Chemicals
Showing 27001–27150 of 41137 results
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MK-0812 is a potent C-C chemokine receptor type 2 (CCR2) antagonist (IC50 = 5 nM for human CCR2).{34341} In a mouse model of antibody-induced arthritis, MK-0812 did not affect disease severity.{34340} Clinical trials for the use of MK-0812 for rheumatoid arthritis and multiple sclerosis were terminated early due to a lack of efficacy.{34342,34339}
Brand:CaymanSKU:21803 -Out of stock
MK-0812 is a potent C-C chemokine receptor type 2 (CCR2) antagonist (IC50 = 5 nM for human CCR2).{34341} In a mouse model of antibody-induced arthritis, MK-0812 did not affect disease severity.{34340} Clinical trials for the use of MK-0812 for rheumatoid arthritis and multiple sclerosis were terminated early due to a lack of efficacy.{34342,34339}
Brand:CaymanSKU:21803 -Out of stock
MK-0812 is a potent C-C chemokine receptor type 2 (CCR2) antagonist (IC50 = 5 nM for human CCR2).{34341} In a mouse model of antibody-induced arthritis, MK-0812 did not affect disease severity.{34340} Clinical trials for the use of MK-0812 for rheumatoid arthritis and multiple sclerosis were terminated early due to a lack of efficacy.{34342,34339}
Brand:CaymanSKU:21803 -Out of stock
MK-0941 is a glucokinase activator with EC50 values of 0.24 and 0.065 µM at low (2.5 mM) and high (10 mM) concentrations of glucose, respectively.{37711} It increases insulin secretion from isolated rat islets of Langerhans and glucose uptake by hepatocytes in vitro. MK-0941 reduces blood glucose levels in high-fat diet-fed db/db mice and in high-fat diet-fed mice with diabetes induced by streptozotocin (Item No. 13104).
Brand:CaymanSKU:25642 - 1 mgAvailable on backorder
MK-0941 is a glucokinase activator with EC50 values of 0.24 and 0.065 µM at low (2.5 mM) and high (10 mM) concentrations of glucose, respectively.{37711} It increases insulin secretion from isolated rat islets of Langerhans and glucose uptake by hepatocytes in vitro. MK-0941 reduces blood glucose levels in high-fat diet-fed db/db mice and in high-fat diet-fed mice with diabetes induced by streptozotocin (Item No. 13104).
Brand:CaymanSKU:25642 - 10 mgAvailable on backorder
MK-0941 is a glucokinase activator with EC50 values of 0.24 and 0.065 µM at low (2.5 mM) and high (10 mM) concentrations of glucose, respectively.{37711} It increases insulin secretion from isolated rat islets of Langerhans and glucose uptake by hepatocytes in vitro. MK-0941 reduces blood glucose levels in high-fat diet-fed db/db mice and in high-fat diet-fed mice with diabetes induced by streptozotocin (Item No. 13104).
Brand:CaymanSKU:25642 - 25 mgAvailable on backorder
MK-0941 is a glucokinase activator with EC50 values of 0.24 and 0.065 µM at low (2.5 mM) and high (10 mM) concentrations of glucose, respectively.{37711} It increases insulin secretion from isolated rat islets of Langerhans and glucose uptake by hepatocytes in vitro. MK-0941 reduces blood glucose levels in high-fat diet-fed db/db mice and in high-fat diet-fed mice with diabetes induced by streptozotocin (Item No. 13104).
Brand:CaymanSKU:25642 - 5 mgAvailable on backorder
MK-0974 is an orally bioavailable antagonist of the calcitonin gene-related peptide (CGRP) receptor complex (Ki = 0.77 μM), which is composed of the calcitonin receptor-like receptor (CRLR) and receptor activity modifying protein 1 (RAMP1).{38703} MK-0974 binds selectively to the human CGRP receptor complex, over the adrenomedullin receptor complexes, which are composed of CRLR and RAMP2 or RAMP3 (Kis = >100 and 29 μM, respectively, in HEK293 cells). MK-0974 also binds to rhesus, canine, and rat CGRP receptor complexes (Kis = 1.2, 1,204, and 1,192 nM, respectively). MK-0974 inhibits cAMP accumulation stimulated by CGRP (Item No. 24405) with an IC50 value of 2.2 nM in HEK293 cells expressing the CGRP receptor complex. Ex vivo, MK-0974 (5 μM) reduces CGRP-induced vasodilation in isolated human meningeal arteries.{38704} MK-0974 also inhibits vasodilation induced by topical application of capsaicin (Item No. 92350) in rhesus monkeys (EC50 = 127 nM).{38703}
Brand:CaymanSKU:23960 - 1 mgAvailable on backorder
MK-0974 is an orally bioavailable antagonist of the calcitonin gene-related peptide (CGRP) receptor complex (Ki = 0.77 μM), which is composed of the calcitonin receptor-like receptor (CRLR) and receptor activity modifying protein 1 (RAMP1).{38703} MK-0974 binds selectively to the human CGRP receptor complex, over the adrenomedullin receptor complexes, which are composed of CRLR and RAMP2 or RAMP3 (Kis = >100 and 29 μM, respectively, in HEK293 cells). MK-0974 also binds to rhesus, canine, and rat CGRP receptor complexes (Kis = 1.2, 1,204, and 1,192 nM, respectively). MK-0974 inhibits cAMP accumulation stimulated by CGRP (Item No. 24405) with an IC50 value of 2.2 nM in HEK293 cells expressing the CGRP receptor complex. Ex vivo, MK-0974 (5 μM) reduces CGRP-induced vasodilation in isolated human meningeal arteries.{38704} MK-0974 also inhibits vasodilation induced by topical application of capsaicin (Item No. 92350) in rhesus monkeys (EC50 = 127 nM).{38703}
Brand:CaymanSKU:23960 - 10 mgAvailable on backorder
MK-0974 is an orally bioavailable antagonist of the calcitonin gene-related peptide (CGRP) receptor complex (Ki = 0.77 μM), which is composed of the calcitonin receptor-like receptor (CRLR) and receptor activity modifying protein 1 (RAMP1).{38703} MK-0974 binds selectively to the human CGRP receptor complex, over the adrenomedullin receptor complexes, which are composed of CRLR and RAMP2 or RAMP3 (Kis = >100 and 29 μM, respectively, in HEK293 cells). MK-0974 also binds to rhesus, canine, and rat CGRP receptor complexes (Kis = 1.2, 1,204, and 1,192 nM, respectively). MK-0974 inhibits cAMP accumulation stimulated by CGRP (Item No. 24405) with an IC50 value of 2.2 nM in HEK293 cells expressing the CGRP receptor complex. Ex vivo, MK-0974 (5 μM) reduces CGRP-induced vasodilation in isolated human meningeal arteries.{38704} MK-0974 also inhibits vasodilation induced by topical application of capsaicin (Item No. 92350) in rhesus monkeys (EC50 = 127 nM).{38703}
Brand:CaymanSKU:23960 - 5 mgAvailable on backorder
MK-1064 is an orexin 2 receptor (OX2R) antagonist that is selective for OX2R over OX1R (IC50s = 18 and 1,789 nM, respectively).{39919} It decreases the amount of time spent in active wake and increases the time spent in rapid eye movement (REM) sleep and slow-wave sleep (SMS) in mice, rats, dogs, and rhesus monkeys when administered at doses of 100, 20, 1, and 10 mg/kg, respectively. MK-1064 (30 mg/kg) inhibits restraint stress-induced increases in plasma adrenocorticotropic hormone (ACTH) levels and struggle behavior, as well as decreases in body weight, in rats expressing the hM3Dq designer receptor exclusively activated by designer drugs (DREADD) activated by clozapine N-oxide (CNO; Item No. 16882) in orexin neurons.{39920}
Brand:CaymanSKU:20993 -Out of stock
MK-1064 is an orexin 2 receptor (OX2R) antagonist that is selective for OX2R over OX1R (IC50s = 18 and 1,789 nM, respectively).{39919} It decreases the amount of time spent in active wake and increases the time spent in rapid eye movement (REM) sleep and slow-wave sleep (SMS) in mice, rats, dogs, and rhesus monkeys when administered at doses of 100, 20, 1, and 10 mg/kg, respectively. MK-1064 (30 mg/kg) inhibits restraint stress-induced increases in plasma adrenocorticotropic hormone (ACTH) levels and struggle behavior, as well as decreases in body weight, in rats expressing the hM3Dq designer receptor exclusively activated by designer drugs (DREADD) activated by clozapine N-oxide (CNO; Item No. 16882) in orexin neurons.{39920}
Brand:CaymanSKU:20993 -Out of stock
MK-1064 is an orexin 2 receptor (OX2R) antagonist that is selective for OX2R over OX1R (IC50s = 18 and 1,789 nM, respectively).{39919} It decreases the amount of time spent in active wake and increases the time spent in rapid eye movement (REM) sleep and slow-wave sleep (SMS) in mice, rats, dogs, and rhesus monkeys when administered at doses of 100, 20, 1, and 10 mg/kg, respectively. MK-1064 (30 mg/kg) inhibits restraint stress-induced increases in plasma adrenocorticotropic hormone (ACTH) levels and struggle behavior, as well as decreases in body weight, in rats expressing the hM3Dq designer receptor exclusively activated by designer drugs (DREADD) activated by clozapine N-oxide (CNO; Item No. 16882) in orexin neurons.{39920}
Brand:CaymanSKU:20993 -Out of stock
MK-1064 is an orexin 2 receptor (OX2R) antagonist that is selective for OX2R over OX1R (IC50s = 18 and 1,789 nM, respectively).{39919} It decreases the amount of time spent in active wake and increases the time spent in rapid eye movement (REM) sleep and slow-wave sleep (SMS) in mice, rats, dogs, and rhesus monkeys when administered at doses of 100, 20, 1, and 10 mg/kg, respectively. MK-1064 (30 mg/kg) inhibits restraint stress-induced increases in plasma adrenocorticotropic hormone (ACTH) levels and struggle behavior, as well as decreases in body weight, in rats expressing the hM3Dq designer receptor exclusively activated by designer drugs (DREADD) activated by clozapine N-oxide (CNO; Item No. 16882) in orexin neurons.{39920}
Brand:CaymanSKU:20993 -Out of stock
MK-1775 is an inhibitor of the checkpoint kinase Wee1 (IC50 = 5.2 nM).{33534} It has been shown to inhibit the phosphorylation of Cdc2 at tryosine-15, which abrogates the G2 DNA damage checkpoint.{33534} In p53-deficient tumors that rely solely on the G2 checkpoint upon DNA damage, MK-1775, in combination with DNA-damaging chemotherapeutic agents, is reported to induce apoptosis in vitro and potentiate the inhibition of tumor growth in vivo.{33534}
Brand:CaymanSKU:21266 -Out of stock
MK-1775 is an inhibitor of the checkpoint kinase Wee1 (IC50 = 5.2 nM).{33534} It has been shown to inhibit the phosphorylation of Cdc2 at tryosine-15, which abrogates the G2 DNA damage checkpoint.{33534} In p53-deficient tumors that rely solely on the G2 checkpoint upon DNA damage, MK-1775, in combination with DNA-damaging chemotherapeutic agents, is reported to induce apoptosis in vitro and potentiate the inhibition of tumor growth in vivo.{33534}
Brand:CaymanSKU:21266 -Out of stock
MK-1775 is an inhibitor of the checkpoint kinase Wee1 (IC50 = 5.2 nM).{33534} It has been shown to inhibit the phosphorylation of Cdc2 at tryosine-15, which abrogates the G2 DNA damage checkpoint.{33534} In p53-deficient tumors that rely solely on the G2 checkpoint upon DNA damage, MK-1775, in combination with DNA-damaging chemotherapeutic agents, is reported to induce apoptosis in vitro and potentiate the inhibition of tumor growth in vivo.{33534}
Brand:CaymanSKU:21266 -Out of stock
MK-1775 is an inhibitor of the checkpoint kinase Wee1 (IC50 = 5.2 nM).{33534} It has been shown to inhibit the phosphorylation of Cdc2 at tryosine-15, which abrogates the G2 DNA damage checkpoint.{33534} In p53-deficient tumors that rely solely on the G2 checkpoint upon DNA damage, MK-1775, in combination with DNA-damaging chemotherapeutic agents, is reported to induce apoptosis in vitro and potentiate the inhibition of tumor growth in vivo.{33534}
Brand:CaymanSKU:21266 -Out of stock
Three related forms of the kinase Akt (1, 2, 3, also known as protein kinase B isoforms PKBα, β, γ) modulate cell proliferation, metabolism, and survival as well as angiogenesis.{15560,16917} MK-2206 is an orally active, allosteric Akt inhibitor that is equally potent toward purified human recombinant Akt1 and Akt2 (IC50s = 5 and 12 nM, respectively) and approximately 5-fold less potent against human Akt3 (IC50 = 65 nM).{24817} In combination with other anticancer agents including topoisomerase inhibitors, antimetabolites, antimicrotubule agents, DNA cross-linkers or growth factor inhibitors, MK-2206 has been shown to synergistically inhibit cell proliferation of human cancer cell lines.{24817} At 5 μM, MK-2206 significantly enhances apoptosis in hematopoietic cells treated with chemotherapeutics.{24816}
Brand:CaymanSKU:11593 - 1 mgAvailable on backorder
Three related forms of the kinase Akt (1, 2, 3, also known as protein kinase B isoforms PKBα, β, γ) modulate cell proliferation, metabolism, and survival as well as angiogenesis.{15560,16917} MK-2206 is an orally active, allosteric Akt inhibitor that is equally potent toward purified human recombinant Akt1 and Akt2 (IC50s = 5 and 12 nM, respectively) and approximately 5-fold less potent against human Akt3 (IC50 = 65 nM).{24817} In combination with other anticancer agents including topoisomerase inhibitors, antimetabolites, antimicrotubule agents, DNA cross-linkers or growth factor inhibitors, MK-2206 has been shown to synergistically inhibit cell proliferation of human cancer cell lines.{24817} At 5 μM, MK-2206 significantly enhances apoptosis in hematopoietic cells treated with chemotherapeutics.{24816}
Brand:CaymanSKU:11593 - 10 mgAvailable on backorder
Three related forms of the kinase Akt (1, 2, 3, also known as protein kinase B isoforms PKBα, β, γ) modulate cell proliferation, metabolism, and survival as well as angiogenesis.{15560,16917} MK-2206 is an orally active, allosteric Akt inhibitor that is equally potent toward purified human recombinant Akt1 and Akt2 (IC50s = 5 and 12 nM, respectively) and approximately 5-fold less potent against human Akt3 (IC50 = 65 nM).{24817} In combination with other anticancer agents including topoisomerase inhibitors, antimetabolites, antimicrotubule agents, DNA cross-linkers or growth factor inhibitors, MK-2206 has been shown to synergistically inhibit cell proliferation of human cancer cell lines.{24817} At 5 μM, MK-2206 significantly enhances apoptosis in hematopoietic cells treated with chemotherapeutics.{24816}
Brand:CaymanSKU:11593 - 25 mgAvailable on backorder
Three related forms of the kinase Akt (1, 2, 3, also known as protein kinase B isoforms PKBα, β, γ) modulate cell proliferation, metabolism, and survival as well as angiogenesis.{15560,16917} MK-2206 is an orally active, allosteric Akt inhibitor that is equally potent toward purified human recombinant Akt1 and Akt2 (IC50s = 5 and 12 nM, respectively) and approximately 5-fold less potent against human Akt3 (IC50 = 65 nM).{24817} In combination with other anticancer agents including topoisomerase inhibitors, antimetabolites, antimicrotubule agents, DNA cross-linkers or growth factor inhibitors, MK-2206 has been shown to synergistically inhibit cell proliferation of human cancer cell lines.{24817} At 5 μM, MK-2206 significantly enhances apoptosis in hematopoietic cells treated with chemotherapeutics.{24816}
Brand:CaymanSKU:11593 - 5 mgAvailable on backorder
MK-3102 is a potent, reversible, and competitive inhibitor of dipeptidyl peptidase 4 (DPP-4; IC50 = 1.6 nM; Ki = 0.8 nM).{37137} It is selective for DPP-4 over 168 proteases, ion channels, and enzymes with IC50 values greater than 10 µM in all assays. MK-3102 significantly reduces blood glucose levels in a dose-dependent manner in vivo in rats. It also has a long half-life (11 and 22 hours in rat and dog, respectively) making it suitable for once weekly dosing. Clinical trials demonstrate that formulations containing MK-3102 reduce plasma glucose and HbA1c in patients with type 2 diabetes mellitus (T2DM).
Brand:CaymanSKU:21454 -Out of stock
MK-3102 is a potent, reversible, and competitive inhibitor of dipeptidyl peptidase 4 (DPP-4; IC50 = 1.6 nM; Ki = 0.8 nM).{37137} It is selective for DPP-4 over 168 proteases, ion channels, and enzymes with IC50 values greater than 10 µM in all assays. MK-3102 significantly reduces blood glucose levels in a dose-dependent manner in vivo in rats. It also has a long half-life (11 and 22 hours in rat and dog, respectively) making it suitable for once weekly dosing. Clinical trials demonstrate that formulations containing MK-3102 reduce plasma glucose and HbA1c in patients with type 2 diabetes mellitus (T2DM).
Brand:CaymanSKU:21454 -Out of stock
MK-3102 is a potent, reversible, and competitive inhibitor of dipeptidyl peptidase 4 (DPP-4; IC50 = 1.6 nM; Ki = 0.8 nM).{37137} It is selective for DPP-4 over 168 proteases, ion channels, and enzymes with IC50 values greater than 10 µM in all assays. MK-3102 significantly reduces blood glucose levels in a dose-dependent manner in vivo in rats. It also has a long half-life (11 and 22 hours in rat and dog, respectively) making it suitable for once weekly dosing. Clinical trials demonstrate that formulations containing MK-3102 reduce plasma glucose and HbA1c in patients with type 2 diabetes mellitus (T2DM).
Brand:CaymanSKU:21454 -Out of stock
MK-3102 is a potent, reversible, and competitive inhibitor of dipeptidyl peptidase 4 (DPP-4; IC50 = 1.6 nM; Ki = 0.8 nM).{37137} It is selective for DPP-4 over 168 proteases, ion channels, and enzymes with IC50 values greater than 10 µM in all assays. MK-3102 significantly reduces blood glucose levels in a dose-dependent manner in vivo in rats. It also has a long half-life (11 and 22 hours in rat and dog, respectively) making it suitable for once weekly dosing. Clinical trials demonstrate that formulations containing MK-3102 reduce plasma glucose and HbA1c in patients with type 2 diabetes mellitus (T2DM).
Brand:CaymanSKU:21454 -Out of stock
MK-3903 is an activator of AMP-activated protein kinase (AMPK; EC50 = 9 nM).{40507} It is selective for AMPK over a kinase panel at 10 µM, as well as the cytochrome P450 (CYP) isoforms CYP3A4 and CYP2D6 (IC50s = >50 µM for both) and the pregnane X receptor (PXR; EC50 = >30 µM). MK-3903 (30 mg/kg) increases muscle and liver levels of phosphorylated ACC, an AMPK substrate, and reduces insulin resistance in diet-induced obese (DIO) mice. It inhibits hepatic fatty acid synthesis in db/db mice when administered at doses ranging from 3 to 30 mg/kg.
Brand:CaymanSKU:29661 - 1 mgAvailable on backorder
MK-3903 is an activator of AMP-activated protein kinase (AMPK; EC50 = 9 nM).{40507} It is selective for AMPK over a kinase panel at 10 µM, as well as the cytochrome P450 (CYP) isoforms CYP3A4 and CYP2D6 (IC50s = >50 µM for both) and the pregnane X receptor (PXR; EC50 = >30 µM). MK-3903 (30 mg/kg) increases muscle and liver levels of phosphorylated ACC, an AMPK substrate, and reduces insulin resistance in diet-induced obese (DIO) mice. It inhibits hepatic fatty acid synthesis in db/db mice when administered at doses ranging from 3 to 30 mg/kg.
Brand:CaymanSKU:29661 - 10 mgAvailable on backorder
MK-3903 is an activator of AMP-activated protein kinase (AMPK; EC50 = 9 nM).{40507} It is selective for AMPK over a kinase panel at 10 µM, as well as the cytochrome P450 (CYP) isoforms CYP3A4 and CYP2D6 (IC50s = >50 µM for both) and the pregnane X receptor (PXR; EC50 = >30 µM). MK-3903 (30 mg/kg) increases muscle and liver levels of phosphorylated ACC, an AMPK substrate, and reduces insulin resistance in diet-induced obese (DIO) mice. It inhibits hepatic fatty acid synthesis in db/db mice when administered at doses ranging from 3 to 30 mg/kg.
Brand:CaymanSKU:29661 - 25 mgAvailable on backorder
MK-3903 is an activator of AMP-activated protein kinase (AMPK; EC50 = 9 nM).{40507} It is selective for AMPK over a kinase panel at 10 µM, as well as the cytochrome P450 (CYP) isoforms CYP3A4 and CYP2D6 (IC50s = >50 µM for both) and the pregnane X receptor (PXR; EC50 = >30 µM). MK-3903 (30 mg/kg) increases muscle and liver levels of phosphorylated ACC, an AMPK substrate, and reduces insulin resistance in diet-induced obese (DIO) mice. It inhibits hepatic fatty acid synthesis in db/db mice when administered at doses ranging from 3 to 30 mg/kg.
Brand:CaymanSKU:29661 - 5 mgAvailable on backorder
MK-4101 is a Smoothened (Smo) receptor antagonist.{48932} It binds to human recombinant Smo expressed in HEK293T cells (IC50 = 1.1 µM) and inhibits Gli1-mediated hedgehog signaling in a reporter assay (IC50 = 1.5 µM). It is also an inhibitor of 11β-hydroxy steroid dehydrogenase-1. MK-4101 (40 and 80 mg/kg per day) reduces tumor growth in a murine medulloblastoma mouse allograft model, induces tumor regression when administered at a dose of 80 mg/kg twice per day, and reduces expression of the hedgehog pathway-associated transcription factor Gli1 in tumor tissue.
Brand:CaymanSKU:29159 - 1 mgAvailable on backorder
MK-4101 is a Smoothened (Smo) receptor antagonist.{48932} It binds to human recombinant Smo expressed in HEK293T cells (IC50 = 1.1 µM) and inhibits Gli1-mediated hedgehog signaling in a reporter assay (IC50 = 1.5 µM). It is also an inhibitor of 11β-hydroxy steroid dehydrogenase-1. MK-4101 (40 and 80 mg/kg per day) reduces tumor growth in a murine medulloblastoma mouse allograft model, induces tumor regression when administered at a dose of 80 mg/kg twice per day, and reduces expression of the hedgehog pathway-associated transcription factor Gli1 in tumor tissue.
Brand:CaymanSKU:29159 - 10 mgAvailable on backorder
MK-4101 is a Smoothened (Smo) receptor antagonist.{48932} It binds to human recombinant Smo expressed in HEK293T cells (IC50 = 1.1 µM) and inhibits Gli1-mediated hedgehog signaling in a reporter assay (IC50 = 1.5 µM). It is also an inhibitor of 11β-hydroxy steroid dehydrogenase-1. MK-4101 (40 and 80 mg/kg per day) reduces tumor growth in a murine medulloblastoma mouse allograft model, induces tumor regression when administered at a dose of 80 mg/kg twice per day, and reduces expression of the hedgehog pathway-associated transcription factor Gli1 in tumor tissue.
Brand:CaymanSKU:29159 - 25 mgAvailable on backorder
MK-4101 is a Smoothened (Smo) receptor antagonist.{48932} It binds to human recombinant Smo expressed in HEK293T cells (IC50 = 1.1 µM) and inhibits Gli1-mediated hedgehog signaling in a reporter assay (IC50 = 1.5 µM). It is also an inhibitor of 11β-hydroxy steroid dehydrogenase-1. MK-4101 (40 and 80 mg/kg per day) reduces tumor growth in a murine medulloblastoma mouse allograft model, induces tumor regression when administered at a dose of 80 mg/kg twice per day, and reduces expression of the hedgehog pathway-associated transcription factor Gli1 in tumor tissue.
Brand:CaymanSKU:29159 - 5 mgAvailable on backorder
MK-4827 is an orally bioavailable inhibitor of poly(ADP-ribose) polymerase 1 (PARP1) and PARP2 (IC50s = 3.8 and 2.1 nM, respectively).{34138} It inhibits the proliferation of cancer cells carrying the breast cancer mutations BRCA1 and BRCA2 in vitro (IC50 values range from 10-100 nM) and has efficacy alone against a xenograft of BRCA1-deficient cancer in mice.{34138,20554} MK-4827 sensitizes human lung and breast cancer xenografts to radiation in mice.{34140} Formulations containing MK-4827 are effective against ovarian cancer, particularly in platinum-sensitive, recurrent ovarian cancer.{34139}
Brand:CaymanSKU:20842 -Out of stock
MK-4827 is an orally bioavailable inhibitor of poly(ADP-ribose) polymerase 1 (PARP1) and PARP2 (IC50s = 3.8 and 2.1 nM, respectively).{34138} It inhibits the proliferation of cancer cells carrying the breast cancer mutations BRCA1 and BRCA2 in vitro (IC50 values range from 10-100 nM) and has efficacy alone against a xenograft of BRCA1-deficient cancer in mice.{34138,20554} MK-4827 sensitizes human lung and breast cancer xenografts to radiation in mice.{34140} Formulations containing MK-4827 are effective against ovarian cancer, particularly in platinum-sensitive, recurrent ovarian cancer.{34139}
Brand:CaymanSKU:20842 -Out of stock
MK-4827 is an orally bioavailable inhibitor of poly(ADP-ribose) polymerase 1 (PARP1) and PARP2 (IC50s = 3.8 and 2.1 nM, respectively).{34138} It inhibits the proliferation of cancer cells carrying the breast cancer mutations BRCA1 and BRCA2 in vitro (IC50 values range from 10-100 nM) and has efficacy alone against a xenograft of BRCA1-deficient cancer in mice.{34138,20554} MK-4827 sensitizes human lung and breast cancer xenografts to radiation in mice.{34140} Formulations containing MK-4827 are effective against ovarian cancer, particularly in platinum-sensitive, recurrent ovarian cancer.{34139}
Brand:CaymanSKU:20842 -Out of stock
MK-4827 is an orally bioavailable inhibitor of poly(ADP-ribose) polymerase 1 (PARP1) and PARP2 (IC50s = 3.8 and 2.1 nM, respectively).{34138} It inhibits the proliferation of cancer cells carrying the breast cancer mutations BRCA1 and BRCA2 in vitro (IC50 values range from 10-100 nM) and has efficacy alone against a xenograft of BRCA1-deficient cancer in mice.{34138,20554} MK-4827 sensitizes human lung and breast cancer xenografts to radiation in mice.{34140} Formulations containing MK-4827 are effective against ovarian cancer, particularly in platinum-sensitive, recurrent ovarian cancer.{34139}
Brand:CaymanSKU:20842 -Out of stock
The Aurora kinases are a family of serine/threonine kinases that are key regulators of mitosis and cytokinesis. MK-5108 is a potent inhibitor of Aurora A (IC50 = 0.064 nM).{30910} It less potently inhibits Aurora B and Aurora C (IC50s =14 and 12 nM, respectively). MK-5108 blocks cell cycle progression and induces apoptosis in a diverse range of human tumor types.{30910,30911} It is effective in vivo, inhibiting the growth of xenograft tumors in mice.{30910}
Brand:CaymanSKU:-Available on backorder
The Aurora kinases are a family of serine/threonine kinases that are key regulators of mitosis and cytokinesis. MK-5108 is a potent inhibitor of Aurora A (IC50 = 0.064 nM).{30910} It less potently inhibits Aurora B and Aurora C (IC50s =14 and 12 nM, respectively). MK-5108 blocks cell cycle progression and induces apoptosis in a diverse range of human tumor types.{30910,30911} It is effective in vivo, inhibiting the growth of xenograft tumors in mice.{30910}
Brand:CaymanSKU:-Available on backorder
The Aurora kinases are a family of serine/threonine kinases that are key regulators of mitosis and cytokinesis. MK-5108 is a potent inhibitor of Aurora A (IC50 = 0.064 nM).{30910} It less potently inhibits Aurora B and Aurora C (IC50s =14 and 12 nM, respectively). MK-5108 blocks cell cycle progression and induces apoptosis in a diverse range of human tumor types.{30910,30911} It is effective in vivo, inhibiting the growth of xenograft tumors in mice.{30910}
Brand:CaymanSKU:-Available on backorder
The cysteinyl leukotrienes (CysLTs), leukotriene (LTC4), LTD4, and LTE4, mediate their actions through two distinct G protein-coupled receptors. LTD4 is the preferred ligand for the CysLT1 receptor, whereas LTC4 and LTD4 bind with approximately equal affinity to the CysLT2 receptor.{7174,8519} MK-571 is a selective, orally active CysLT1 receptor antagonist.{1501} It blocks the binding of LTD4, but not LTC4, to human and guinea pig lung membranes with Ki values of 0.22 nM and 2.1 nM, respectively, which is indicative of CysLT1 receptor-mediated activity in these preparations.{1501} MK-571 effectively blocks LTD4 activation of recombinant human and murine CysLT1 receptors{7174,10167} but is ineffective at blocking LTC4 or LTD4 activation of the recombinant human or murine CysLT2 receptors.{8519,10167}
Brand:CaymanSKU:10029 - 1 mgAvailable on backorder
The cysteinyl leukotrienes (CysLTs), leukotriene (LTC4), LTD4, and LTE4, mediate their actions through two distinct G protein-coupled receptors. LTD4 is the preferred ligand for the CysLT1 receptor, whereas LTC4 and LTD4 bind with approximately equal affinity to the CysLT2 receptor.{7174,8519} MK-571 is a selective, orally active CysLT1 receptor antagonist.{1501} It blocks the binding of LTD4, but not LTC4, to human and guinea pig lung membranes with Ki values of 0.22 nM and 2.1 nM, respectively, which is indicative of CysLT1 receptor-mediated activity in these preparations.{1501} MK-571 effectively blocks LTD4 activation of recombinant human and murine CysLT1 receptors{7174,10167} but is ineffective at blocking LTC4 or LTD4 activation of the recombinant human or murine CysLT2 receptors.{8519,10167}
Brand:CaymanSKU:10029 - 10 mgAvailable on backorder
The cysteinyl leukotrienes (CysLTs), leukotriene (LTC4), LTD4, and LTE4, mediate their actions through two distinct G protein-coupled receptors. LTD4 is the preferred ligand for the CysLT1 receptor, whereas LTC4 and LTD4 bind with approximately equal affinity to the CysLT2 receptor.{7174,8519} MK-571 is a selective, orally active CysLT1 receptor antagonist.{1501} It blocks the binding of LTD4, but not LTC4, to human and guinea pig lung membranes with Ki values of 0.22 nM and 2.1 nM, respectively, which is indicative of CysLT1 receptor-mediated activity in these preparations.{1501} MK-571 effectively blocks LTD4 activation of recombinant human and murine CysLT1 receptors{7174,10167} but is ineffective at blocking LTC4 or LTD4 activation of the recombinant human or murine CysLT2 receptors.{8519,10167}
Brand:CaymanSKU:10029 - 5 mgAvailable on backorder
The cysteinyl leukotrienes (CysLTs), leukotriene (LTC4), LTD4, and LTE4, mediate their actions through two distinct G protein-coupled receptors. LTD4 is the preferred ligand for the CysLT1 receptor, whereas LTC4 and LTD4 bind with approximately equal affinity to the CysLT2 receptor.{7174,8519} MK-571 is a selective, orally active CysLT1 receptor antagonist.{1501} It blocks the binding of LTD4, but not LTC4, to human and guinea pig lung membranes with Ki values of 0.22 nM and 2.1 nM, respectively, which is indicative of CysLT1 receptor-mediated activity in these preparations.{1501} MK-571 effectively blocks LTD4 activation of recombinant human and murine CysLT1 receptors{7174,10167} but is ineffective at blocking LTC4 or LTD4 activation of the recombinant human or murine CysLT2 receptors.{8519,10167}
Brand:CaymanSKU:10029 - 50 mgAvailable on backorder
The cysteinyl leukotrienes (CysLTs), LTC4, LTD4, and LTE4, mediate their actions through two distinct G protein-coupled receptors. LTD4 is the preferred ligand for the cysLT1 receptor,{7174} whereas LTC4 and LTD4 bind with approximately equal affinity to the CysLT2 receptor.{8519} MK-571 is a selective, orally active CysLT1 receptor antagonist.{1501} It blocks the binding of LTD4, but not LTC4, to human and guinea pig lung membranes with Ki values of 0.22 nM and 2.1 nM, respectively, which is indicative of CysLT1 receptor-mediated activity in these preparations.{1501} MK-571 effectively blocks LTD4 activation of recombinant human and mouse CysLT1 receptors{7174,10167} but is ineffective at blocking LTC4 or LTD4 activation of the recombinant human or mouse CysLT2 receptors.{8519,10167}
Brand:CaymanSKU:70720 - 1 mgAvailable on backorder
The cysteinyl leukotrienes (CysLTs), LTC4, LTD4, and LTE4, mediate their actions through two distinct G protein-coupled receptors. LTD4 is the preferred ligand for the cysLT1 receptor,{7174} whereas LTC4 and LTD4 bind with approximately equal affinity to the CysLT2 receptor.{8519} MK-571 is a selective, orally active CysLT1 receptor antagonist.{1501} It blocks the binding of LTD4, but not LTC4, to human and guinea pig lung membranes with Ki values of 0.22 nM and 2.1 nM, respectively, which is indicative of CysLT1 receptor-mediated activity in these preparations.{1501} MK-571 effectively blocks LTD4 activation of recombinant human and mouse CysLT1 receptors{7174,10167} but is ineffective at blocking LTC4 or LTD4 activation of the recombinant human or mouse CysLT2 receptors.{8519,10167}
Brand:CaymanSKU:70720 - 10 mgAvailable on backorder
The cysteinyl leukotrienes (CysLTs), LTC4, LTD4, and LTE4, mediate their actions through two distinct G protein-coupled receptors. LTD4 is the preferred ligand for the cysLT1 receptor,{7174} whereas LTC4 and LTD4 bind with approximately equal affinity to the CysLT2 receptor.{8519} MK-571 is a selective, orally active CysLT1 receptor antagonist.{1501} It blocks the binding of LTD4, but not LTC4, to human and guinea pig lung membranes with Ki values of 0.22 nM and 2.1 nM, respectively, which is indicative of CysLT1 receptor-mediated activity in these preparations.{1501} MK-571 effectively blocks LTD4 activation of recombinant human and mouse CysLT1 receptors{7174,10167} but is ineffective at blocking LTC4 or LTD4 activation of the recombinant human or mouse CysLT2 receptors.{8519,10167}
Brand:CaymanSKU:70720 - 5 mgAvailable on backorder
The cysteinyl leukotrienes (CysLTs), LTC4, LTD4, and LTE4, mediate their actions through two distinct G protein-coupled receptors. LTD4 is the preferred ligand for the cysLT1 receptor,{7174} whereas LTC4 and LTD4 bind with approximately equal affinity to the CysLT2 receptor.{8519} MK-571 is a selective, orally active CysLT1 receptor antagonist.{1501} It blocks the binding of LTD4, but not LTC4, to human and guinea pig lung membranes with Ki values of 0.22 nM and 2.1 nM, respectively, which is indicative of CysLT1 receptor-mediated activity in these preparations.{1501} MK-571 effectively blocks LTD4 activation of recombinant human and mouse CysLT1 receptors{7174,10167} but is ineffective at blocking LTC4 or LTD4 activation of the recombinant human or mouse CysLT2 receptors.{8519,10167}
Brand:CaymanSKU:70720 - 50 mgAvailable on backorder
MK-7655 is a β-lactamase inhibitor that inhibits hydrolysis of nitrocefin by KPC-2 β-lactamase from K. pneumoniae and AmpC β-lactamase from P. aeruginosa (IC50s = 210 and 465 nM, respectively).{41428} It restores imipenem-susceptibility in imipenem-resistant K. pneumoniae and P. aeruginosa when used at concentrations of 12.5 and 4.7 μM, respectively. MK-7655 also restores imipenem sensitivity to resistant clinical isolates of P. aeruginosa and K. pneumoniae (MIC50s = 0.25-2 and 8-16 μM in the presence and absence of MK-7655, respectively), but not A. baumannii.{41429} In vivo, MK-7655 (48.9 mg/kg per day) produces a bacteriostatic effect in mouse thigh models of K. pneumoniae and P. aeruginosa infection when administered with imipenem (Item No. 16039) and cilastatin (Item No. 23511).{41430}
Brand:CaymanSKU:23890 - 1 mgAvailable on backorder
MK-7655 is a β-lactamase inhibitor that inhibits hydrolysis of nitrocefin by KPC-2 β-lactamase from K. pneumoniae and AmpC β-lactamase from P. aeruginosa (IC50s = 210 and 465 nM, respectively).{41428} It restores imipenem-susceptibility in imipenem-resistant K. pneumoniae and P. aeruginosa when used at concentrations of 12.5 and 4.7 μM, respectively. MK-7655 also restores imipenem sensitivity to resistant clinical isolates of P. aeruginosa and K. pneumoniae (MIC50s = 0.25-2 and 8-16 μM in the presence and absence of MK-7655, respectively), but not A. baumannii.{41429} In vivo, MK-7655 (48.9 mg/kg per day) produces a bacteriostatic effect in mouse thigh models of K. pneumoniae and P. aeruginosa infection when administered with imipenem (Item No. 16039) and cilastatin (Item No. 23511).{41430}
Brand:CaymanSKU:23890 - 10 mgAvailable on backorder
MK-7655 is a β-lactamase inhibitor that inhibits hydrolysis of nitrocefin by KPC-2 β-lactamase from K. pneumoniae and AmpC β-lactamase from P. aeruginosa (IC50s = 210 and 465 nM, respectively).{41428} It restores imipenem-susceptibility in imipenem-resistant K. pneumoniae and P. aeruginosa when used at concentrations of 12.5 and 4.7 μM, respectively. MK-7655 also restores imipenem sensitivity to resistant clinical isolates of P. aeruginosa and K. pneumoniae (MIC50s = 0.25-2 and 8-16 μM in the presence and absence of MK-7655, respectively), but not A. baumannii.{41429} In vivo, MK-7655 (48.9 mg/kg per day) produces a bacteriostatic effect in mouse thigh models of K. pneumoniae and P. aeruginosa infection when administered with imipenem (Item No. 16039) and cilastatin (Item No. 23511).{41430}
Brand:CaymanSKU:23890 - 25 mgAvailable on backorder
MK-7655 is a β-lactamase inhibitor that inhibits hydrolysis of nitrocefin by KPC-2 β-lactamase from K. pneumoniae and AmpC β-lactamase from P. aeruginosa (IC50s = 210 and 465 nM, respectively).{41428} It restores imipenem-susceptibility in imipenem-resistant K. pneumoniae and P. aeruginosa when used at concentrations of 12.5 and 4.7 μM, respectively. MK-7655 also restores imipenem sensitivity to resistant clinical isolates of P. aeruginosa and K. pneumoniae (MIC50s = 0.25-2 and 8-16 μM in the presence and absence of MK-7655, respectively), but not A. baumannii.{41429} In vivo, MK-7655 (48.9 mg/kg per day) produces a bacteriostatic effect in mouse thigh models of K. pneumoniae and P. aeruginosa infection when administered with imipenem (Item No. 16039) and cilastatin (Item No. 23511).{41430}
Brand:CaymanSKU:23890 - 5 mgAvailable on backorder
MK-8245 is a liver-targeted inhibitor of stearoyl-CoA desaturase (SCD; IC50s = 3, 3, and 1 nM for rat, mouse, and human SCD1, respectively).{53163} It is selective for SCD1 over Δ5- and Δ6-desaturases (IC50s = >100,000 nM). MK-8245 (20-60 mg/kg) reduces the hepatic, but not Harderian gland, ratio of oleic acid to stearic acid, a marker of chronic SCD activity, and blood glucose levels, without inducing the formation of skin lesions or eye squinting behavior, in a mouse model of high-fat diet-induced obesity. It also inhibits hepatitis C virus (HCV) replication without inducing cytotoxicity in LucNeo2 cells (IC50 = 39.8 nM).{53164}
Brand:CaymanSKU:29421 - 1 mgAvailable on backorder
MK-8245 is a liver-targeted inhibitor of stearoyl-CoA desaturase (SCD; IC50s = 3, 3, and 1 nM for rat, mouse, and human SCD1, respectively).{53163} It is selective for SCD1 over Δ5- and Δ6-desaturases (IC50s = >100,000 nM). MK-8245 (20-60 mg/kg) reduces the hepatic, but not Harderian gland, ratio of oleic acid to stearic acid, a marker of chronic SCD activity, and blood glucose levels, without inducing the formation of skin lesions or eye squinting behavior, in a mouse model of high-fat diet-induced obesity. It also inhibits hepatitis C virus (HCV) replication without inducing cytotoxicity in LucNeo2 cells (IC50 = 39.8 nM).{53164}
Brand:CaymanSKU:29421 - 10 mgAvailable on backorder
MK-8245 is a liver-targeted inhibitor of stearoyl-CoA desaturase (SCD; IC50s = 3, 3, and 1 nM for rat, mouse, and human SCD1, respectively).{53163} It is selective for SCD1 over Δ5- and Δ6-desaturases (IC50s = >100,000 nM). MK-8245 (20-60 mg/kg) reduces the hepatic, but not Harderian gland, ratio of oleic acid to stearic acid, a marker of chronic SCD activity, and blood glucose levels, without inducing the formation of skin lesions or eye squinting behavior, in a mouse model of high-fat diet-induced obesity. It also inhibits hepatitis C virus (HCV) replication without inducing cytotoxicity in LucNeo2 cells (IC50 = 39.8 nM).{53164}
Brand:CaymanSKU:29421 - 25 mgAvailable on backorder
MK-8245 is a liver-targeted inhibitor of stearoyl-CoA desaturase (SCD; IC50s = 3, 3, and 1 nM for rat, mouse, and human SCD1, respectively).{53163} It is selective for SCD1 over Δ5- and Δ6-desaturases (IC50s = >100,000 nM). MK-8245 (20-60 mg/kg) reduces the hepatic, but not Harderian gland, ratio of oleic acid to stearic acid, a marker of chronic SCD activity, and blood glucose levels, without inducing the formation of skin lesions or eye squinting behavior, in a mouse model of high-fat diet-induced obesity. It also inhibits hepatitis C virus (HCV) replication without inducing cytotoxicity in LucNeo2 cells (IC50 = 39.8 nM).{53164}
Brand:CaymanSKU:29421 - 5 mgAvailable on backorder
MK-8669 is a rapamycin analog that selectively inhibits mTOR (IC50 = 0.2 nM). Like rapamycin, MK-8669 binds FKBP12 to form a complex that associates with the FKBP-rapamycin binding domain on mTOR and allosterically inhibits mTORC1 kinase activity.{27495} MK-8669 is more water soluble than rapamycin and is amenable to oral or intravenous administration. Formulations containing rapalogs, including MK-8669, have promise against a subset of cancers, including advanced kidney cancer.{27495} MK-8669 is also being examined for effectiveness against cancers when used in combination with other chemotherapeutic compounds.{33801,33802,33803}
Brand:CaymanSKU:10543 - 1 mgAvailable on backorder
MK-8669 is a rapamycin analog that selectively inhibits mTOR (IC50 = 0.2 nM). Like rapamycin, MK-8669 binds FKBP12 to form a complex that associates with the FKBP-rapamycin binding domain on mTOR and allosterically inhibits mTORC1 kinase activity.{27495} MK-8669 is more water soluble than rapamycin and is amenable to oral or intravenous administration. Formulations containing rapalogs, including MK-8669, have promise against a subset of cancers, including advanced kidney cancer.{27495} MK-8669 is also being examined for effectiveness against cancers when used in combination with other chemotherapeutic compounds.{33801,33802,33803}
Brand:CaymanSKU:10543 - 10 mgAvailable on backorder
MK-8669 is a rapamycin analog that selectively inhibits mTOR (IC50 = 0.2 nM). Like rapamycin, MK-8669 binds FKBP12 to form a complex that associates with the FKBP-rapamycin binding domain on mTOR and allosterically inhibits mTORC1 kinase activity.{27495} MK-8669 is more water soluble than rapamycin and is amenable to oral or intravenous administration. Formulations containing rapalogs, including MK-8669, have promise against a subset of cancers, including advanced kidney cancer.{27495} MK-8669 is also being examined for effectiveness against cancers when used in combination with other chemotherapeutic compounds.{33801,33802,33803}
Brand:CaymanSKU:10543 - 5 mgAvailable on backorder
MK-8745 is an Aurora A kinase inhibitor (IC50 = 0.6 nM) that is selective for Aurora A over Aurora B kinase (IC50 = 280 nM).{49031} It induces cell cycle arrest at the G2/M phase in non-Hodgkin lymphoma cells when used at a concentration of 1 μM.{49032} MK-8745 (5 μM) induces apoptosis and polyploidy in p53-positive and -negative HCT116 colon cancer cells, respectively.{49031} It also induces apoptosis in sarcoma, melanoma, and pancreatic cancer cell lines in a p53-dependent manner when used at a concentration of 5 μM.
Brand:CaymanSKU:26190 - 10 mgAvailable on backorder
MK-8745 is an Aurora A kinase inhibitor (IC50 = 0.6 nM) that is selective for Aurora A over Aurora B kinase (IC50 = 280 nM).{49031} It induces cell cycle arrest at the G2/M phase in non-Hodgkin lymphoma cells when used at a concentration of 1 μM.{49032} MK-8745 (5 μM) induces apoptosis and polyploidy in p53-positive and -negative HCT116 colon cancer cells, respectively.{49031} It also induces apoptosis in sarcoma, melanoma, and pancreatic cancer cell lines in a p53-dependent manner when used at a concentration of 5 μM.
Brand:CaymanSKU:26190 - 25 mgAvailable on backorder
MK-8745 is an Aurora A kinase inhibitor (IC50 = 0.6 nM) that is selective for Aurora A over Aurora B kinase (IC50 = 280 nM).{49031} It induces cell cycle arrest at the G2/M phase in non-Hodgkin lymphoma cells when used at a concentration of 1 μM.{49032} MK-8745 (5 μM) induces apoptosis and polyploidy in p53-positive and -negative HCT116 colon cancer cells, respectively.{49031} It also induces apoptosis in sarcoma, melanoma, and pancreatic cancer cell lines in a p53-dependent manner when used at a concentration of 5 μM.
Brand:CaymanSKU:26190 - 5 mgAvailable on backorder
MK-8745 is an Aurora A kinase inhibitor (IC50 = 0.6 nM) that is selective for Aurora A over Aurora B kinase (IC50 = 280 nM).{49031} It induces cell cycle arrest at the G2/M phase in non-Hodgkin lymphoma cells when used at a concentration of 1 μM.{49032} MK-8745 (5 μM) induces apoptosis and polyploidy in p53-positive and -negative HCT116 colon cancer cells, respectively.{49031} It also induces apoptosis in sarcoma, melanoma, and pancreatic cancer cell lines in a p53-dependent manner when used at a concentration of 5 μM.
Brand:CaymanSKU:26190 - 50 mgAvailable on backorder
MK-886 is a potent, selective inhibitor of 5-lipoxygenase-activating protein (FLAP) that prevents 5-lipoxygenase activation in vivo and inhibits leukotriene biosynthesis in leukocytes with an IC50 of 2.5 nM.{2078} In human whole blood, leukotriene biosynthesis is inhibited by MK-886 with an IC50 of 1.1 µM.
Brand:CaymanSKU:21753 -Out of stock
MK-886 is a potent, selective inhibitor of 5-lipoxygenase-activating protein (FLAP) that prevents 5-lipoxygenase activation in vivo and inhibits leukotriene biosynthesis in leukocytes with an IC50 of 2.5 nM.{2078} In human whole blood, leukotriene biosynthesis is inhibited by MK-886 with an IC50 of 1.1 µM.
Brand:CaymanSKU:21753 -Out of stock
MK-886 is a potent, selective inhibitor of 5-lipoxygenase-activating protein (FLAP) that prevents 5-lipoxygenase activation in vivo and inhibits leukotriene biosynthesis in leukocytes with an IC50 of 2.5 nM.{2078} In human whole blood, leukotriene biosynthesis is inhibited by MK-886 with an IC50 of 1.1 µM.
Brand:CaymanSKU:21753 -Out of stock
MK-886 is a potent, selective inhibitor of 5-lipoxygenase-activating protein (FLAP) that prevents 5-lipoxygenase activation in vivo and inhibits leukotriene biosynthesis in leukocytes with an IC50 of 2.5 nM.{2078} In human whole blood, leukotriene biosynthesis is inhibited by MK-886 with an IC50 of 1.1 µM.
Brand:CaymanSKU:21753 -Out of stock
Arachidonic acid (Item No. 90010) and selected other polyunsaturated fatty acids are stereoselectively oxygenated at carbon 5 by the non-heme iron containing enzyme 5-lipoxygenase (5-LO).{6777} The intervention of a second protein, 5-LO-activating protein (FLAP), is required before 5-LO can become catalytically active.{7937} MK-886 binds to FLAP with high-affinity and prevents 5-LO activation. MK-886 inhibits leukotriene biosynthesis in leukocytes with an IC50 of 2.5 nM.{2078} In human whole blood, leukotriene biosynthesis is inhibited by MK-886 with an IC50 of 1.1 µM.
Brand:CaymanSKU:10133 - 1 mgAvailable on backorder
Arachidonic acid (Item No. 90010) and selected other polyunsaturated fatty acids are stereoselectively oxygenated at carbon 5 by the non-heme iron containing enzyme 5-lipoxygenase (5-LO).{6777} The intervention of a second protein, 5-LO-activating protein (FLAP), is required before 5-LO can become catalytically active.{7937} MK-886 binds to FLAP with high-affinity and prevents 5-LO activation. MK-886 inhibits leukotriene biosynthesis in leukocytes with an IC50 of 2.5 nM.{2078} In human whole blood, leukotriene biosynthesis is inhibited by MK-886 with an IC50 of 1.1 µM.
Brand:CaymanSKU:10133 - 10 mgAvailable on backorder
Arachidonic acid (Item No. 90010) and selected other polyunsaturated fatty acids are stereoselectively oxygenated at carbon 5 by the non-heme iron containing enzyme 5-lipoxygenase (5-LO).{6777} The intervention of a second protein, 5-LO-activating protein (FLAP), is required before 5-LO can become catalytically active.{7937} MK-886 binds to FLAP with high-affinity and prevents 5-LO activation. MK-886 inhibits leukotriene biosynthesis in leukocytes with an IC50 of 2.5 nM.{2078} In human whole blood, leukotriene biosynthesis is inhibited by MK-886 with an IC50 of 1.1 µM.
Brand:CaymanSKU:10133 - 25 mgAvailable on backorder
Arachidonic acid (Item No. 90010) and selected other polyunsaturated fatty acids are stereoselectively oxygenated at carbon 5 by the non-heme iron containing enzyme 5-lipoxygenase (5-LO).{6777} The intervention of a second protein, 5-LO-activating protein (FLAP), is required before 5-LO can become catalytically active.{7937} MK-886 binds to FLAP with high-affinity and prevents 5-LO activation. MK-886 inhibits leukotriene biosynthesis in leukocytes with an IC50 of 2.5 nM.{2078} In human whole blood, leukotriene biosynthesis is inhibited by MK-886 with an IC50 of 1.1 µM.
Brand:CaymanSKU:10133 - 5 mgAvailable on backorder
MAP kinase-activated protein kinase 2 (MAPKAP2, MK2) is a stress-activated serine/threonine protein kinase that is phosphorylated by p38 MAP kinase and is involved in diverse cellular functions with a central role in inflammation.{22830,17013,22949} MK2 inhibitor III is a potent, cell-permeable inhibitor of MK2 (IC50 = 8.5 nM).{25966} It less potently blocks MK3 and MK5 (IC50s = 210 and 81 nM, respectively) and is weak or inactive against several other kinases, including other p38 MAP kinase targets.{25966} MK2 inhibitor III prevents LPS-induced synthesis of TNF-α in human monocyte-like U937 cells (IC50 = 4.4 µM).{25966}
Brand:CaymanSKU:- MAP kinase-activated protein kinase 2 (MAPKAP2, MK2) is a stress-activated serine/threonine protein kinase that is phosphorylated by p38 MAP kinase and is involved in diverse cellular functions with a central role in inflammation.{22830,17013,22949} MK2 inhibitor III is a potent, cell-permeable inhibitor of MK2 (IC50 = 8.5 nM).{25966} It less potently blocks MK3 and MK5 (IC50s = 210 and 81 nM, respectively) and is weak or inactive against several other kinases, including other p38 MAP kinase targets.{25966} MK2 inhibitor III prevents LPS-induced synthesis of TNF-α in human monocyte-like U937 cells (IC50 = 4.4 µM).{25966}
Brand:CaymanSKU:- MAP kinase-activated protein kinase 2 (MAPKAP2, MK2) is a stress-activated serine/threonine protein kinase that is phosphorylated by p38 MAP kinase and is involved in diverse cellular functions with a central role in inflammation.{22830,17013,22949} MK2 inhibitor III is a potent, cell-permeable inhibitor of MK2 (IC50 = 8.5 nM).{25966} It less potently blocks MK3 and MK5 (IC50s = 210 and 81 nM, respectively) and is weak or inactive against several other kinases, including other p38 MAP kinase targets.{25966} MK2 inhibitor III prevents LPS-induced synthesis of TNF-α in human monocyte-like U937 cells (IC50 = 4.4 µM).{25966}
Brand:CaymanSKU:-
Activation of the p38/mitogen-activated protein kinase-activated protein kinase 2 (MAPKAPK2 or MK2) pathway has been implicated in promoting pro-inflammatory cytokine production and related inflammatory diseases. MK2 Inhibitor IV is a highly selective, non-ATP competitive MK2 inhibitor with an IC50 value of 0.11 μM.{22830} MK2 Inhibitor IV has been shown to inhibit pro-inflammatory cytokine secretion from the human THP-1 acute monocytic leukemia cell line, causing inhibition of LPS-stimulated TNF-α (IC50 = 4.4 μM) and IL-6 (IC50 = 5.2 μM) secretion.{22830} It can also inhibit IL-1β-stimulated matrixmetalloprotease 13 secretion from the SW1353 chondrosarcoma cell line (IC50 = 5.7 μM) and human primary chondrocyte cultures (IC50 = 2.2 μM).{22830}
Brand:CaymanSKU:- Activation of the p38/mitogen-activated protein kinase-activated protein kinase 2 (MAPKAPK2 or MK2) pathway has been implicated in promoting pro-inflammatory cytokine production and related inflammatory diseases. MK2 Inhibitor IV is a highly selective, non-ATP competitive MK2 inhibitor with an IC50 value of 0.11 μM.{22830} MK2 Inhibitor IV has been shown to inhibit pro-inflammatory cytokine secretion from the human THP-1 acute monocytic leukemia cell line, causing inhibition of LPS-stimulated TNF-α (IC50 = 4.4 μM) and IL-6 (IC50 = 5.2 μM) secretion.{22830} It can also inhibit IL-1β-stimulated matrixmetalloprotease 13 secretion from the SW1353 chondrosarcoma cell line (IC50 = 5.7 μM) and human primary chondrocyte cultures (IC50 = 2.2 μM).{22830}
Brand:CaymanSKU:- Activation of the p38/mitogen-activated protein kinase-activated protein kinase 2 (MAPKAPK2 or MK2) pathway has been implicated in promoting pro-inflammatory cytokine production and related inflammatory diseases. MK2 Inhibitor IV is a highly selective, non-ATP competitive MK2 inhibitor with an IC50 value of 0.11 μM.{22830} MK2 Inhibitor IV has been shown to inhibit pro-inflammatory cytokine secretion from the human THP-1 acute monocytic leukemia cell line, causing inhibition of LPS-stimulated TNF-α (IC50 = 4.4 μM) and IL-6 (IC50 = 5.2 μM) secretion.{22830} It can also inhibit IL-1β-stimulated matrixmetalloprotease 13 secretion from the SW1353 chondrosarcoma cell line (IC50 = 5.7 μM) and human primary chondrocyte cultures (IC50 = 2.2 μM).{22830}
Brand:CaymanSKU:-
MK2a inhibitor is a substrate-selective inhibitor of p38α MAPK that selectively inhibits p38α-dependent phosphorylation of MAPKAPK-2 (MK2) over activating transcription factor 2 (ATF2; Kiapps = 330 and >20,000 nM, respectively, in cell-free assays).{46548} It inhibits proliferation of U87, A172, and U251 glioblastoma cells (EC50s = 0.6-1 μM) via inhibition of tubulin polymerization and induction of apoptosis.{46549}
Brand:CaymanSKU:-Available on backorder
MK2a inhibitor is a substrate-selective inhibitor of p38α MAPK that selectively inhibits p38α-dependent phosphorylation of MAPKAPK-2 (MK2) over activating transcription factor 2 (ATF2; Kiapps = 330 and >20,000 nM, respectively, in cell-free assays).{46548} It inhibits proliferation of U87, A172, and U251 glioblastoma cells (EC50s = 0.6-1 μM) via inhibition of tubulin polymerization and induction of apoptosis.{46549}
Brand:CaymanSKU:-Available on backorder
MK2a inhibitor is a substrate-selective inhibitor of p38α MAPK that selectively inhibits p38α-dependent phosphorylation of MAPKAPK-2 (MK2) over activating transcription factor 2 (ATF2; Kiapps = 330 and >20,000 nM, respectively, in cell-free assays).{46548} It inhibits proliferation of U87, A172, and U251 glioblastoma cells (EC50s = 0.6-1 μM) via inhibition of tubulin polymerization and induction of apoptosis.{46549}
Brand:CaymanSKU:-Available on backorder