504} MRT67307 prevents the phosphorylation of IRF3 and the production of IFN-β and increases toll-like receptor-induced IL-10 and IL-1ra secretion in macrophages.{32502,30901} Through its effects on ULK1 and ULK2, MRT67307 blocks autophagy.{32504}
Brand:CaymanSKU:19916 -Available on backorder
MRT67307 is a kinase inhibitor that has been shown to inhibit TBK1, MARK1-4, IKKε, and NUAK1 (IC50 values are 19, 27-52, 160, and 230 nM, respectively), the salt-inducible kinases (SIKs; IC50s = 250, 67, and 430 nM for SIK1, SIK2, and SIK3, respectively) and ULK1 and ULK2 (IC50s = 45 and 38 nM, respectively).{32502,32503,30901,32504} MRT67307 prevents the phosphorylation of IRF3 and the production of IFN-β and increases toll-like receptor-induced IL-10 and IL-1ra secretion in macrophages.{32502,30901} Through its effects on ULK1 and ULK2, MRT67307 blocks autophagy.{32504}
Brand:CaymanSKU:19916 -Available on backorder
MRT68921 is an inhibitor of ULK1 and ULK2 (IC50s = 2.9 and 1.1 nM, respectively).{32504} Through its effects on ULK1, MRT68921 blocks autophagy in cells, driving the accumulation of stalled early autophagosomal structures.{32504}
Brand:CaymanSKU:19905 -Available on backorder
MRT68921 is an inhibitor of ULK1 and ULK2 (IC50s = 2.9 and 1.1 nM, respectively).{32504} Through its effects on ULK1, MRT68921 blocks autophagy in cells, driving the accumulation of stalled early autophagosomal structures.{32504}
Brand:CaymanSKU:19905 -Available on backorder
MRT68921 is an inhibitor of ULK1 and ULK2 (IC50s = 2.9 and 1.1 nM, respectively).{32504} Through its effects on ULK1, MRT68921 blocks autophagy in cells, driving the accumulation of stalled early autophagosomal structures.{32504}
Brand:CaymanSKU:19905 -Available on backorder
MRT68921 is an inhibitor of ULK1 and ULK2 (IC50s = 2.9 and 1.1 nM, respectively).{32504} Through its effects on ULK1, MRT68921 blocks autophagy in cells, driving the accumulation of stalled early autophagosomal structures.{32504}
Brand:CaymanSKU:19905 -Available on backorder
MRTX-849 is a covalent inhibitor of K-RasG12C, a mutant form of K-Ras that accumulates in cancer cells.{52771} It binds to and stabilizes GDP-bound inactive K-RasG12C in an electrophoretic mobility shift assay when used at concentrations ranging from 2 to 15.6 nM. MRTX-849 (33-1,000 nM) reduces phosphorylation of the K-Ras targets ERK and S6 in MIA PaCa-2 cancer cells, which express K-RasG12C. In vivo, MRTX-849 (100 mg/kg) reduces tumor volume in 17 K-RasG12C-expressing lung, colon, pancreatic, cervical, and esophageal cancer mouse xenograft models but not wild-type K-Ras-expressing A549, HCT116, and H1299 mouse xenograft models.
Brand:CaymanSKU:31440 - 1 mgAvailable on backorder
MRTX-849 is a covalent inhibitor of K-RasG12C, a mutant form of K-Ras that accumulates in cancer cells.{52771} It binds to and stabilizes GDP-bound inactive K-RasG12C in an electrophoretic mobility shift assay when used at concentrations ranging from 2 to 15.6 nM. MRTX-849 (33-1,000 nM) reduces phosphorylation of the K-Ras targets ERK and S6 in MIA PaCa-2 cancer cells, which express K-RasG12C. In vivo, MRTX-849 (100 mg/kg) reduces tumor volume in 17 K-RasG12C-expressing lung, colon, pancreatic, cervical, and esophageal cancer mouse xenograft models but not wild-type K-Ras-expressing A549, HCT116, and H1299 mouse xenograft models.
Brand:CaymanSKU:31440 - 10 mgAvailable on backorder
MRTX-849 is a covalent inhibitor of K-RasG12C, a mutant form of K-Ras that accumulates in cancer cells.{52771} It binds to and stabilizes GDP-bound inactive K-RasG12C in an electrophoretic mobility shift assay when used at concentrations ranging from 2 to 15.6 nM. MRTX-849 (33-1,000 nM) reduces phosphorylation of the K-Ras targets ERK and S6 in MIA PaCa-2 cancer cells, which express K-RasG12C. In vivo, MRTX-849 (100 mg/kg) reduces tumor volume in 17 K-RasG12C-expressing lung, colon, pancreatic, cervical, and esophageal cancer mouse xenograft models but not wild-type K-Ras-expressing A549, HCT116, and H1299 mouse xenograft models.
Brand:CaymanSKU:31440 - 5 mgAvailable on backorder
MRX-2843 is an inhibitor of Mer and FMS-like tyrosine kinase 3 (FLT3; IC50s = 1.3 and 1 nM, respectively).{26933} It also inhibits Axl and Tyro3 (IC50s = 15 and 17 nM, respectively). MRX-2843 (10-300 nM) inhibits Mer phosphorylation in MOLM-14 and MV4-11 acute myeloid leukemia (AML) cells and reduces clonal expansion of Kasumi-1 AML cells (IC50 = 143.5 nM).{51170} In vivo, MRX-2843 increases survival in NOMO-1 and MOLM-14 AML mouse xenograft models when administered at doses of 65 and 50 mg/kg, respectively.
Brand:CaymanSKU:27923 - 1 mgAvailable on backorder
MRX-2843 is an inhibitor of Mer and FMS-like tyrosine kinase 3 (FLT3; IC50s = 1.3 and 1 nM, respectively).{26933} It also inhibits Axl and Tyro3 (IC50s = 15 and 17 nM, respectively). MRX-2843 (10-300 nM) inhibits Mer phosphorylation in MOLM-14 and MV4-11 acute myeloid leukemia (AML) cells and reduces clonal expansion of Kasumi-1 AML cells (IC50 = 143.5 nM).{51170} In vivo, MRX-2843 increases survival in NOMO-1 and MOLM-14 AML mouse xenograft models when administered at doses of 65 and 50 mg/kg, respectively.
Brand:CaymanSKU:27923 - 10 mgAvailable on backorder
MRX-2843 is an inhibitor of Mer and FMS-like tyrosine kinase 3 (FLT3; IC50s = 1.3 and 1 nM, respectively).{26933} It also inhibits Axl and Tyro3 (IC50s = 15 and 17 nM, respectively). MRX-2843 (10-300 nM) inhibits Mer phosphorylation in MOLM-14 and MV4-11 acute myeloid leukemia (AML) cells and reduces clonal expansion of Kasumi-1 AML cells (IC50 = 143.5 nM).{51170} In vivo, MRX-2843 increases survival in NOMO-1 and MOLM-14 AML mouse xenograft models when administered at doses of 65 and 50 mg/kg, respectively.
Brand:CaymanSKU:27923 - 5 mgAvailable on backorder
MS 245 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT6 (Ki = 2.3 nM for the human recombinant receptor).{42927} It is selective for 5-HT6 over 5-HT2A and 5-HT2C receptors (Kis = 130 and 23 nM, respectively), as well as 5-HT1A, 5-HT1B, 5-HT1E, 5-HT3, and 5-HT7 receptors (Kis = 720, 9,200, 4,220, 2,390, and 600 nM, respectively). MS 245 decreases cAMP production induced by 5-HT in HEK293 cells expressing 5-HT6 (pA2 = 8.88 nM). It potentiates drug discrimination induced by (+)-amphetamine, but has no effect on cocaine or (–)-nicotine (Item No. 20887) drug discrimination in rats when administered at a dose of 5 mg/kg.{42928,42929}
Brand:CaymanSKU:11936 - 1 mgAvailable on backorder
MS 245 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT6 (Ki = 2.3 nM for the human recombinant receptor).{42927} It is selective for 5-HT6 over 5-HT2A and 5-HT2C receptors (Kis = 130 and 23 nM, respectively), as well as 5-HT1A, 5-HT1B, 5-HT1E, 5-HT3, and 5-HT7 receptors (Kis = 720, 9,200, 4,220, 2,390, and 600 nM, respectively). MS 245 decreases cAMP production induced by 5-HT in HEK293 cells expressing 5-HT6 (pA2 = 8.88 nM). It potentiates drug discrimination induced by (+)-amphetamine, but has no effect on cocaine or (–)-nicotine (Item No. 20887) drug discrimination in rats when administered at a dose of 5 mg/kg.{42928,42929}
Brand:CaymanSKU:11936 - 10 mgAvailable on backorder
MS 245 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT6 (Ki = 2.3 nM for the human recombinant receptor).{42927} It is selective for 5-HT6 over 5-HT2A and 5-HT2C receptors (Kis = 130 and 23 nM, respectively), as well as 5-HT1A, 5-HT1B, 5-HT1E, 5-HT3, and 5-HT7 receptors (Kis = 720, 9,200, 4,220, 2,390, and 600 nM, respectively). MS 245 decreases cAMP production induced by 5-HT in HEK293 cells expressing 5-HT6 (pA2 = 8.88 nM). It potentiates drug discrimination induced by (+)-amphetamine, but has no effect on cocaine or (–)-nicotine (Item No. 20887) drug discrimination in rats when administered at a dose of 5 mg/kg.{42928,42929}
Brand:CaymanSKU:11936 - 5 mgAvailable on backorder