Cayman
Showing 34651–34800 of 45550 results
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PF-06282999 is an irreversible inhibitor of myeloperoxidase (MPO; Ki = 316.23 nM in a cell-free assay).{51086} It is selective for MPO over thyroid peroxidase (TPO) in a resorufin formation assay, as well as a panel of more than 50 enzymes, receptors, transporters, and ion channels at 100 µM. PF-06282999 inhibits MPO activity in isolated human whole blood with an IC50 value of 1.9 µM. It reduces the necrotic core area in atherosclerotic lesions by 37% in the aortic root of Ldlr-/- mice fed a Western diet when administered at a dose of 15 mg/kg twice per day for 14 weeks.{48865}
Brand:CaymanSKU:28406 - 1 mgAvailable on backorder
PF-06282999 is an irreversible inhibitor of myeloperoxidase (MPO; Ki = 316.23 nM in a cell-free assay).{51086} It is selective for MPO over thyroid peroxidase (TPO) in a resorufin formation assay, as well as a panel of more than 50 enzymes, receptors, transporters, and ion channels at 100 µM. PF-06282999 inhibits MPO activity in isolated human whole blood with an IC50 value of 1.9 µM. It reduces the necrotic core area in atherosclerotic lesions by 37% in the aortic root of Ldlr-/- mice fed a Western diet when administered at a dose of 15 mg/kg twice per day for 14 weeks.{48865}
Brand:CaymanSKU:28406 - 10 mgAvailable on backorder
PF-06282999 is an irreversible inhibitor of myeloperoxidase (MPO; Ki = 316.23 nM in a cell-free assay).{51086} It is selective for MPO over thyroid peroxidase (TPO) in a resorufin formation assay, as well as a panel of more than 50 enzymes, receptors, transporters, and ion channels at 100 µM. PF-06282999 inhibits MPO activity in isolated human whole blood with an IC50 value of 1.9 µM. It reduces the necrotic core area in atherosclerotic lesions by 37% in the aortic root of Ldlr-/- mice fed a Western diet when administered at a dose of 15 mg/kg twice per day for 14 weeks.{48865}
Brand:CaymanSKU:28406 - 25 mgAvailable on backorder
PF-06282999 is an irreversible inhibitor of myeloperoxidase (MPO; Ki = 316.23 nM in a cell-free assay).{51086} It is selective for MPO over thyroid peroxidase (TPO) in a resorufin formation assay, as well as a panel of more than 50 enzymes, receptors, transporters, and ion channels at 100 µM. PF-06282999 inhibits MPO activity in isolated human whole blood with an IC50 value of 1.9 µM. It reduces the necrotic core area in atherosclerotic lesions by 37% in the aortic root of Ldlr-/- mice fed a Western diet when administered at a dose of 15 mg/kg twice per day for 14 weeks.{48865}
Brand:CaymanSKU:28406 - 5 mgAvailable on backorder
PF-06409577 is an activator of AMP-activated protein kinase (AMPK) heterotrimers (Kd = 9 nM for α1β1γ1).{47255} In vitro, it selectively activates β1-containing AMPK isoforms (EC50s = 2.18-7.03 nM) over β2-containing isoforms (EC50s = ≥10 μM). PF-06409577 has an EC50 value of 7 nM in an activation/protection TR-FRET assay using α1β1γ1 AMPK. In vivo, PF-06409577 (≥10 mg/kg) increases phosphorylation of AMPK in rat kidney. It decreases urinary albumin levels in a ZSF1 obese rat model of diabetes, metabolic syndrome, and renal disease when administered at a dose of 100 mg/kg.
Brand:CaymanSKU:27366 - 1 mgAvailable on backorder
PF-06409577 is an activator of AMP-activated protein kinase (AMPK) heterotrimers (Kd = 9 nM for α1β1γ1).{47255} In vitro, it selectively activates β1-containing AMPK isoforms (EC50s = 2.18-7.03 nM) over β2-containing isoforms (EC50s = ≥10 μM). PF-06409577 has an EC50 value of 7 nM in an activation/protection TR-FRET assay using α1β1γ1 AMPK. In vivo, PF-06409577 (≥10 mg/kg) increases phosphorylation of AMPK in rat kidney. It decreases urinary albumin levels in a ZSF1 obese rat model of diabetes, metabolic syndrome, and renal disease when administered at a dose of 100 mg/kg.
Brand:CaymanSKU:27366 - 10 mgAvailable on backorder
PF-06409577 is an activator of AMP-activated protein kinase (AMPK) heterotrimers (Kd = 9 nM for α1β1γ1).{47255} In vitro, it selectively activates β1-containing AMPK isoforms (EC50s = 2.18-7.03 nM) over β2-containing isoforms (EC50s = ≥10 μM). PF-06409577 has an EC50 value of 7 nM in an activation/protection TR-FRET assay using α1β1γ1 AMPK. In vivo, PF-06409577 (≥10 mg/kg) increases phosphorylation of AMPK in rat kidney. It decreases urinary albumin levels in a ZSF1 obese rat model of diabetes, metabolic syndrome, and renal disease when administered at a dose of 100 mg/kg.
Brand:CaymanSKU:27366 - 25 mgAvailable on backorder
PF-06409577 is an activator of AMP-activated protein kinase (AMPK) heterotrimers (Kd = 9 nM for α1β1γ1).{47255} In vitro, it selectively activates β1-containing AMPK isoforms (EC50s = 2.18-7.03 nM) over β2-containing isoforms (EC50s = ≥10 μM). PF-06409577 has an EC50 value of 7 nM in an activation/protection TR-FRET assay using α1β1γ1 AMPK. In vivo, PF-06409577 (≥10 mg/kg) increases phosphorylation of AMPK in rat kidney. It decreases urinary albumin levels in a ZSF1 obese rat model of diabetes, metabolic syndrome, and renal disease when administered at a dose of 100 mg/kg.
Brand:CaymanSKU:27366 - 5 mgAvailable on backorder
PF-06424439 is an orally bioavailable inhibitor of diacylglycerol acyltransferase 2 (DGAT-2; IC50 = 14 nM).{46032} It is selective for DGAT-2 over the related acyltransferases DGAT-1, MGAT-2, and MGAT-3 (IC50s = >50 μM). PF-06424439 (0.1-10 mg/kg) reduces plasma triglyceride levels in sucrose-fed rats in a dose-dependent manner. It also reduces plasma levels of cholesterol and triglycerides as well as hepatic triglycerides in LDL receptor knockout mice fed a high-fat, high-cholesterol diet when administered at a dose of 60 mg/kg per day.
Brand:CaymanSKU:-Available on backorder
PF-06424439 is an orally bioavailable inhibitor of diacylglycerol acyltransferase 2 (DGAT-2; IC50 = 14 nM).{46032} It is selective for DGAT-2 over the related acyltransferases DGAT-1, MGAT-2, and MGAT-3 (IC50s = >50 μM). PF-06424439 (0.1-10 mg/kg) reduces plasma triglyceride levels in sucrose-fed rats in a dose-dependent manner. It also reduces plasma levels of cholesterol and triglycerides as well as hepatic triglycerides in LDL receptor knockout mice fed a high-fat, high-cholesterol diet when administered at a dose of 60 mg/kg per day.
Brand:CaymanSKU:-Available on backorder
PF-06424439 is an orally bioavailable inhibitor of diacylglycerol acyltransferase 2 (DGAT-2; IC50 = 14 nM).{46032} It is selective for DGAT-2 over the related acyltransferases DGAT-1, MGAT-2, and MGAT-3 (IC50s = >50 μM). PF-06424439 (0.1-10 mg/kg) reduces plasma triglyceride levels in sucrose-fed rats in a dose-dependent manner. It also reduces plasma levels of cholesterol and triglycerides as well as hepatic triglycerides in LDL receptor knockout mice fed a high-fat, high-cholesterol diet when administered at a dose of 60 mg/kg per day.
Brand:CaymanSKU:-Available on backorder
Anaplastic lymphoma kinase (ALK) is a receptor tyrosine kinase that promotes cell proliferation and blocks apoptosis. PF-06463922 is an ATP-competitive, selective inhibitor of ALK (Ki = i = 0.7 nM).{29757} It has strong activity against all known ALK and ROS1 mutants identified in patients, including the EML4-L1196M mutant of ALK (Ki = < 0.02 nM).{29757,29756,29759} PF-06463922 is orally available, displaying inhibition of ALK phosphorylation and antitumor efficacy in a xenograft model expressing EML4-L1196M ALK.{29757,29758} It demonstrates efficient blood-brain barrier penetration, produces brain tumor regression in mice harboring EML4-ALK tumors, and increases overall survival.{29756}
Brand:CaymanSKU:-Available on backorder
Anaplastic lymphoma kinase (ALK) is a receptor tyrosine kinase that promotes cell proliferation and blocks apoptosis. PF-06463922 is an ATP-competitive, selective inhibitor of ALK (Ki = i = 0.7 nM).{29757} It has strong activity against all known ALK and ROS1 mutants identified in patients, including the EML4-L1196M mutant of ALK (Ki = < 0.02 nM).{29757,29756,29759} PF-06463922 is orally available, displaying inhibition of ALK phosphorylation and antitumor efficacy in a xenograft model expressing EML4-L1196M ALK.{29757,29758} It demonstrates efficient blood-brain barrier penetration, produces brain tumor regression in mice harboring EML4-ALK tumors, and increases overall survival.{29756}
Brand:CaymanSKU:-Available on backorder
Anaplastic lymphoma kinase (ALK) is a receptor tyrosine kinase that promotes cell proliferation and blocks apoptosis. PF-06463922 is an ATP-competitive, selective inhibitor of ALK (Ki = i = 0.7 nM).{29757} It has strong activity against all known ALK and ROS1 mutants identified in patients, including the EML4-L1196M mutant of ALK (Ki = < 0.02 nM).{29757,29756,29759} PF-06463922 is orally available, displaying inhibition of ALK phosphorylation and antitumor efficacy in a xenograft model expressing EML4-L1196M ALK.{29757,29758} It demonstrates efficient blood-brain barrier penetration, produces brain tumor regression in mice harboring EML4-ALK tumors, and increases overall survival.{29756}
Brand:CaymanSKU:-Available on backorder
PF-06650833 is an inhibitor of interleukin-1 receptor associated kinase 4 (IRAK4; IC50 = 0.2 nM in a cell-free assay).{46434} It inhibits 100% of IRAK4 activity and is selective for IRAK4 over 273 kinases in a panel at 200 nM, but does inhibit IRAK1, MNK2, LRRK2, CLK4, and CLKɣ1 activity by greater than 70%. PF-06650833 reduces levels of TNF-α and IL-6 in R848-stimulated isolated human whole blood and peripheral blood mononuclear cells (PBMCs), respectively (IC50 = ~2 nM for both). It decreases LPS-induced increases in rat serum levels of TNF-α when administered at doses of 1, 3, and 30 mg/kg.
Brand:CaymanSKU:28397 - 10 mgAvailable on backorder
PF-06650833 is an inhibitor of interleukin-1 receptor associated kinase 4 (IRAK4; IC50 = 0.2 nM in a cell-free assay).{46434} It inhibits 100% of IRAK4 activity and is selective for IRAK4 over 273 kinases in a panel at 200 nM, but does inhibit IRAK1, MNK2, LRRK2, CLK4, and CLKɣ1 activity by greater than 70%. PF-06650833 reduces levels of TNF-α and IL-6 in R848-stimulated isolated human whole blood and peripheral blood mononuclear cells (PBMCs), respectively (IC50 = ~2 nM for both). It decreases LPS-induced increases in rat serum levels of TNF-α when administered at doses of 1, 3, and 30 mg/kg.
Brand:CaymanSKU:28397 - 25 mgAvailable on backorder
PF-06650833 is an inhibitor of interleukin-1 receptor associated kinase 4 (IRAK4; IC50 = 0.2 nM in a cell-free assay).{46434} It inhibits 100% of IRAK4 activity and is selective for IRAK4 over 273 kinases in a panel at 200 nM, but does inhibit IRAK1, MNK2, LRRK2, CLK4, and CLKɣ1 activity by greater than 70%. PF-06650833 reduces levels of TNF-α and IL-6 in R848-stimulated isolated human whole blood and peripheral blood mononuclear cells (PBMCs), respectively (IC50 = ~2 nM for both). It decreases LPS-induced increases in rat serum levels of TNF-α when administered at doses of 1, 3, and 30 mg/kg.
Brand:CaymanSKU:28397 - 5 mgAvailable on backorder
PF-06650833 is an inhibitor of interleukin-1 receptor associated kinase 4 (IRAK4; IC50 = 0.2 nM in a cell-free assay).{46434} It inhibits 100% of IRAK4 activity and is selective for IRAK4 over 273 kinases in a panel at 200 nM, but does inhibit IRAK1, MNK2, LRRK2, CLK4, and CLKɣ1 activity by greater than 70%. PF-06650833 reduces levels of TNF-α and IL-6 in R848-stimulated isolated human whole blood and peripheral blood mononuclear cells (PBMCs), respectively (IC50 = ~2 nM for both). It decreases LPS-induced increases in rat serum levels of TNF-α when administered at doses of 1, 3, and 30 mg/kg.
Brand:CaymanSKU:28397 - 50 mgAvailable on backorder
PF-06700841 is an inhibitor of JAK1 and tyrosine kinase 2 (TYK2; IC50s = 17 and 23 nM, respectively).{44011} It is selective for JAK1 and TYK2 over JAK2 and JAK3 (IC50s = 77 and 6,494 nM, respectively). PF-06700841 selectively inhibits IFN-α/STAT3 signaling over erythropoietin/STAT5 signaling in human whole blood (IC50s = 30 and 577 nM, respectively). It reduces increases in hind paw volume in a rat model of adjuvant-induced arthritis in a dose-dependent manner.
Brand:CaymanSKU:26125 - 1 mgAvailable on backorder
PF-06700841 is an inhibitor of JAK1 and tyrosine kinase 2 (TYK2; IC50s = 17 and 23 nM, respectively).{44011} It is selective for JAK1 and TYK2 over JAK2 and JAK3 (IC50s = 77 and 6,494 nM, respectively). PF-06700841 selectively inhibits IFN-α/STAT3 signaling over erythropoietin/STAT5 signaling in human whole blood (IC50s = 30 and 577 nM, respectively). It reduces increases in hind paw volume in a rat model of adjuvant-induced arthritis in a dose-dependent manner.
Brand:CaymanSKU:26125 - 10 mgAvailable on backorder
PF-06700841 is an inhibitor of JAK1 and tyrosine kinase 2 (TYK2; IC50s = 17 and 23 nM, respectively).{44011} It is selective for JAK1 and TYK2 over JAK2 and JAK3 (IC50s = 77 and 6,494 nM, respectively). PF-06700841 selectively inhibits IFN-α/STAT3 signaling over erythropoietin/STAT5 signaling in human whole blood (IC50s = 30 and 577 nM, respectively). It reduces increases in hind paw volume in a rat model of adjuvant-induced arthritis in a dose-dependent manner.
Brand:CaymanSKU:26125 - 5 mgAvailable on backorder
PF-06869206 is an orally bioavailable inhibitor of sodium-phosphate cotransporter 2a (NaPi2a; IC50 = 380 nM).{35938} It is selective for NaPi2a over NaPi2b, NaPi2c, PiT-1, and PiT-2 (IC50s = >25 μM).
Brand:CaymanSKU:28158 - 1 mgAvailable on backorder
PF-06869206 is an orally bioavailable inhibitor of sodium-phosphate cotransporter 2a (NaPi2a; IC50 = 380 nM).{35938} It is selective for NaPi2a over NaPi2b, NaPi2c, PiT-1, and PiT-2 (IC50s = >25 μM).
Brand:CaymanSKU:28158 - 10 mgAvailable on backorder
PF-06869206 is an orally bioavailable inhibitor of sodium-phosphate cotransporter 2a (NaPi2a; IC50 = 380 nM).{35938} It is selective for NaPi2a over NaPi2b, NaPi2c, PiT-1, and PiT-2 (IC50s = >25 μM).
Brand:CaymanSKU:28158 - 25 mgAvailable on backorder
PF-06869206 is an orally bioavailable inhibitor of sodium-phosphate cotransporter 2a (NaPi2a; IC50 = 380 nM).{35938} It is selective for NaPi2a over NaPi2b, NaPi2c, PiT-1, and PiT-2 (IC50s = >25 μM).
Brand:CaymanSKU:28158 - 5 mgAvailable on backorder
PF-1022A is a cyclodepsipeptide fungal metabolite originally isolated from mycelia sterilia and has anthelmintic activity.{48890} Oral administration of PF-1022A (0.5-2 mg/kg) induces worm excretion in a chicken model of A. galli infection. It induces parasite clearance in jird models of H. contortus, O. ostertagi, or T. colubriformis infection (ED95s = 0.11, 0.33, and 0.11 mg/animal).{48891}
Brand:CaymanSKU:29700 - 1 mgAvailable on backorder
PF-1022A is a cyclodepsipeptide fungal metabolite originally isolated from mycelia sterilia and has anthelmintic activity.{48890} Oral administration of PF-1022A (0.5-2 mg/kg) induces worm excretion in a chicken model of A. galli infection. It induces parasite clearance in jird models of H. contortus, O. ostertagi, or T. colubriformis infection (ED95s = 0.11, 0.33, and 0.11 mg/animal).{48891}
Brand:CaymanSKU:29700 - 5 mgAvailable on backorder
PF-1163B is a depsipeptide antifungal isolated from Penicillium that inhibits ergosterol (ERG) synthesis (IC50 = 34 ng/ml).{39013,39015} It inhibits growth of C. albicans (MIC = 32 µg/ml) but not of other Candida strains, A. fumigatus, or HepG2 cells.{39013} It acts synergistically with fluconazole (Item No. 11594) to reduce growth of azole-resistant C. albicans (MIC = 2 and 0.0016 µg/ml alone and in combination, respectively).{39014} PF-1163B is a hydroxy form of PF-1163A (Item No. 22065).
Brand:CaymanSKU:22066 -Out of stock
PF-1163B is a depsipeptide antifungal isolated from Penicillium that inhibits ergosterol (ERG) synthesis (IC50 = 34 ng/ml).{39013,39015} It inhibits growth of C. albicans (MIC = 32 µg/ml) but not of other Candida strains, A. fumigatus, or HepG2 cells.{39013} It acts synergistically with fluconazole (Item No. 11594) to reduce growth of azole-resistant C. albicans (MIC = 2 and 0.0016 µg/ml alone and in combination, respectively).{39014} PF-1163B is a hydroxy form of PF-1163A (Item No. 22065).
Brand:CaymanSKU:22066 -Out of stock
PF-1355 is an irreversible myeloperoxidase (MPO) inhibitor (Ki = 346.74 nM in a cell-free assay).{51086} It is selective for MPO over thyroid peroxidase (TPO) and over a panel of more than 50 enzymes, receptors, transporters, and ion channels. It inhibits MPO activity in isolated human whole blood with an IC50 value of 1.5 µM. PF-1355 reduces MPO activity in plasma and peritoneal lavage fluid in a mouse model of peritonitis.{51087} It also reduces lung edema, decreases plasma levels of TNF-α, MCP-1/CCL2, MIP-2/CXCL2, and KC/CXCL1 and transiently increases and then reduces neutrophil levels in bronchoalveolar lavage fluid (BALF) in a mouse model of pulmonary immune complex vasculitis when administered at doses of 20 and 100 mg/kg.
Brand:CaymanSKU:22222 -Out of stock
PF-1355 is an irreversible myeloperoxidase (MPO) inhibitor (Ki = 346.74 nM in a cell-free assay).{51086} It is selective for MPO over thyroid peroxidase (TPO) and over a panel of more than 50 enzymes, receptors, transporters, and ion channels. It inhibits MPO activity in isolated human whole blood with an IC50 value of 1.5 µM. PF-1355 reduces MPO activity in plasma and peritoneal lavage fluid in a mouse model of peritonitis.{51087} It also reduces lung edema, decreases plasma levels of TNF-α, MCP-1/CCL2, MIP-2/CXCL2, and KC/CXCL1 and transiently increases and then reduces neutrophil levels in bronchoalveolar lavage fluid (BALF) in a mouse model of pulmonary immune complex vasculitis when administered at doses of 20 and 100 mg/kg.
Brand:CaymanSKU:22222 -Out of stock
PF-1355 is an irreversible myeloperoxidase (MPO) inhibitor (Ki = 346.74 nM in a cell-free assay).{51086} It is selective for MPO over thyroid peroxidase (TPO) and over a panel of more than 50 enzymes, receptors, transporters, and ion channels. It inhibits MPO activity in isolated human whole blood with an IC50 value of 1.5 µM. PF-1355 reduces MPO activity in plasma and peritoneal lavage fluid in a mouse model of peritonitis.{51087} It also reduces lung edema, decreases plasma levels of TNF-α, MCP-1/CCL2, MIP-2/CXCL2, and KC/CXCL1 and transiently increases and then reduces neutrophil levels in bronchoalveolar lavage fluid (BALF) in a mouse model of pulmonary immune complex vasculitis when administered at doses of 20 and 100 mg/kg.
Brand:CaymanSKU:22222 -Out of stock
PF-2545920 is a potent inhibitor of phosphodiesterase 10A (PDE10A; IC50 = 1.26 nM for the human recombinant enzyme).{38516} It is selective for PDE10A over other PDEs with IC50 values ranging from 1.7 to >10 μM. In vivo, PF-2545920 (0.1-3 mg/kg, i.p.) increases cAMP and cGMP production as well as phosphorylation of CREB and GluR1 in mouse striatum in a dose-dependent manner. It reduces climbing behavior induced by apomorphine (Item No. 16094) in mice (ID50 = 0.375 mg/kg) and disrupts the conditioned avoidance response in mice and rats (ID50s = 0.441 and 1.079 mg/kg, respectively). PF-2545920 reverses deficits in prepulse inhibition and social odor recognition induced by (+)-MK-801 (Item No. 10009019) in rats. Formulations containing PF-2545920 are under clinical investigation for the treatment of schizophrenia and Huntington’s disease.
Brand:CaymanSKU:-Available on backorder
PF-2545920 is a potent inhibitor of phosphodiesterase 10A (PDE10A; IC50 = 1.26 nM for the human recombinant enzyme).{38516} It is selective for PDE10A over other PDEs with IC50 values ranging from 1.7 to >10 μM. In vivo, PF-2545920 (0.1-3 mg/kg, i.p.) increases cAMP and cGMP production as well as phosphorylation of CREB and GluR1 in mouse striatum in a dose-dependent manner. It reduces climbing behavior induced by apomorphine (Item No. 16094) in mice (ID50 = 0.375 mg/kg) and disrupts the conditioned avoidance response in mice and rats (ID50s = 0.441 and 1.079 mg/kg, respectively). PF-2545920 reverses deficits in prepulse inhibition and social odor recognition induced by (+)-MK-801 (Item No. 10009019) in rats. Formulations containing PF-2545920 are under clinical investigation for the treatment of schizophrenia and Huntington’s disease.
Brand:CaymanSKU:-Available on backorder
PF-2545920 is a potent inhibitor of phosphodiesterase 10A (PDE10A; IC50 = 1.26 nM for the human recombinant enzyme).{38516} It is selective for PDE10A over other PDEs with IC50 values ranging from 1.7 to >10 μM. In vivo, PF-2545920 (0.1-3 mg/kg, i.p.) increases cAMP and cGMP production as well as phosphorylation of CREB and GluR1 in mouse striatum in a dose-dependent manner. It reduces climbing behavior induced by apomorphine (Item No. 16094) in mice (ID50 = 0.375 mg/kg) and disrupts the conditioned avoidance response in mice and rats (ID50s = 0.441 and 1.079 mg/kg, respectively). PF-2545920 reverses deficits in prepulse inhibition and social odor recognition induced by (+)-MK-801 (Item No. 10009019) in rats. Formulations containing PF-2545920 are under clinical investigation for the treatment of schizophrenia and Huntington’s disease.
Brand:CaymanSKU:-Available on backorder
PF-2545920 is a potent inhibitor of phosphodiesterase 10A (PDE10A; IC50 = 1.26 nM for the human recombinant enzyme).{38516} It is selective for PDE10A over other PDEs with IC50 values ranging from 1.7 to >10 μM. In vivo, PF-2545920 (0.1-3 mg/kg, i.p.) increases cAMP and cGMP production as well as phosphorylation of CREB and GluR1 in mouse striatum in a dose-dependent manner. It reduces climbing behavior induced by apomorphine (Item No. 16094) in mice (ID50 = 0.375 mg/kg) and disrupts the conditioned avoidance response in mice and rats (ID50s = 0.441 and 1.079 mg/kg, respectively). PF-2545920 reverses deficits in prepulse inhibition and social odor recognition induced by (+)-MK-801 (Item No. 10009019) in rats. Formulations containing PF-2545920 are under clinical investigation for the treatment of schizophrenia and Huntington’s disease.
Brand:CaymanSKU:-Available on backorder
The epidermal growth factor receptors (EGFR), whose members include ErbB1 (HER1), ErbB2 (HER2), ErbB3 (HER3), and ErbB4 (HER4), are receptor tyrosine kinases that are often over-expressed in cancer.{17857,18353} PF-299804 is a second generation pan-ErbB receptor tyrosine kinase inhibitor (IC50s = 6, 45.7, and 73.7 nM for ErbB1, ErbB2, and ErbB4, respectively) that irreversibly binds to the ATP site in the catalytic domains of ErbB receptors.{27742,27743} At 15 mg/kg, it demonstrates antitumor activity ranging from delay in tumor growth to complete regression in various tumor xenograft models expressing either wild-type ErbB or mutant ErbB family members that show resistance to first generation ErbB kinase inhibitors.{27742,27743}
Brand:CaymanSKU:9001879 - 1 mgAvailable on backorder
The epidermal growth factor receptors (EGFR), whose members include ErbB1 (HER1), ErbB2 (HER2), ErbB3 (HER3), and ErbB4 (HER4), are receptor tyrosine kinases that are often over-expressed in cancer.{17857,18353} PF-299804 is a second generation pan-ErbB receptor tyrosine kinase inhibitor (IC50s = 6, 45.7, and 73.7 nM for ErbB1, ErbB2, and ErbB4, respectively) that irreversibly binds to the ATP site in the catalytic domains of ErbB receptors.{27742,27743} At 15 mg/kg, it demonstrates antitumor activity ranging from delay in tumor growth to complete regression in various tumor xenograft models expressing either wild-type ErbB or mutant ErbB family members that show resistance to first generation ErbB kinase inhibitors.{27742,27743}
Brand:CaymanSKU:9001879 - 10 mgAvailable on backorder
The epidermal growth factor receptors (EGFR), whose members include ErbB1 (HER1), ErbB2 (HER2), ErbB3 (HER3), and ErbB4 (HER4), are receptor tyrosine kinases that are often over-expressed in cancer.{17857,18353} PF-299804 is a second generation pan-ErbB receptor tyrosine kinase inhibitor (IC50s = 6, 45.7, and 73.7 nM for ErbB1, ErbB2, and ErbB4, respectively) that irreversibly binds to the ATP site in the catalytic domains of ErbB receptors.{27742,27743} At 15 mg/kg, it demonstrates antitumor activity ranging from delay in tumor growth to complete regression in various tumor xenograft models expressing either wild-type ErbB or mutant ErbB family members that show resistance to first generation ErbB kinase inhibitors.{27742,27743}
Brand:CaymanSKU:9001879 - 5 mgAvailable on backorder
The epidermal growth factor receptors (EGFR), whose members include ErbB1 (HER1), ErbB2 (HER2), ErbB3 (HER3), and ErbB4 (HER4), are receptor tyrosine kinases that are often over-expressed in cancer.{17857,18353} PF-299804 is a second generation pan-ErbB receptor tyrosine kinase inhibitor (IC50s = 6, 45.7, and 73.7 nM for ErbB1, ErbB2, and ErbB4, respectively) that irreversibly binds to the ATP site in the catalytic domains of ErbB receptors.{27742,27743} At 15 mg/kg, it demonstrates antitumor activity ranging from delay in tumor growth to complete regression in various tumor xenograft models expressing either wild-type ErbB or mutant ErbB family members that show resistance to first generation ErbB kinase inhibitors.{27742,27743}
Brand:CaymanSKU:9001879 - 50 mgAvailable on backorder
PF-3084014 is a γ-secretase inhibitor (IC50s = 6.2 and 1.2 nM in an enzyme assay and in whole cells, respectively).{45150} It inhibits γ-secretase activity without inducing Notch-related toxicity (EC50s = 1,300-3,000 nM for B cells in fetal thymic organ cultures). It reduces the level of amyloid-β (1-40) (Aβ40) fragments in mouse brain three hours following administration of 1 to 18 mg/kg doses and reduces Aβ42 fragment levels when administered at doses of 9 or 18 mg/kg. It also reduces Aβ fragments in guinea pig brain when administered at doses ranging from 0.3 to 3 mg/kg per day for five days.
Brand:CaymanSKU:27061 - 1 mgAvailable on backorder
PF-3084014 is a γ-secretase inhibitor (IC50s = 6.2 and 1.2 nM in an enzyme assay and in whole cells, respectively).{45150} It inhibits γ-secretase activity without inducing Notch-related toxicity (EC50s = 1,300-3,000 nM for B cells in fetal thymic organ cultures). It reduces the level of amyloid-β (1-40) (Aβ40) fragments in mouse brain three hours following administration of 1 to 18 mg/kg doses and reduces Aβ42 fragment levels when administered at doses of 9 or 18 mg/kg. It also reduces Aβ fragments in guinea pig brain when administered at doses ranging from 0.3 to 3 mg/kg per day for five days.
Brand:CaymanSKU:27061 - 10 mgAvailable on backorder
PF-3084014 is a γ-secretase inhibitor (IC50s = 6.2 and 1.2 nM in an enzyme assay and in whole cells, respectively).{45150} It inhibits γ-secretase activity without inducing Notch-related toxicity (EC50s = 1,300-3,000 nM for B cells in fetal thymic organ cultures). It reduces the level of amyloid-β (1-40) (Aβ40) fragments in mouse brain three hours following administration of 1 to 18 mg/kg doses and reduces Aβ42 fragment levels when administered at doses of 9 or 18 mg/kg. It also reduces Aβ fragments in guinea pig brain when administered at doses ranging from 0.3 to 3 mg/kg per day for five days.
Brand:CaymanSKU:27061 - 25 mgAvailable on backorder
PF-3084014 is a γ-secretase inhibitor (IC50s = 6.2 and 1.2 nM in an enzyme assay and in whole cells, respectively).{45150} It inhibits γ-secretase activity without inducing Notch-related toxicity (EC50s = 1,300-3,000 nM for B cells in fetal thymic organ cultures). It reduces the level of amyloid-β (1-40) (Aβ40) fragments in mouse brain three hours following administration of 1 to 18 mg/kg doses and reduces Aβ42 fragment levels when administered at doses of 9 or 18 mg/kg. It also reduces Aβ fragments in guinea pig brain when administered at doses ranging from 0.3 to 3 mg/kg per day for five days.
Brand:CaymanSKU:27061 - 5 mgAvailable on backorder
PF-3274167 is an oxytocin receptor antagonist (Ki = 9.5 nM).{43621} It is selective for the oxytocin receptor over the vasopressin receptors V1A and V2 (Kis = 1,120 and 10,000 nM, respectively).
Brand:CaymanSKU:26189 - 1 mgAvailable on backorder
PF-3274167 is an oxytocin receptor antagonist (Ki = 9.5 nM).{43621} It is selective for the oxytocin receptor over the vasopressin receptors V1A and V2 (Kis = 1,120 and 10,000 nM, respectively).
Brand:CaymanSKU:26189 - 10 mgAvailable on backorder
PF-3274167 is an oxytocin receptor antagonist (Ki = 9.5 nM).{43621} It is selective for the oxytocin receptor over the vasopressin receptors V1A and V2 (Kis = 1,120 and 10,000 nM, respectively).
Brand:CaymanSKU:26189 - 25 mgAvailable on backorder
PF-3274167 is an oxytocin receptor antagonist (Ki = 9.5 nM).{43621} It is selective for the oxytocin receptor over the vasopressin receptors V1A and V2 (Kis = 1,120 and 10,000 nM, respectively).
Brand:CaymanSKU:26189 - 5 mgAvailable on backorder
PF-3716556 is a potent and selective hydrogen-potassium pump (H+/K+-ATPase) inhibitor in a new class of acid suppressants, the potassium-competitive acid blockers or acid pump antagonists.{34027} PF-3716556 inhibited H+/K+-ATPase activity in porcine membrane vesicles, as well as canine and human recombinant cells under ion-leaky conditions (pIC50s = 6.026, 6.038, and 6.009, respectively). PF-3716556 showed 3-fold greater inhibition than revaprazan in ion-tight (neutral pH) conditions.
Brand:CaymanSKU:-Available on backorder
PF-3716556 is a potent and selective hydrogen-potassium pump (H+/K+-ATPase) inhibitor in a new class of acid suppressants, the potassium-competitive acid blockers or acid pump antagonists.{34027} PF-3716556 inhibited H+/K+-ATPase activity in porcine membrane vesicles, as well as canine and human recombinant cells under ion-leaky conditions (pIC50s = 6.026, 6.038, and 6.009, respectively). PF-3716556 showed 3-fold greater inhibition than revaprazan in ion-tight (neutral pH) conditions.
Brand:CaymanSKU:-Available on backorder
PF-3716556 is a potent and selective hydrogen-potassium pump (H+/K+-ATPase) inhibitor in a new class of acid suppressants, the potassium-competitive acid blockers or acid pump antagonists.{34027} PF-3716556 inhibited H+/K+-ATPase activity in porcine membrane vesicles, as well as canine and human recombinant cells under ion-leaky conditions (pIC50s = 6.026, 6.038, and 6.009, respectively). PF-3716556 showed 3-fold greater inhibition than revaprazan in ion-tight (neutral pH) conditions.
Brand:CaymanSKU:-Available on backorder
PF-3716556 is a potent and selective hydrogen-potassium pump (H+/K+-ATPase) inhibitor in a new class of acid suppressants, the potassium-competitive acid blockers or acid pump antagonists.{34027} PF-3716556 inhibited H+/K+-ATPase activity in porcine membrane vesicles, as well as canine and human recombinant cells under ion-leaky conditions (pIC50s = 6.026, 6.038, and 6.009, respectively). PF-3716556 showed 3-fold greater inhibition than revaprazan in ion-tight (neutral pH) conditions.
Brand:CaymanSKU:-Available on backorder
p21-Activated kinases (PAKs) are STE20 serine/threonine kinases that are vital to normal cell function. Binding of various upstream partners to PAKs results in release of an autoinhibitory domain that blocks activity of the kinase domain.{23498} PAKs are upregulated in several human cancers and are potential therapeutic targets for cancer intervention.{23498} PF-3758309 is an ATP-competitive inhibitor of PAK4, preventing the phosphorylation of the PAK4 substrate GEF-H1 (IC50 = 1.3 nM) and blocking anchorage-independent growth of a panel of tumor cell lines (IC50 = 4.7 nM).{30920} It also inhibits the ability of kinase domains from other PAKs to phosphorylate peptide substrates (Kis = 18.1, 17.1, 13.7, 190, and 99 nM for PAKs 5, 6, 1, 2, and 3, respectively).{30920} PF-3758309 blocks the growth of multiple human tumor xenografts.{30920}
Brand:CaymanSKU:-Available on backorder
p21-Activated kinases (PAKs) are STE20 serine/threonine kinases that are vital to normal cell function. Binding of various upstream partners to PAKs results in release of an autoinhibitory domain that blocks activity of the kinase domain.{23498} PAKs are upregulated in several human cancers and are potential therapeutic targets for cancer intervention.{23498} PF-3758309 is an ATP-competitive inhibitor of PAK4, preventing the phosphorylation of the PAK4 substrate GEF-H1 (IC50 = 1.3 nM) and blocking anchorage-independent growth of a panel of tumor cell lines (IC50 = 4.7 nM).{30920} It also inhibits the ability of kinase domains from other PAKs to phosphorylate peptide substrates (Kis = 18.1, 17.1, 13.7, 190, and 99 nM for PAKs 5, 6, 1, 2, and 3, respectively).{30920} PF-3758309 blocks the growth of multiple human tumor xenografts.{30920}
Brand:CaymanSKU:-Available on backorder
p21-Activated kinases (PAKs) are STE20 serine/threonine kinases that are vital to normal cell function. Binding of various upstream partners to PAKs results in release of an autoinhibitory domain that blocks activity of the kinase domain.{23498} PAKs are upregulated in several human cancers and are potential therapeutic targets for cancer intervention.{23498} PF-3758309 is an ATP-competitive inhibitor of PAK4, preventing the phosphorylation of the PAK4 substrate GEF-H1 (IC50 = 1.3 nM) and blocking anchorage-independent growth of a panel of tumor cell lines (IC50 = 4.7 nM).{30920} It also inhibits the ability of kinase domains from other PAKs to phosphorylate peptide substrates (Kis = 18.1, 17.1, 13.7, 190, and 99 nM for PAKs 5, 6, 1, 2, and 3, respectively).{30920} PF-3758309 blocks the growth of multiple human tumor xenografts.{30920}
Brand:CaymanSKU:-Available on backorder
Fatty acid amide hydrolase (FAAH) degrades N-acyl ethanolamines (NAEs), including the endocannabinoid arachidonoyl ethanolamide (AEA). PF-3845 is a potent, selective, and irreversible inhibitor of FAAH (Ki = 0.23 μM).{17090} It covalently binds FAAH on Ser241 at the catalytic site, resulting in prolonged elevation of AEA in the brain and plasma in rats after treatment.{17090} PF-3845 significantly and persistently reduces inflammatory pain in rats through a cannabinoid receptor-dependent mechanism.{17090}
Brand:CaymanSKU:- Fatty acid amide hydrolase (FAAH) degrades N-acyl ethanolamines (NAEs), including the endocannabinoid arachidonoyl ethanolamide (AEA). PF-3845 is a potent, selective, and irreversible inhibitor of FAAH (Ki = 0.23 μM).{17090} It covalently binds FAAH on Ser241 at the catalytic site, resulting in prolonged elevation of AEA in the brain and plasma in rats after treatment.{17090} PF-3845 significantly and persistently reduces inflammatory pain in rats through a cannabinoid receptor-dependent mechanism.{17090}
Brand:CaymanSKU:- Fatty acid amide hydrolase (FAAH) degrades N-acyl ethanolamines (NAEs), including the endocannabinoid arachidonoyl ethanolamide (AEA). PF-3845 is a potent, selective, and irreversible inhibitor of FAAH (Ki = 0.23 μM).{17090} It covalently binds FAAH on Ser241 at the catalytic site, resulting in prolonged elevation of AEA in the brain and plasma in rats after treatment.{17090} PF-3845 significantly and persistently reduces inflammatory pain in rats through a cannabinoid receptor-dependent mechanism.{17090}
Brand:CaymanSKU:- Fatty acid amide hydrolase (FAAH) degrades N-acyl ethanolamines (NAEs), including the endocannabinoid arachidonoyl ethanolamide (AEA). PF-3845 is a potent, selective, and irreversible inhibitor of FAAH (Ki = 0.23 μM).{17090} It covalently binds FAAH on Ser241 at the catalytic site, resulting in prolonged elevation of AEA in the brain and plasma in rats after treatment.{17090} PF-3845 significantly and persistently reduces inflammatory pain in rats through a cannabinoid receptor-dependent mechanism.{17090}
Brand:CaymanSKU:-
PF-4136309 is a chemokine (C-C motif) receptor 2 (CCR2) antagonist (IC50s = 5.2, 13, and 17 nM for the human, rat, and mouse receptors, respectively).{53022} It also inhibits the voltage-gated potassium channel subtype Kv11.1 by 35% when used at a concentration of 10 µM. PF-4136309 decreases isolated human monocyte chemotaxis induced by chemokine (C-C motif) ligand 2 (CCL2) with an IC50 value of 3.9 nM.
Brand:CaymanSKU:21965 -Out of stock
PF-4136309 is a chemokine (C-C motif) receptor 2 (CCR2) antagonist (IC50s = 5.2, 13, and 17 nM for the human, rat, and mouse receptors, respectively).{53022} It also inhibits the voltage-gated potassium channel subtype Kv11.1 by 35% when used at a concentration of 10 µM. PF-4136309 decreases isolated human monocyte chemotaxis induced by chemokine (C-C motif) ligand 2 (CCL2) with an IC50 value of 3.9 nM.
Brand:CaymanSKU:21965 -Out of stock
PF-4136309 is a chemokine (C-C motif) receptor 2 (CCR2) antagonist (IC50s = 5.2, 13, and 17 nM for the human, rat, and mouse receptors, respectively).{53022} It also inhibits the voltage-gated potassium channel subtype Kv11.1 by 35% when used at a concentration of 10 µM. PF-4136309 decreases isolated human monocyte chemotaxis induced by chemokine (C-C motif) ligand 2 (CCL2) with an IC50 value of 3.9 nM.
Brand:CaymanSKU:21965 -Out of stock
PF-4136309 is a chemokine (C-C motif) receptor 2 (CCR2) antagonist (IC50s = 5.2, 13, and 17 nM for the human, rat, and mouse receptors, respectively).{53022} It also inhibits the voltage-gated potassium channel subtype Kv11.1 by 35% when used at a concentration of 10 µM. PF-4136309 decreases isolated human monocyte chemotaxis induced by chemokine (C-C motif) ligand 2 (CCL2) with an IC50 value of 3.9 nM.
Brand:CaymanSKU:21965 -Out of stock
PF-429242 is an inhibitor of site-1 protease with an IC50 value of 170 nM for human recombinant site-1 protease.{38306} It is selective for site-1 protease over trypsin, elastase, proteinase K, plasmin, kallikren, factor XIa, thrombin, and furin at concentrations up to 100 μM. PF-429242 completely inhibits proteolytic processing and nuclear translocation of sterol regulatory element-binding protein (SREBP) in HepG2 cells at a concentration of 10 μM. It also reduces expression of HMG-CoA synthase and fatty acid synthase (EC50s = 0.3 and 2 μM, respectively) and inhibits cholesterol synthesis (EC50 = 600 nM) in HepG2 cells and reduces cholesterol and fatty acid synthesis in CD-1 mice. PF-429242 inhibits replication of dengue virus serotypes 1-4 in infected HeLa cells.{38307} It also reduces growth of T98G, U87-MG, and A172 glioblastoma cells (IC50s = 0.32, 15.2, and 27.6 μM, respectively).{38308}
Brand:CaymanSKU:- PF-429242 is an inhibitor of site-1 protease with an IC50 value of 170 nM for human recombinant site-1 protease.{38306} It is selective for site-1 protease over trypsin, elastase, proteinase K, plasmin, kallikren, factor XIa, thrombin, and furin at concentrations up to 100 μM. PF-429242 completely inhibits proteolytic processing and nuclear translocation of sterol regulatory element-binding protein (SREBP) in HepG2 cells at a concentration of 10 μM. It also reduces expression of HMG-CoA synthase and fatty acid synthase (EC50s = 0.3 and 2 μM, respectively) and inhibits cholesterol synthesis (EC50 = 600 nM) in HepG2 cells and reduces cholesterol and fatty acid synthesis in CD-1 mice. PF-429242 inhibits replication of dengue virus serotypes 1-4 in infected HeLa cells.{38307} It also reduces growth of T98G, U87-MG, and A172 glioblastoma cells (IC50s = 0.32, 15.2, and 27.6 μM, respectively).{38308}
Brand:CaymanSKU:- PF-429242 is an inhibitor of site-1 protease with an IC50 value of 170 nM for human recombinant site-1 protease.{38306} It is selective for site-1 protease over trypsin, elastase, proteinase K, plasmin, kallikren, factor XIa, thrombin, and furin at concentrations up to 100 μM. PF-429242 completely inhibits proteolytic processing and nuclear translocation of sterol regulatory element-binding protein (SREBP) in HepG2 cells at a concentration of 10 μM. It also reduces expression of HMG-CoA synthase and fatty acid synthase (EC50s = 0.3 and 2 μM, respectively) and inhibits cholesterol synthesis (EC50 = 600 nM) in HepG2 cells and reduces cholesterol and fatty acid synthesis in CD-1 mice. PF-429242 inhibits replication of dengue virus serotypes 1-4 in infected HeLa cells.{38307} It also reduces growth of T98G, U87-MG, and A172 glioblastoma cells (IC50s = 0.32, 15.2, and 27.6 μM, respectively).{38308}
Brand:CaymanSKU:- PF-429242 is an inhibitor of site-1 protease with an IC50 value of 170 nM for human recombinant site-1 protease.{38306} It is selective for site-1 protease over trypsin, elastase, proteinase K, plasmin, kallikren, factor XIa, thrombin, and furin at concentrations up to 100 μM. PF-429242 completely inhibits proteolytic processing and nuclear translocation of sterol regulatory element-binding protein (SREBP) in HepG2 cells at a concentration of 10 μM. It also reduces expression of HMG-CoA synthase and fatty acid synthase (EC50s = 0.3 and 2 μM, respectively) and inhibits cholesterol synthesis (EC50 = 600 nM) in HepG2 cells and reduces cholesterol and fatty acid synthesis in CD-1 mice. PF-429242 inhibits replication of dengue virus serotypes 1-4 in infected HeLa cells.{38307} It also reduces growth of T98G, U87-MG, and A172 glioblastoma cells (IC50s = 0.32, 15.2, and 27.6 μM, respectively).{38308}
Brand:CaymanSKU:-
Proline-rich tyrosine kinase 2 (PYK2) and focal adhesion kinase (FAK) are nonreceptor tyrosine kinases that constitute the focal adhesion kinase subfamily. PYK2 is expressed in both bone-forming osteoblasts and bone-resorbing osteoclasts where it has a positive role in osteoclast maturation and bone resorption. PF-431396 is a pyrimidine-based dual inhibitor of FAK and PYK2 (IC50s = 2 and 11 nM, respectively).{28820} In ovariectomized rats, it has been shown to increase bone formation, promoting osteoblast recruitment and activity.{28821}
Brand:CaymanSKU:-Available on backorder
Proline-rich tyrosine kinase 2 (PYK2) and focal adhesion kinase (FAK) are nonreceptor tyrosine kinases that constitute the focal adhesion kinase subfamily. PYK2 is expressed in both bone-forming osteoblasts and bone-resorbing osteoclasts where it has a positive role in osteoclast maturation and bone resorption. PF-431396 is a pyrimidine-based dual inhibitor of FAK and PYK2 (IC50s = 2 and 11 nM, respectively).{28820} In ovariectomized rats, it has been shown to increase bone formation, promoting osteoblast recruitment and activity.{28821}
Brand:CaymanSKU:-Available on backorder
Proline-rich tyrosine kinase 2 (PYK2) and focal adhesion kinase (FAK) are nonreceptor tyrosine kinases that constitute the focal adhesion kinase subfamily. PYK2 is expressed in both bone-forming osteoblasts and bone-resorbing osteoclasts where it has a positive role in osteoclast maturation and bone resorption. PF-431396 is a pyrimidine-based dual inhibitor of FAK and PYK2 (IC50s = 2 and 11 nM, respectively).{28820} In ovariectomized rats, it has been shown to increase bone formation, promoting osteoblast recruitment and activity.{28821}
Brand:CaymanSKU:-Available on backorder
Proline-rich tyrosine kinase 2 (PYK2) and focal adhesion kinase (FAK) are nonreceptor tyrosine kinases that constitute the focal adhesion kinase subfamily. PYK2 is expressed in both bone-forming osteoblasts and bone-resorbing osteoclasts where it has a positive role in osteoclast maturation and bone resorption. PF-431396 is a pyrimidine-based dual inhibitor of FAK and PYK2 (IC50s = 2 and 11 nM, respectively).{28820} In ovariectomized rats, it has been shown to increase bone formation, promoting osteoblast recruitment and activity.{28821}
Brand:CaymanSKU:-Available on backorder
PF-4693627 is an orally bioavailable inhibitor of microsomal prostaglandin E (PGE) synthase-1 (mPGES-1; IC50 = 3 nM).{40125} It is selective for mPGES-1 over PGDS, TXAS, and 5-LO in HWB-1483 cells, which have IC50 values greater than 50 μM, as well as COX-2 in fetal fibroblasts (IC50 = >10 μM). PF-4693627 inhibits LPS-stimulated synthesis of PGE2 in human whole blood (IC50 = 109 nM). In vivo, PF-4693627 (10 mg/kg) inhibits PGE2 production in a guinea pig model of carrageenan-induced air pouch inflammation.
Brand:CaymanSKU:22768 -Out of stock
PF-4693627 is an orally bioavailable inhibitor of microsomal prostaglandin E (PGE) synthase-1 (mPGES-1; IC50 = 3 nM).{40125} It is selective for mPGES-1 over PGDS, TXAS, and 5-LO in HWB-1483 cells, which have IC50 values greater than 50 μM, as well as COX-2 in fetal fibroblasts (IC50 = >10 μM). PF-4693627 inhibits LPS-stimulated synthesis of PGE2 in human whole blood (IC50 = 109 nM). In vivo, PF-4693627 (10 mg/kg) inhibits PGE2 production in a guinea pig model of carrageenan-induced air pouch inflammation.
Brand:CaymanSKU:22768 -Out of stock
PF-4693627 is an orally bioavailable inhibitor of microsomal prostaglandin E (PGE) synthase-1 (mPGES-1; IC50 = 3 nM).{40125} It is selective for mPGES-1 over PGDS, TXAS, and 5-LO in HWB-1483 cells, which have IC50 values greater than 50 μM, as well as COX-2 in fetal fibroblasts (IC50 = >10 μM). PF-4693627 inhibits LPS-stimulated synthesis of PGE2 in human whole blood (IC50 = 109 nM). In vivo, PF-4693627 (10 mg/kg) inhibits PGE2 production in a guinea pig model of carrageenan-induced air pouch inflammation.
Brand:CaymanSKU:22768 -Out of stock
PF-4693627 is an orally bioavailable inhibitor of microsomal prostaglandin E (PGE) synthase-1 (mPGES-1; IC50 = 3 nM).{40125} It is selective for mPGES-1 over PGDS, TXAS, and 5-LO in HWB-1483 cells, which have IC50 values greater than 50 μM, as well as COX-2 in fetal fibroblasts (IC50 = >10 μM). PF-4693627 inhibits LPS-stimulated synthesis of PGE2 in human whole blood (IC50 = 109 nM). In vivo, PF-4693627 (10 mg/kg) inhibits PGE2 production in a guinea pig model of carrageenan-induced air pouch inflammation.
Brand:CaymanSKU:22768 -Out of stock
Checkpoint kinase 1 (Chk1) regulates S and G2-M phase cell cycle checkpoints in response to DNA damage. PF-477736 is an ATP-competitive inhibitor of Chk1 with a Ki value of 0.49 nM that demonstrates 100-fold selectivity over Chk2.{29021} When used in combination with various chemotherapeutics, PF-477736 abrogates DNA damage-induced cell cycle arrest, potentiating the antiproliferative effects of these compounds in tumor cell lines and xenografts.{29021,29022,29023}
Brand:CaymanSKU:-Available on backorder
Checkpoint kinase 1 (Chk1) regulates S and G2-M phase cell cycle checkpoints in response to DNA damage. PF-477736 is an ATP-competitive inhibitor of Chk1 with a Ki value of 0.49 nM that demonstrates 100-fold selectivity over Chk2.{29021} When used in combination with various chemotherapeutics, PF-477736 abrogates DNA damage-induced cell cycle arrest, potentiating the antiproliferative effects of these compounds in tumor cell lines and xenografts.{29021,29022,29023}
Brand:CaymanSKU:-Available on backorder
Checkpoint kinase 1 (Chk1) regulates S and G2-M phase cell cycle checkpoints in response to DNA damage. PF-477736 is an ATP-competitive inhibitor of Chk1 with a Ki value of 0.49 nM that demonstrates 100-fold selectivity over Chk2.{29021} When used in combination with various chemotherapeutics, PF-477736 abrogates DNA damage-induced cell cycle arrest, potentiating the antiproliferative effects of these compounds in tumor cell lines and xenografts.{29021,29022,29023}
Brand:CaymanSKU:-Available on backorder
Checkpoint kinase 1 (Chk1) regulates S and G2-M phase cell cycle checkpoints in response to DNA damage. PF-477736 is an ATP-competitive inhibitor of Chk1 with a Ki value of 0.49 nM that demonstrates 100-fold selectivity over Chk2.{29021} When used in combination with various chemotherapeutics, PF-477736 abrogates DNA damage-induced cell cycle arrest, potentiating the antiproliferative effects of these compounds in tumor cell lines and xenografts.{29021,29022,29023}
Brand:CaymanSKU:-Available on backorder
PF-4800567 is a selective inhibitor of casein kinase 1ε (CK1ε; IC50 = 32 nM) with greater than 20-fold selectivity over CK1δ.{30939} It blocks CK1ε-mediated PER3 nuclear localization and PER2 degradation, both of which are proteins important for maintaining circadian rhythms in cells.{30939} PF-4800567 has been used in the study of the CK1 enzymes in the regulation of circadian rhythm and is also reported to have neuroprotective effects.{30939,30937,30938}
Brand:CaymanSKU:-Available on backorder
PF-4800567 is a selective inhibitor of casein kinase 1ε (CK1ε; IC50 = 32 nM) with greater than 20-fold selectivity over CK1δ.{30939} It blocks CK1ε-mediated PER3 nuclear localization and PER2 degradation, both of which are proteins important for maintaining circadian rhythms in cells.{30939} PF-4800567 has been used in the study of the CK1 enzymes in the regulation of circadian rhythm and is also reported to have neuroprotective effects.{30939,30937,30938}
Brand:CaymanSKU:-Available on backorder