Chemicals
Showing 31501–31650 of 41137 results
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Peroxynitrite is formed in vivo by the reaction of NO with superoxide.{2738,5439,1678} It is a powerful oxidizing agent that can initiate lipid peroxidation, oxidize sulfhydryls, and nitrate the aromatic residues of proteins.
Brand:CaymanSKU:81565 - 1 mlAvailable on backorder
Peroxynitrite is formed in vivo by the reaction of NO with superoxide.{2738,5439,1678} It is a powerful oxidizing agent that can initiate lipid peroxidation, oxidize sulfhydryls, and nitrate the aromatic residues of proteins.
Brand:CaymanSKU:81565 - 5 mlAvailable on backorder
Perphenazine is a phenothiazine that binds with high affinity to a wide variety of receptors, including dopamine, serotonin (5-HT), histamine, and α-adrenergic receptors (Kis = 1.4, 5.6, 8, 10, and 17 nM for D2, 5-HT2A, H1, α1A, and 5-HT6, respectively).{24253} It is described as a typical antipsychotic and has been used extensively for schizophrenia and schizophrenia-like psychoses.{32677}
Brand:CaymanSKU:20735 -Available on backorder
Perphenazine is a phenothiazine that binds with high affinity to a wide variety of receptors, including dopamine, serotonin (5-HT), histamine, and α-adrenergic receptors (Kis = 1.4, 5.6, 8, 10, and 17 nM for D2, 5-HT2A, H1, α1A, and 5-HT6, respectively).{24253} It is described as a typical antipsychotic and has been used extensively for schizophrenia and schizophrenia-like psychoses.{32677}
Brand:CaymanSKU:20735 -Available on backorder
Perphenazine is a phenothiazine that binds with high affinity to a wide variety of receptors, including dopamine, serotonin (5-HT), histamine, and α-adrenergic receptors (Kis = 1.4, 5.6, 8, 10, and 17 nM for D2, 5-HT2A, H1, α1A, and 5-HT6, respectively).{24253} It is described as a typical antipsychotic and has been used extensively for schizophrenia and schizophrenia-like psychoses.{32677}
Brand:CaymanSKU:20735 -Available on backorder
Perphenazine is a phenothiazine that binds with high affinity to a wide variety of receptors, including dopamine, serotonin (5-HT), histamine, and α-adrenergic receptors (Kis = 1.4, 5.6, 8, 10, and 17 nM for D2, 5-HT2A, H1, α1A, and 5-HT6, respectively).{24253} It is described as a typical antipsychotic and has been used extensively for schizophrenia and schizophrenia-like psychoses.{32677}
Brand:CaymanSKU:20735 -Available on backorder
Pertussis toxin (islet-activating protein) is a toxin, first isolated from B. pertussis, that is used to study G protein-coupled receptor signaling in cells and experimental autoimmune encephalomyelitis (EAE) in animals. Pertussis toxin catalyzes the transfer of the ADP-ribose moiety of NAD to the α subunits of heterotrimeric Gi/o proteins, resulting in the receptors being uncoupled from Gi/o proteins.{31502,31505} Pertussis toxin is also used as an adjuvant, given with specific antigens, to immunize animals and induce EAE, an animal model of multiple sclerosis.{31501,31504} Pertussis toxin was first described as an islet-activating protein because it caused a sustained potentiation of the secretory response of pancreatic islet cells to various stimuli that stimulate Gi-linked α-adrenergic receptors.{31500,31503}
Brand:CaymanSKU:-Available on backorder
Pestalotin is a fungal metabolite originally isolated from P. cryptomeriaecola with diverse biological activities.{37633} It induces reducing sugar release in embryoless rice endosperms when used at concentrations ranging from 3 to 100 mg/L and enhances growth of rice seedlings (O. sativa) when used in combination with gibberellin A3 at concentrations ranging from 30 to 500 mg/L. Pestalotin has antifungal activity, reducing the growth of C. albicans, C. neoformans, T. rubrum, and A. fumigatus (MICs = 12.5, 50, 50, and 50 μg/ml, respectively).{37634} It is cytotoxic to HL-60, MKN45, LoVo, and A549 cells (IC50s = 64.87-182.92 μM). Pestalotin has been used as a standard for dereplication of natural products.{41781}
Brand:CaymanSKU:25516 - 2.5 mgAvailable on backorder
Pestalotin is a fungal metabolite originally isolated from P. cryptomeriaecola with diverse biological activities.{37633} It induces reducing sugar release in embryoless rice endosperms when used at concentrations ranging from 3 to 100 mg/L and enhances growth of rice seedlings (O. sativa) when used in combination with gibberellin A3 at concentrations ranging from 30 to 500 mg/L. Pestalotin has antifungal activity, reducing the growth of C. albicans, C. neoformans, T. rubrum, and A. fumigatus (MICs = 12.5, 50, 50, and 50 μg/ml, respectively).{37634} It is cytotoxic to HL-60, MKN45, LoVo, and A549 cells (IC50s = 64.87-182.92 μM). Pestalotin has been used as a standard for dereplication of natural products.{41781}
Brand:CaymanSKU:25516 - 500 µgAvailable on backorder
Petromurin C is a bis-indolyl benzenoid fungal metabolite originally isolated from the ascostromata of P. muricatus.{36676} It is cytotoxic to NS-1 mouse myeloma cells (IC50 = 33 μg/ml) and has activity against T. foetus in vitro (IC50 = 100 μg/ml).{39715}
Brand:CaymanSKU:25089 - 2.5 mgAvailable on backorder
Petromurin C is a bis-indolyl benzenoid fungal metabolite originally isolated from the ascostromata of P. muricatus.{36676} It is cytotoxic to NS-1 mouse myeloma cells (IC50 = 33 μg/ml) and has activity against T. foetus in vitro (IC50 = 100 μg/ml).{39715}
Brand:CaymanSKU:25089 - 500 µgAvailable on backorder
Petromyzonol is a tetrahydroxy stearol which serves as the primary spawning pheromone in adult sea lamprey. It is produced in the bile of sea lamprey larvae from the bile acid precursor allocholic acid. While the adult sea lamprey is relatively insensitive to petromyzonol itself, the C-24 sulfate ester (petromyzonol sulfate) is a pheromone and a spawning chemoattractant which can be detected at very low concentrations by lamprey olfactory chemoreceptors. Petromyzonol, petromyzonol sulfate, and allocholic acid are all found in water samples from fresh water streams bearing larval lamprey populations.{7478}
Brand:CaymanSKU:98250 - 1 mgAvailable on backorder
Petromyzonol is a tetrahydroxy stearol which serves as the primary spawning pheromone in adult sea lamprey. It is produced in the bile of sea lamprey larvae from the bile acid precursor allocholic acid. While the adult sea lamprey is relatively insensitive to petromyzonol itself, the C-24 sulfate ester (petromyzonol sulfate) is a pheromone and a spawning chemoattractant which can be detected at very low concentrations by lamprey olfactory chemoreceptors. Petromyzonol, petromyzonol sulfate, and allocholic acid are all found in water samples from fresh water streams bearing larval lamprey populations.{7478}
Brand:CaymanSKU:98250 - 10 mgAvailable on backorder
Petromyzonol is a tetrahydroxy stearol which serves as the primary spawning pheromone in adult sea lamprey. It is produced in the bile of sea lamprey larvae from the bile acid precursor allocholic acid. While the adult sea lamprey is relatively insensitive to petromyzonol itself, the C-24 sulfate ester (petromyzonol sulfate) is a pheromone and a spawning chemoattractant which can be detected at very low concentrations by lamprey olfactory chemoreceptors. Petromyzonol, petromyzonol sulfate, and allocholic acid are all found in water samples from fresh water streams bearing larval lamprey populations.{7478}
Brand:CaymanSKU:98250 - 5 mgAvailable on backorder
Petunidin is an O-methylated anthocyanidin derived from delphinidin (Item No. 11012) that imparts blue-red pigments to flowers, fruits, and red wine. It has been shown to bind with and suppress the activity of focal adhesion kinase and to inhibit platelet-derived growth factor-induced aortic smooth muscle cell migration, which may confer a protective effect against atherosclerosis.{31754} Extracts from E. jambolana fruit, which is rich in anthocyanins including petunidin, have been used to suppress the proliferation of an HCT116 colon cancer cell line, as well as colon cancer stem cells.{31753}
Brand:CaymanSKU:19755 -Available on backorder
Petunidin is an O-methylated anthocyanidin derived from delphinidin (Item No. 11012) that imparts blue-red pigments to flowers, fruits, and red wine. It has been shown to bind with and suppress the activity of focal adhesion kinase and to inhibit platelet-derived growth factor-induced aortic smooth muscle cell migration, which may confer a protective effect against atherosclerosis.{31754} Extracts from E. jambolana fruit, which is rich in anthocyanins including petunidin, have been used to suppress the proliferation of an HCT116 colon cancer cell line, as well as colon cancer stem cells.{31753}
Brand:CaymanSKU:19755 -Available on backorder
Petunidin is an O-methylated anthocyanidin derived from delphinidin (Item No. 11012) that imparts blue-red pigments to flowers, fruits, and red wine. It has been shown to bind with and suppress the activity of focal adhesion kinase and to inhibit platelet-derived growth factor-induced aortic smooth muscle cell migration, which may confer a protective effect against atherosclerosis.{31754} Extracts from E. jambolana fruit, which is rich in anthocyanins including petunidin, have been used to suppress the proliferation of an HCT116 colon cancer cell line, as well as colon cancer stem cells.{31753}
Brand:CaymanSKU:19755 -Available on backorder
Petunidin is an O-methylated anthocyanidin derived from delphinidin (Item No. 11012) that imparts blue-red pigments to flowers, fruits, and red wine. It has been shown to bind with and suppress the activity of focal adhesion kinase and to inhibit platelet-derived growth factor-induced aortic smooth muscle cell migration, which may confer a protective effect against atherosclerosis.{31754} Extracts from E. jambolana fruit, which is rich in anthocyanins including petunidin, have been used to suppress the proliferation of an HCT116 colon cancer cell line, as well as colon cancer stem cells.{31753}
Brand:CaymanSKU:19755 -Available on backorder
Petunidin 3-O-glucoside is an anthocyanin that has been found in red grapes and red wines with antiproliferative properties.{43543} It reduces DBTRG-05MG glioblastoma cell growth in a time- and concentration-dependent manner by increasing production of reactive oxygen species (ROS) and Bax protein levels and reducing Bcl-2 and caspase-3 activities. Petunidin 3-O-glucoside also reduces glucose uptake, lactic acid production, and NAD levels in DBTRG-05MG cells.
Brand:CaymanSKU:25686 - 1 mgAvailable on backorder
Petunidin 3-O-glucoside is an anthocyanin that has been found in red grapes and red wines with antiproliferative properties.{43543} It reduces DBTRG-05MG glioblastoma cell growth in a time- and concentration-dependent manner by increasing production of reactive oxygen species (ROS) and Bax protein levels and reducing Bcl-2 and caspase-3 activities. Petunidin 3-O-glucoside also reduces glucose uptake, lactic acid production, and NAD levels in DBTRG-05MG cells.
Brand:CaymanSKU:25686 - 5 mgAvailable on backorder
Colony stimulating factor 1 (CSF1) is a cytokine that is involved in the recruitment and activation of tissue macrophages. It exerts these effects by binding to its corresponding receptor tyrosine kinase, the cFMS/CSF1 receptor (CSF1R). Pexidartinib is a brain-penetrant inhibitor of CSF1R, as well as c-Kit and FLT3 (IC50s = 20, 10, and 160 nM in vitro, respectively).{30529} It has been used in combination with paclitaxel (Item No. 10461) to block macrophage recruitment in mammary tumor-bearing mice, thus slowing primary tumor development and metastasis.{30529} Pexidartinib has also been used to block microglial stimulation of glioblastoma invasion in both cell culture and a mouse model of glioblastoma multiforme.{30528}
Brand:CaymanSKU:-Available on backorder
Colony stimulating factor 1 (CSF1) is a cytokine that is involved in the recruitment and activation of tissue macrophages. It exerts these effects by binding to its corresponding receptor tyrosine kinase, the cFMS/CSF1 receptor (CSF1R). Pexidartinib is a brain-penetrant inhibitor of CSF1R, as well as c-Kit and FLT3 (IC50s = 20, 10, and 160 nM in vitro, respectively).{30529} It has been used in combination with paclitaxel (Item No. 10461) to block macrophage recruitment in mammary tumor-bearing mice, thus slowing primary tumor development and metastasis.{30529} Pexidartinib has also been used to block microglial stimulation of glioblastoma invasion in both cell culture and a mouse model of glioblastoma multiforme.{30528}
Brand:CaymanSKU:-Available on backorder
Colony stimulating factor 1 (CSF1) is a cytokine that is involved in the recruitment and activation of tissue macrophages. It exerts these effects by binding to its corresponding receptor tyrosine kinase, the cFMS/CSF1 receptor (CSF1R). Pexidartinib is a brain-penetrant inhibitor of CSF1R, as well as c-Kit and FLT3 (IC50s = 20, 10, and 160 nM in vitro, respectively).{30529} It has been used in combination with paclitaxel (Item No. 10461) to block macrophage recruitment in mammary tumor-bearing mice, thus slowing primary tumor development and metastasis.{30529} Pexidartinib has also been used to block microglial stimulation of glioblastoma invasion in both cell culture and a mouse model of glioblastoma multiforme.{30528}
Brand:CaymanSKU:-Available on backorder
Colony stimulating factor 1 (CSF1) is a cytokine that is involved in the recruitment and activation of tissue macrophages. It exerts these effects by binding to its corresponding receptor tyrosine kinase, the cFMS/CSF1 receptor (CSF1R). Pexidartinib is a brain-penetrant inhibitor of CSF1R, as well as c-Kit and FLT3 (IC50s = 20, 10, and 160 nM in vitro, respectively).{30529} It has been used in combination with paclitaxel (Item No. 10461) to block macrophage recruitment in mammary tumor-bearing mice, thus slowing primary tumor development and metastasis.{30529} Pexidartinib has also been used to block microglial stimulation of glioblastoma invasion in both cell culture and a mouse model of glioblastoma multiforme.{30528}
Brand:CaymanSKU:-Available on backorder
Pexmetinib is a dual inhibitor of Tie2 and p38 MAPK (IC50s = 1, 26, and 35 nM for Tie2, p38α, and p38β, respectively).{43849} It also inhibits Abl, ARG, FGFR, FLT1, FLT4, Fyn, HCK, LYN, and MINK (IC50s = 4, 10, 28, 47, 42, 41, 26, 25, and 26 nM, respectively). Pexmetinib (0.5 and 1 µM) reduces proliferation of KG-1 and KT-1 leukemic cells in vitro.
Brand:CaymanSKU:26187 - 1 mgAvailable on backorder
Pexmetinib is a dual inhibitor of Tie2 and p38 MAPK (IC50s = 1, 26, and 35 nM for Tie2, p38α, and p38β, respectively).{43849} It also inhibits Abl, ARG, FGFR, FLT1, FLT4, Fyn, HCK, LYN, and MINK (IC50s = 4, 10, 28, 47, 42, 41, 26, 25, and 26 nM, respectively). Pexmetinib (0.5 and 1 µM) reduces proliferation of KG-1 and KT-1 leukemic cells in vitro.
Brand:CaymanSKU:26187 - 10 mgAvailable on backorder
Pexmetinib is a dual inhibitor of Tie2 and p38 MAPK (IC50s = 1, 26, and 35 nM for Tie2, p38α, and p38β, respectively).{43849} It also inhibits Abl, ARG, FGFR, FLT1, FLT4, Fyn, HCK, LYN, and MINK (IC50s = 4, 10, 28, 47, 42, 41, 26, 25, and 26 nM, respectively). Pexmetinib (0.5 and 1 µM) reduces proliferation of KG-1 and KT-1 leukemic cells in vitro.
Brand:CaymanSKU:26187 - 5 mgAvailable on backorder
PF-01247324 is a blocker of the tetrodotoxin-resistant (TTX-R) sodium channel Nav1.8 (IC50 = 0.19 μM for human Nav1.8).{36846} It is selective for Nav1.8 over Nav1.1, Nav1.2, Nav1.5, and Nav1.7 channels (IC50s = 13, 12.8, 9, and 19 μM, respectively) as well as ether-a-go-go (ERG) potassium channels (IC50 = 30 μM). PF-01247324 blocks Nav1.8 channels in a VSP-FRET assay using HEK293 cells (IC50 = 2.6 μM). In vivo, PF-01247324 (100 mg/kg) reduces phase 2 flinching in a rat model of formalin-induced persistent pain.{36847} It increases latency to lift the inflamed paw and latency to paw withdrawal in rat models of carrageenan-induced thermal hyperalgesia and mechanical hyperalgesia induced by complete Freund’s adjuvant (CFA), respectively.
Brand:CaymanSKU:22111 -Out of stock
PF-01247324 is a blocker of the tetrodotoxin-resistant (TTX-R) sodium channel Nav1.8 (IC50 = 0.19 μM for human Nav1.8).{36846} It is selective for Nav1.8 over Nav1.1, Nav1.2, Nav1.5, and Nav1.7 channels (IC50s = 13, 12.8, 9, and 19 μM, respectively) as well as ether-a-go-go (ERG) potassium channels (IC50 = 30 μM). PF-01247324 blocks Nav1.8 channels in a VSP-FRET assay using HEK293 cells (IC50 = 2.6 μM). In vivo, PF-01247324 (100 mg/kg) reduces phase 2 flinching in a rat model of formalin-induced persistent pain.{36847} It increases latency to lift the inflamed paw and latency to paw withdrawal in rat models of carrageenan-induced thermal hyperalgesia and mechanical hyperalgesia induced by complete Freund’s adjuvant (CFA), respectively.
Brand:CaymanSKU:22111 -Out of stock
PF-01247324 is a blocker of the tetrodotoxin-resistant (TTX-R) sodium channel Nav1.8 (IC50 = 0.19 μM for human Nav1.8).{36846} It is selective for Nav1.8 over Nav1.1, Nav1.2, Nav1.5, and Nav1.7 channels (IC50s = 13, 12.8, 9, and 19 μM, respectively) as well as ether-a-go-go (ERG) potassium channels (IC50 = 30 μM). PF-01247324 blocks Nav1.8 channels in a VSP-FRET assay using HEK293 cells (IC50 = 2.6 μM). In vivo, PF-01247324 (100 mg/kg) reduces phase 2 flinching in a rat model of formalin-induced persistent pain.{36847} It increases latency to lift the inflamed paw and latency to paw withdrawal in rat models of carrageenan-induced thermal hyperalgesia and mechanical hyperalgesia induced by complete Freund’s adjuvant (CFA), respectively.
Brand:CaymanSKU:22111 -Out of stock
PF-01247324 is a blocker of the tetrodotoxin-resistant (TTX-R) sodium channel Nav1.8 (IC50 = 0.19 μM for human Nav1.8).{36846} It is selective for Nav1.8 over Nav1.1, Nav1.2, Nav1.5, and Nav1.7 channels (IC50s = 13, 12.8, 9, and 19 μM, respectively) as well as ether-a-go-go (ERG) potassium channels (IC50 = 30 μM). PF-01247324 blocks Nav1.8 channels in a VSP-FRET assay using HEK293 cells (IC50 = 2.6 μM). In vivo, PF-01247324 (100 mg/kg) reduces phase 2 flinching in a rat model of formalin-induced persistent pain.{36847} It increases latency to lift the inflamed paw and latency to paw withdrawal in rat models of carrageenan-induced thermal hyperalgesia and mechanical hyperalgesia induced by complete Freund’s adjuvant (CFA), respectively.
Brand:CaymanSKU:22111 -Out of stock
PF-03550096 is a synthetic cannabinoid (CB) that selectively targets the peripheral CB2 receptor over the central CB1 receptor (Kis = 7.9 and 1,500 nM for human isoforms, respectively).{28936,28937} It shows similar selectivity for inhibiting forskolin-stimulated cAMP production in CHO cells expressing human CB1 and CB2 receptors (EC50s = 450 and 2.1 nM, respectively).{28937} PF-03550096 is orally bioavailable and significantly reduces colonic pain induced by 2,4,6-trinitrobenzene sulfonic acid in rats.{28937} This product is intended for forensic and research applications.
Brand:CaymanSKU:- PF-03550096 is a synthetic cannabinoid (CB) that selectively targets the peripheral CB2 receptor over the central CB1 receptor (Kis = 7.9 and 1,500 nM for human isoforms, respectively).{28936,28937} It shows similar selectivity for inhibiting forskolin-stimulated cAMP production in CHO cells expressing human CB1 and CB2 receptors (EC50s = 450 and 2.1 nM, respectively).{28937} PF-03550096 is orally bioavailable and significantly reduces colonic pain induced by 2,4,6-trinitrobenzene sulfonic acid in rats.{28937} This product is intended for forensic and research applications.
Brand:CaymanSKU:- PF-03550096 is a synthetic cannabinoid (CB) that selectively targets the peripheral CB2 receptor over the central CB1 receptor (Kis = 7.9 and 1,500 nM for human isoforms, respectively).{28936,28937} It shows similar selectivity for inhibiting forskolin-stimulated cAMP production in CHO cells expressing human CB1 and CB2 receptors (EC50s = 450 and 2.1 nM, respectively).{28937} PF-03550096 is orally bioavailable and significantly reduces colonic pain induced by 2,4,6-trinitrobenzene sulfonic acid in rats.{28937} This product is intended for forensic and research applications.
Brand:CaymanSKU:-
The Aurora kinases are a family of serine/threonine kinases that are key regulators of mitosis and cytokinesis. PF-03814735 is a reversible inhibitor of both Aurora A and B kinases with IC50 values of 0.8 and 5 nM, respectively, in in vitro activity assays.{22524} PF-03814735 also inhibits the kinases FLT1, FAK, TrkA, Met, and FGFR1 with IC50 values of 10, 22, 30, 100, and 100 nM, respectively.{22524} PF-03814735 inhibits cell proliferation of HCT116, HL-60, A549, and H125 tumor cell lines with IC50 values ranging from 42-150 nM and shows in vivo efficacy in an HCT116 tumor xenograft mouse model.{22524} PF-03814735 has been shown to be particularly sensitive towards inhibiting the growth of small cell lung cancer cell lines and other tumors driven by the Myc family genes.{22525}
Brand:CaymanSKU:- The Aurora kinases are a family of serine/threonine kinases that are key regulators of mitosis and cytokinesis. PF-03814735 is a reversible inhibitor of both Aurora A and B kinases with IC50 values of 0.8 and 5 nM, respectively, in in vitro activity assays.{22524} PF-03814735 also inhibits the kinases FLT1, FAK, TrkA, Met, and FGFR1 with IC50 values of 10, 22, 30, 100, and 100 nM, respectively.{22524} PF-03814735 inhibits cell proliferation of HCT116, HL-60, A549, and H125 tumor cell lines with IC50 values ranging from 42-150 nM and shows in vivo efficacy in an HCT116 tumor xenograft mouse model.{22524} PF-03814735 has been shown to be particularly sensitive towards inhibiting the growth of small cell lung cancer cell lines and other tumors driven by the Myc family genes.{22525}
Brand:CaymanSKU:- The Aurora kinases are a family of serine/threonine kinases that are key regulators of mitosis and cytokinesis. PF-03814735 is a reversible inhibitor of both Aurora A and B kinases with IC50 values of 0.8 and 5 nM, respectively, in in vitro activity assays.{22524} PF-03814735 also inhibits the kinases FLT1, FAK, TrkA, Met, and FGFR1 with IC50 values of 10, 22, 30, 100, and 100 nM, respectively.{22524} PF-03814735 inhibits cell proliferation of HCT116, HL-60, A549, and H125 tumor cell lines with IC50 values ranging from 42-150 nM and shows in vivo efficacy in an HCT116 tumor xenograft mouse model.{22524} PF-03814735 has been shown to be particularly sensitive towards inhibiting the growth of small cell lung cancer cell lines and other tumors driven by the Myc family genes.{22525}
Brand:CaymanSKU:- The Aurora kinases are a family of serine/threonine kinases that are key regulators of mitosis and cytokinesis. PF-03814735 is a reversible inhibitor of both Aurora A and B kinases with IC50 values of 0.8 and 5 nM, respectively, in in vitro activity assays.{22524} PF-03814735 also inhibits the kinases FLT1, FAK, TrkA, Met, and FGFR1 with IC50 values of 10, 22, 30, 100, and 100 nM, respectively.{22524} PF-03814735 inhibits cell proliferation of HCT116, HL-60, A549, and H125 tumor cell lines with IC50 values ranging from 42-150 nM and shows in vivo efficacy in an HCT116 tumor xenograft mouse model.{22524} PF-03814735 has been shown to be particularly sensitive towards inhibiting the growth of small cell lung cancer cell lines and other tumors driven by the Myc family genes.{22525}
Brand:CaymanSKU:-
MET is a proto-oncogene that encodes the hepatocyte growth factor receptor c-Met. It has normal roles in morphogenesis, migration, apoptosis, and angiogenesis. Dysregulation of c-Met occurs in many types of cancer. PF-04217903 is a class I c-Met kinase inhibitor (Ki = 4.8 nM) that demonstrates more than 1,000-fold selectivity for c-Met compared with more than 150 kinases.{29778} It can inhibit tumor cell proliferation, survival, and migration/invasion in MET-amplified cell lines in vitro (IC50s = 12-31 nM), and shows antitumor activity in in vivo tumor models harboring either MET gene amplification or a hepatocyte growth factor/c-Met autocrine loop.{29778} PF-04217903 underwent phase I clinical trials in 2010.{23657}
Brand:CaymanSKU:-Available on backorder
MET is a proto-oncogene that encodes the hepatocyte growth factor receptor c-Met. It has normal roles in morphogenesis, migration, apoptosis, and angiogenesis. Dysregulation of c-Met occurs in many types of cancer. PF-04217903 is a class I c-Met kinase inhibitor (Ki = 4.8 nM) that demonstrates more than 1,000-fold selectivity for c-Met compared with more than 150 kinases.{29778} It can inhibit tumor cell proliferation, survival, and migration/invasion in MET-amplified cell lines in vitro (IC50s = 12-31 nM), and shows antitumor activity in in vivo tumor models harboring either MET gene amplification or a hepatocyte growth factor/c-Met autocrine loop.{29778} PF-04217903 underwent phase I clinical trials in 2010.{23657}
Brand:CaymanSKU:-Available on backorder
MET is a proto-oncogene that encodes the hepatocyte growth factor receptor c-Met. It has normal roles in morphogenesis, migration, apoptosis, and angiogenesis. Dysregulation of c-Met occurs in many types of cancer. PF-04217903 is a class I c-Met kinase inhibitor (Ki = 4.8 nM) that demonstrates more than 1,000-fold selectivity for c-Met compared with more than 150 kinases.{29778} It can inhibit tumor cell proliferation, survival, and migration/invasion in MET-amplified cell lines in vitro (IC50s = 12-31 nM), and shows antitumor activity in in vivo tumor models harboring either MET gene amplification or a hepatocyte growth factor/c-Met autocrine loop.{29778} PF-04217903 underwent phase I clinical trials in 2010.{23657}
Brand:CaymanSKU:-Available on backorder
MET is a proto-oncogene that encodes the hepatocyte growth factor receptor c-Met. It has normal roles in morphogenesis, migration, apoptosis, and angiogenesis. Dysregulation of c-Met occurs in many types of cancer. PF-04217903 is a class I c-Met kinase inhibitor (Ki = 4.8 nM) that demonstrates more than 1,000-fold selectivity for c-Met compared with more than 150 kinases.{29778} It can inhibit tumor cell proliferation, survival, and migration/invasion in MET-amplified cell lines in vitro (IC50s = 12-31 nM), and shows antitumor activity in in vivo tumor models harboring either MET gene amplification or a hepatocyte growth factor/c-Met autocrine loop.{29778} PF-04217903 underwent phase I clinical trials in 2010.{23657}
Brand:CaymanSKU:-Available on backorder
Prostaglandin E2 (PGE2) evokes distinct responses through four different ‘E prostanoid’ (EP) receptors. EP2 is a G protein-coupled receptor which signals preferentially through Gs proteins. PF-04418948 is an orally active, potent, and selective EP2 receptor antagonist (IC50 = 16 nM).{22584} It is over a thousand-fold less active at other prostanoid receptors, including other EP receptors. PF-04418948 can be used in cells and tissues.{22583,22585} In rats, it significantly reduces the effects of the EP2-selective agonist butaprost on cutaneous blood flow when given orally.{22584}
Brand:CaymanSKU:- Prostaglandin E2 (PGE2) evokes distinct responses through four different ‘E prostanoid’ (EP) receptors. EP2 is a G protein-coupled receptor which signals preferentially through Gs proteins. PF-04418948 is an orally active, potent, and selective EP2 receptor antagonist (IC50 = 16 nM).{22584} It is over a thousand-fold less active at other prostanoid receptors, including other EP receptors. PF-04418948 can be used in cells and tissues.{22583,22585} In rats, it significantly reduces the effects of the EP2-selective agonist butaprost on cutaneous blood flow when given orally.{22584}
Brand:CaymanSKU:- Prostaglandin E2 (PGE2) evokes distinct responses through four different ‘E prostanoid’ (EP) receptors. EP2 is a G protein-coupled receptor which signals preferentially through Gs proteins. PF-04418948 is an orally active, potent, and selective EP2 receptor antagonist (IC50 = 16 nM).{22584} It is over a thousand-fold less active at other prostanoid receptors, including other EP receptors. PF-04418948 can be used in cells and tissues.{22583,22585} In rats, it significantly reduces the effects of the EP2-selective agonist butaprost on cutaneous blood flow when given orally.{22584}
Brand:CaymanSKU:- Prostaglandin E2 (PGE2) evokes distinct responses through four different ‘E prostanoid’ (EP) receptors. EP2 is a G protein-coupled receptor which signals preferentially through Gs proteins. PF-04418948 is an orally active, potent, and selective EP2 receptor antagonist (IC50 = 16 nM).{22584} It is over a thousand-fold less active at other prostanoid receptors, including other EP receptors. PF-04418948 can be used in cells and tissues.{22583,22585} In rats, it significantly reduces the effects of the EP2-selective agonist butaprost on cutaneous blood flow when given orally.{22584}
Brand:CaymanSKU:-
PF-04447943 is a brain-permeable phosphodiesterase (PDE) inhibitor that is selective for PDE9A (IC50 = 12 nM) over other PDEs (IC50s = >940 nM) in enzymatic assays of second messenger hydrolysis.{41434} It is over 1,000-fold more selective for PDE9A over 79 non-PDE targets, with the exception of the melatonin MT3/ML2 receptor (Ki = 3,800 nM). PF-04447943 also inhibits rat and rhesus monkey PDE9A (Kis = 18.1 and 4.5 nM, respectively).{41435} It increases neurite outgrowth and the density of synapsin puncta in primary rat hippocampal neurons when used at a concentration of 0.03 μM. PF-04447943 increases the cGMP level in the striatum and frontal cortex of mice and in the cerebrospinal fluid (CSF) of rats when administered at 10 and 1 mg/kg, respectively.{41434} It improves deficits in episodic memory induced by scopolamine (Item No. 14108) in rats and increases the time spent exploring the novel object in the novel object recognition (NOR) test when administered at a dose of 1 mg/kg. PF-04447943 (3.2 mg/kg) also improves spatial memory in the Morris water maze (MWM) and decreases the distance traveled to the hidden platform.
Brand:CaymanSKU:24299 - 1 mgAvailable on backorder
PF-04447943 is a brain-permeable phosphodiesterase (PDE) inhibitor that is selective for PDE9A (IC50 = 12 nM) over other PDEs (IC50s = >940 nM) in enzymatic assays of second messenger hydrolysis.{41434} It is over 1,000-fold more selective for PDE9A over 79 non-PDE targets, with the exception of the melatonin MT3/ML2 receptor (Ki = 3,800 nM). PF-04447943 also inhibits rat and rhesus monkey PDE9A (Kis = 18.1 and 4.5 nM, respectively).{41435} It increases neurite outgrowth and the density of synapsin puncta in primary rat hippocampal neurons when used at a concentration of 0.03 μM. PF-04447943 increases the cGMP level in the striatum and frontal cortex of mice and in the cerebrospinal fluid (CSF) of rats when administered at 10 and 1 mg/kg, respectively.{41434} It improves deficits in episodic memory induced by scopolamine (Item No. 14108) in rats and increases the time spent exploring the novel object in the novel object recognition (NOR) test when administered at a dose of 1 mg/kg. PF-04447943 (3.2 mg/kg) also improves spatial memory in the Morris water maze (MWM) and decreases the distance traveled to the hidden platform.
Brand:CaymanSKU:24299 - 10 mgAvailable on backorder
PF-04447943 is a brain-permeable phosphodiesterase (PDE) inhibitor that is selective for PDE9A (IC50 = 12 nM) over other PDEs (IC50s = >940 nM) in enzymatic assays of second messenger hydrolysis.{41434} It is over 1,000-fold more selective for PDE9A over 79 non-PDE targets, with the exception of the melatonin MT3/ML2 receptor (Ki = 3,800 nM). PF-04447943 also inhibits rat and rhesus monkey PDE9A (Kis = 18.1 and 4.5 nM, respectively).{41435} It increases neurite outgrowth and the density of synapsin puncta in primary rat hippocampal neurons when used at a concentration of 0.03 μM. PF-04447943 increases the cGMP level in the striatum and frontal cortex of mice and in the cerebrospinal fluid (CSF) of rats when administered at 10 and 1 mg/kg, respectively.{41434} It improves deficits in episodic memory induced by scopolamine (Item No. 14108) in rats and increases the time spent exploring the novel object in the novel object recognition (NOR) test when administered at a dose of 1 mg/kg. PF-04447943 (3.2 mg/kg) also improves spatial memory in the Morris water maze (MWM) and decreases the distance traveled to the hidden platform.
Brand:CaymanSKU:24299 - 25 mgAvailable on backorder
PF-04447943 is a brain-permeable phosphodiesterase (PDE) inhibitor that is selective for PDE9A (IC50 = 12 nM) over other PDEs (IC50s = >940 nM) in enzymatic assays of second messenger hydrolysis.{41434} It is over 1,000-fold more selective for PDE9A over 79 non-PDE targets, with the exception of the melatonin MT3/ML2 receptor (Ki = 3,800 nM). PF-04447943 also inhibits rat and rhesus monkey PDE9A (Kis = 18.1 and 4.5 nM, respectively).{41435} It increases neurite outgrowth and the density of synapsin puncta in primary rat hippocampal neurons when used at a concentration of 0.03 μM. PF-04447943 increases the cGMP level in the striatum and frontal cortex of mice and in the cerebrospinal fluid (CSF) of rats when administered at 10 and 1 mg/kg, respectively.{41434} It improves deficits in episodic memory induced by scopolamine (Item No. 14108) in rats and increases the time spent exploring the novel object in the novel object recognition (NOR) test when administered at a dose of 1 mg/kg. PF-04447943 (3.2 mg/kg) also improves spatial memory in the Morris water maze (MWM) and decreases the distance traveled to the hidden platform.
Brand:CaymanSKU:24299 - 5 mgAvailable on backorder
PF-04449613 is a phosphodiesterase 9A (PDE9A) inhibitor (IC50 = 22 nM).{54234} It is selective for PDE9A over PDE1C (IC50 = >1,000 nM), as well as over a variety of other PDEs, inhibiting PDE2-8, -10, and -11 activity by less than 30% in a panel of enzymes, ion channels, and transporters at 1 µM but does inhibit the human dopamine transporter (DAT; Ki = 293 nM). PF-04449613 (0.1-100 mg/kg, s.c.) increases cerebrospinal fluid (CSF) levels of cyclic GMP (cGMP) in rats. Subcutaneous administration of PF-04449613 (10 mg/kg) increases the rate of dendritic spine formation and elimination in mouse primary motor cortex pyramidal neurons in vivo.{54235} It increases the average running speed of mice in an accelerating rotarod task, indicating improved motor learning, at the same dose.
Brand:CaymanSKU:30946 - 1 mgAvailable on backorder
PF-04449613 is a phosphodiesterase 9A (PDE9A) inhibitor (IC50 = 22 nM).{54234} It is selective for PDE9A over PDE1C (IC50 = >1,000 nM), as well as over a variety of other PDEs, inhibiting PDE2-8, -10, and -11 activity by less than 30% in a panel of enzymes, ion channels, and transporters at 1 µM but does inhibit the human dopamine transporter (DAT; Ki = 293 nM). PF-04449613 (0.1-100 mg/kg, s.c.) increases cerebrospinal fluid (CSF) levels of cyclic GMP (cGMP) in rats. Subcutaneous administration of PF-04449613 (10 mg/kg) increases the rate of dendritic spine formation and elimination in mouse primary motor cortex pyramidal neurons in vivo.{54235} It increases the average running speed of mice in an accelerating rotarod task, indicating improved motor learning, at the same dose.
Brand:CaymanSKU:30946 - 10 mgAvailable on backorder
PF-04449613 is a phosphodiesterase 9A (PDE9A) inhibitor (IC50 = 22 nM).{54234} It is selective for PDE9A over PDE1C (IC50 = >1,000 nM), as well as over a variety of other PDEs, inhibiting PDE2-8, -10, and -11 activity by less than 30% in a panel of enzymes, ion channels, and transporters at 1 µM but does inhibit the human dopamine transporter (DAT; Ki = 293 nM). PF-04449613 (0.1-100 mg/kg, s.c.) increases cerebrospinal fluid (CSF) levels of cyclic GMP (cGMP) in rats. Subcutaneous administration of PF-04449613 (10 mg/kg) increases the rate of dendritic spine formation and elimination in mouse primary motor cortex pyramidal neurons in vivo.{54235} It increases the average running speed of mice in an accelerating rotarod task, indicating improved motor learning, at the same dose.
Brand:CaymanSKU:30946 - 25 mgAvailable on backorder
PF-04449613 is a phosphodiesterase 9A (PDE9A) inhibitor (IC50 = 22 nM).{54234} It is selective for PDE9A over PDE1C (IC50 = >1,000 nM), as well as over a variety of other PDEs, inhibiting PDE2-8, -10, and -11 activity by less than 30% in a panel of enzymes, ion channels, and transporters at 1 µM but does inhibit the human dopamine transporter (DAT; Ki = 293 nM). PF-04449613 (0.1-100 mg/kg, s.c.) increases cerebrospinal fluid (CSF) levels of cyclic GMP (cGMP) in rats. Subcutaneous administration of PF-04449613 (10 mg/kg) increases the rate of dendritic spine formation and elimination in mouse primary motor cortex pyramidal neurons in vivo.{54235} It increases the average running speed of mice in an accelerating rotarod task, indicating improved motor learning, at the same dose.
Brand:CaymanSKU:30946 - 5 mgAvailable on backorder
PF-04449913 is an orally available Hedgehog pathway inhibitor that acts by binding Smoothened (Smo) and blocking signal transduction (IC50 = 5 nM).{33585} It has been shown to attenuate leukemia stem cell self-renewal and cell cycle progression in primary acute myeloid leukemia cells and in an in vivo Drosophila model.{33586,33584}
Brand:CaymanSKU:9002936 - 1 mgAvailable on backorder
PF-04449913 is an orally available Hedgehog pathway inhibitor that acts by binding Smoothened (Smo) and blocking signal transduction (IC50 = 5 nM).{33585} It has been shown to attenuate leukemia stem cell self-renewal and cell cycle progression in primary acute myeloid leukemia cells and in an in vivo Drosophila model.{33586,33584}
Brand:CaymanSKU:9002936 - 10 mgAvailable on backorder
PF-04449913 is an orally available Hedgehog pathway inhibitor that acts by binding Smoothened (Smo) and blocking signal transduction (IC50 = 5 nM).{33585} It has been shown to attenuate leukemia stem cell self-renewal and cell cycle progression in primary acute myeloid leukemia cells and in an in vivo Drosophila model.{33586,33584}
Brand:CaymanSKU:9002936 - 25 mgAvailable on backorder
PF-04449913 is an orally available Hedgehog pathway inhibitor that acts by binding Smoothened (Smo) and blocking signal transduction (IC50 = 5 nM).{33585} It has been shown to attenuate leukemia stem cell self-renewal and cell cycle progression in primary acute myeloid leukemia cells and in an in vivo Drosophila model.{33586,33584}
Brand:CaymanSKU:9002936 - 5 mgAvailable on backorder
PF-04457845 is an orally active, irreversible inhibitor of fatty acid amide hydrolase (FAAH; IC50 = 7.2 nM) that is selective against other serine hydrolases.{20459} It is a covalent inhibitor that carbamylates the active site serine nucleophile of FAAH.{20459} In a rat model of inflammatory pain, oral administration of 0.1 mg/kg PF-04457845 has been shown to reduce inflammatory pain with efficacy comparable to that of naproxen.{20459}
Brand:CaymanSKU:-Available on backorder
PF-04457845 is an orally active, irreversible inhibitor of fatty acid amide hydrolase (FAAH; IC50 = 7.2 nM) that is selective against other serine hydrolases.{20459} It is a covalent inhibitor that carbamylates the active site serine nucleophile of FAAH.{20459} In a rat model of inflammatory pain, oral administration of 0.1 mg/kg PF-04457845 has been shown to reduce inflammatory pain with efficacy comparable to that of naproxen.{20459}
Brand:CaymanSKU:-Available on backorder
PF-04457845 is an orally active, irreversible inhibitor of fatty acid amide hydrolase (FAAH; IC50 = 7.2 nM) that is selective against other serine hydrolases.{20459} It is a covalent inhibitor that carbamylates the active site serine nucleophile of FAAH.{20459} In a rat model of inflammatory pain, oral administration of 0.1 mg/kg PF-04457845 has been shown to reduce inflammatory pain with efficacy comparable to that of naproxen.{20459}
Brand:CaymanSKU:-Available on backorder
PF-04457845 is an orally active, irreversible inhibitor of fatty acid amide hydrolase (FAAH; IC50 = 7.2 nM) that is selective against other serine hydrolases.{20459} It is a covalent inhibitor that carbamylates the active site serine nucleophile of FAAH.{20459} In a rat model of inflammatory pain, oral administration of 0.1 mg/kg PF-04457845 has been shown to reduce inflammatory pain with efficacy comparable to that of naproxen.{20459}
Brand:CaymanSKU:-Available on backorder
Acyl-CoA:diacylglycerol acyltransferase-1 (DGAT-1) catalyzes the final committed step in the biosynthesis of triglycerides and has potential roles in obesity, diabetes, and atherosclerosis.{12021,15816,10960} PF-04620110 is a potent inhibitor of DGAT-1 (IC50 = 19 nM) that is without effect on DGAT-2.{26854} It has high oral bioavailability (100%) in rats, with a moderate half-life of 6.8 hours.{26854} PF-04620110 significantly blocks an increase in plasma triglyceride levels following a corn oil bolus in rats.{26854}
Brand:CaymanSKU:-Out of stock
Acyl-CoA:diacylglycerol acyltransferase-1 (DGAT-1) catalyzes the final committed step in the biosynthesis of triglycerides and has potential roles in obesity, diabetes, and atherosclerosis.{12021,15816,10960} PF-04620110 is a potent inhibitor of DGAT-1 (IC50 = 19 nM) that is without effect on DGAT-2.{26854} It has high oral bioavailability (100%) in rats, with a moderate half-life of 6.8 hours.{26854} PF-04620110 significantly blocks an increase in plasma triglyceride levels following a corn oil bolus in rats.{26854}
Brand:CaymanSKU:-Out of stock
Acyl-CoA:diacylglycerol acyltransferase-1 (DGAT-1) catalyzes the final committed step in the biosynthesis of triglycerides and has potential roles in obesity, diabetes, and atherosclerosis.{12021,15816,10960} PF-04620110 is a potent inhibitor of DGAT-1 (IC50 = 19 nM) that is without effect on DGAT-2.{26854} It has high oral bioavailability (100%) in rats, with a moderate half-life of 6.8 hours.{26854} PF-04620110 significantly blocks an increase in plasma triglyceride levels following a corn oil bolus in rats.{26854}
Brand:CaymanSKU:-Out of stock
P70 ribosomal S6 kinase (S6K1) is a serine/threonine kinase which is activated by insulin and growth factors through PI3K and mTORC1 signaling pathways. PF-04708671 is a specific, cell-permeable inhibitor of S6K1 (IC50 = 160 nM).{22617} It does not inhibit S6K2, MSK, or RSK, or many other unrelated kinases, under conditions in which it inhibits S6K1 activity.{22617} It is useful in evaluating the role of S6K1 and, indirectly, mTORC1, in cell signaling.{22618,22616}
Brand:CaymanSKU:- P70 ribosomal S6 kinase (S6K1) is a serine/threonine kinase which is activated by insulin and growth factors through PI3K and mTORC1 signaling pathways. PF-04708671 is a specific, cell-permeable inhibitor of S6K1 (IC50 = 160 nM).{22617} It does not inhibit S6K2, MSK, or RSK, or many other unrelated kinases, under conditions in which it inhibits S6K1 activity.{22617} It is useful in evaluating the role of S6K1 and, indirectly, mTORC1, in cell signaling.{22618,22616}
Brand:CaymanSKU:- P70 ribosomal S6 kinase (S6K1) is a serine/threonine kinase which is activated by insulin and growth factors through PI3K and mTORC1 signaling pathways. PF-04708671 is a specific, cell-permeable inhibitor of S6K1 (IC50 = 160 nM).{22617} It does not inhibit S6K2, MSK, or RSK, or many other unrelated kinases, under conditions in which it inhibits S6K1 activity.{22617} It is useful in evaluating the role of S6K1 and, indirectly, mTORC1, in cell signaling.{22618,22616}
Brand:CaymanSKU:- P70 ribosomal S6 kinase (S6K1) is a serine/threonine kinase which is activated by insulin and growth factors through PI3K and mTORC1 signaling pathways. PF-04708671 is a specific, cell-permeable inhibitor of S6K1 (IC50 = 160 nM).{22617} It does not inhibit S6K2, MSK, or RSK, or many other unrelated kinases, under conditions in which it inhibits S6K1 activity.{22617} It is useful in evaluating the role of S6K1 and, indirectly, mTORC1, in cell signaling.{22618,22616}
Brand:CaymanSKU:-
PF-04859989 is an inhibitor of kynurenine aminotransferase II (KAT II; IC50s = 0.032 and 0.263 µM for human and rat recombinant enzymes, respectively).{59036} It is selective for KAT II over KAT I, -III, and -IV (IC50s = 21.6, 107, and >50 µM, respectively). In vivo, PF-04859989 (10 mg/kg, s.c.) reduces basal striatum, prefrontal cortex, and hippocampus kynurenic acid levels in rats. It prevents ketamine- or amphetamine-induced disruption of auditory gating in rats, as well as prevents ketamine-induced deficits in spatial memory in non-human primates. PF-04859989 also inhibits glutamate oxaloacetate transaminase 1 (GOT1; IC50 = 8 µM) and reduces the viability of PaTu 8988t and PaTu 8902 pancreatic cancer cells in a concentration-dependent manner.{59037}
Brand:CaymanSKU:31383 - 1 mgAvailable on backorder
PF-04859989 is an inhibitor of kynurenine aminotransferase II (KAT II; IC50s = 0.032 and 0.263 µM for human and rat recombinant enzymes, respectively).{59036} It is selective for KAT II over KAT I, -III, and -IV (IC50s = 21.6, 107, and >50 µM, respectively). In vivo, PF-04859989 (10 mg/kg, s.c.) reduces basal striatum, prefrontal cortex, and hippocampus kynurenic acid levels in rats. It prevents ketamine- or amphetamine-induced disruption of auditory gating in rats, as well as prevents ketamine-induced deficits in spatial memory in non-human primates. PF-04859989 also inhibits glutamate oxaloacetate transaminase 1 (GOT1; IC50 = 8 µM) and reduces the viability of PaTu 8988t and PaTu 8902 pancreatic cancer cells in a concentration-dependent manner.{59037}
Brand:CaymanSKU:31383 - 10 mgAvailable on backorder
PF-04859989 is an inhibitor of kynurenine aminotransferase II (KAT II; IC50s = 0.032 and 0.263 µM for human and rat recombinant enzymes, respectively).{59036} It is selective for KAT II over KAT I, -III, and -IV (IC50s = 21.6, 107, and >50 µM, respectively). In vivo, PF-04859989 (10 mg/kg, s.c.) reduces basal striatum, prefrontal cortex, and hippocampus kynurenic acid levels in rats. It prevents ketamine- or amphetamine-induced disruption of auditory gating in rats, as well as prevents ketamine-induced deficits in spatial memory in non-human primates. PF-04859989 also inhibits glutamate oxaloacetate transaminase 1 (GOT1; IC50 = 8 µM) and reduces the viability of PaTu 8988t and PaTu 8902 pancreatic cancer cells in a concentration-dependent manner.{59037}
Brand:CaymanSKU:31383 - 25 mgAvailable on backorder
PF-04859989 is an inhibitor of kynurenine aminotransferase II (KAT II; IC50s = 0.032 and 0.263 µM for human and rat recombinant enzymes, respectively).{59036} It is selective for KAT II over KAT I, -III, and -IV (IC50s = 21.6, 107, and >50 µM, respectively). In vivo, PF-04859989 (10 mg/kg, s.c.) reduces basal striatum, prefrontal cortex, and hippocampus kynurenic acid levels in rats. It prevents ketamine- or amphetamine-induced disruption of auditory gating in rats, as well as prevents ketamine-induced deficits in spatial memory in non-human primates. PF-04859989 also inhibits glutamate oxaloacetate transaminase 1 (GOT1; IC50 = 8 µM) and reduces the viability of PaTu 8988t and PaTu 8902 pancreatic cancer cells in a concentration-dependent manner.{59037}
Brand:CaymanSKU:31383 - 5 mgAvailable on backorder
PF-04929113 is a prodrug for the Hsp90 inhibitor, PF-04958473 (SNX-2112; Item No. 22359), which binds both Hsp90α and Hsp90β with an IC50 value of 30 nM.{31149,31150} The prodrug, PF-04929113, is rapidly absorbed and converted into the active inhibitor after oral administration.{31150} The active inhibitor causes degradation of Hsp90 client proteins, including HER2, and reduces phosphorylation of downstream kinases, including Akt and ERK1/2, leading to apoptosis in cancer cells.{31149,31152} Oral administration of the prodrug, PF-04929113, reduces tumor growth and prolongs survival in mouse models of multiple myeloma and prostate cancer.{31152,31151}
Brand:CaymanSKU:-Available on backorder
PF-04929113 is a prodrug for the Hsp90 inhibitor, PF-04958473 (SNX-2112; Item No. 22359), which binds both Hsp90α and Hsp90β with an IC50 value of 30 nM.{31149,31150} The prodrug, PF-04929113, is rapidly absorbed and converted into the active inhibitor after oral administration.{31150} The active inhibitor causes degradation of Hsp90 client proteins, including HER2, and reduces phosphorylation of downstream kinases, including Akt and ERK1/2, leading to apoptosis in cancer cells.{31149,31152} Oral administration of the prodrug, PF-04929113, reduces tumor growth and prolongs survival in mouse models of multiple myeloma and prostate cancer.{31152,31151}
Brand:CaymanSKU:-Available on backorder
PF-04929113 is a prodrug for the Hsp90 inhibitor, PF-04958473 (SNX-2112; Item No. 22359), which binds both Hsp90α and Hsp90β with an IC50 value of 30 nM.{31149,31150} The prodrug, PF-04929113, is rapidly absorbed and converted into the active inhibitor after oral administration.{31150} The active inhibitor causes degradation of Hsp90 client proteins, including HER2, and reduces phosphorylation of downstream kinases, including Akt and ERK1/2, leading to apoptosis in cancer cells.{31149,31152} Oral administration of the prodrug, PF-04929113, reduces tumor growth and prolongs survival in mouse models of multiple myeloma and prostate cancer.{31152,31151}
Brand:CaymanSKU:-Available on backorder
PF-04929113 is a prodrug for the Hsp90 inhibitor, PF-04958473 (SNX-2112; Item No. 22359), which binds both Hsp90α and Hsp90β with an IC50 value of 30 nM.{31149,31150} The prodrug, PF-04929113, is rapidly absorbed and converted into the active inhibitor after oral administration.{31150} The active inhibitor causes degradation of Hsp90 client proteins, including HER2, and reduces phosphorylation of downstream kinases, including Akt and ERK1/2, leading to apoptosis in cancer cells.{31149,31152} Oral administration of the prodrug, PF-04929113, reduces tumor growth and prolongs survival in mouse models of multiple myeloma and prostate cancer.{31152,31151}
Brand:CaymanSKU:-Available on backorder
PF-04981517 is a potent, time-dependent inhibitor of the cytochrome P450 (CYP450) isoform CYP3A4 (IC50 = 30 nM).{22614} It is less effective against CYP3A5 and CYP3A7 (IC50s = 17 and 70 μM, respectively).{22614} PF-04981517 will be useful for understanding the relative roles of CYP3A4 and CYP3A5 in drug metabolism.
Brand:CaymanSKU:- PF-04981517 is a potent, time-dependent inhibitor of the cytochrome P450 (CYP450) isoform CYP3A4 (IC50 = 30 nM).{22614} It is less effective against CYP3A5 and CYP3A7 (IC50s = 17 and 70 μM, respectively).{22614} PF-04981517 will be useful for understanding the relative roles of CYP3A4 and CYP3A5 in drug metabolism.
Brand:CaymanSKU:- PF-04981517 is a potent, time-dependent inhibitor of the cytochrome P450 (CYP450) isoform CYP3A4 (IC50 = 30 nM).{22614} It is less effective against CYP3A5 and CYP3A7 (IC50s = 17 and 70 μM, respectively).{22614} PF-04981517 will be useful for understanding the relative roles of CYP3A4 and CYP3A5 in drug metabolism.
Brand:CaymanSKU:- PF-04981517 is a potent, time-dependent inhibitor of the cytochrome P450 (CYP450) isoform CYP3A4 (IC50 = 30 nM).{22614} It is less effective against CYP3A5 and CYP3A7 (IC50s = 17 and 70 μM, respectively).{22614} PF-04981517 will be useful for understanding the relative roles of CYP3A4 and CYP3A5 in drug metabolism.
Brand:CaymanSKU:-