Chemicals
Showing 31651–31800 of 41137 results
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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}
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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}
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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}
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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}
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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}
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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}
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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}
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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}
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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}
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PF-4840154 is a transient receptor potential ankyrin 1 (TRPA1) agonist.{53404} It induces calcium influx into HEK293 cells expressing recombinant human or rat TRPA1 (EC50s = 23 and 97 nM, respectively). Intraplantar injection of PF-4840154 (30 nmol) increases paw licking time in mice in a TRPA1-dependent manner.
Brand:CaymanSKU:28915 - 1 mgAvailable on backorder
PF-4840154 is a transient receptor potential ankyrin 1 (TRPA1) agonist.{53404} It induces calcium influx into HEK293 cells expressing recombinant human or rat TRPA1 (EC50s = 23 and 97 nM, respectively). Intraplantar injection of PF-4840154 (30 nmol) increases paw licking time in mice in a TRPA1-dependent manner.
Brand:CaymanSKU:28915 - 10 mgAvailable on backorder
PF-4840154 is a transient receptor potential ankyrin 1 (TRPA1) agonist.{53404} It induces calcium influx into HEK293 cells expressing recombinant human or rat TRPA1 (EC50s = 23 and 97 nM, respectively). Intraplantar injection of PF-4840154 (30 nmol) increases paw licking time in mice in a TRPA1-dependent manner.
Brand:CaymanSKU:28915 - 25 mgAvailable on backorder
PF-4840154 is a transient receptor potential ankyrin 1 (TRPA1) agonist.{53404} It induces calcium influx into HEK293 cells expressing recombinant human or rat TRPA1 (EC50s = 23 and 97 nM, respectively). Intraplantar injection of PF-4840154 (30 nmol) increases paw licking time in mice in a TRPA1-dependent manner.
Brand:CaymanSKU:28915 - 5 mgAvailable on backorder
PF-4989216 is an orally bioavailable broad-spectrum PI3K inhibitor (IC50s = 2, 142, 65, 1, and 110 nM for p110α, p110β, p110γ, p110δ, and VPS34, respectively).{32573} It inhibits the cell viability of small-cell lung cancer (SCLC) cells with a mutation in PIK3CA, blocking PI3K downstream signaling and inducing apoptosis.{32573} PF-4989216 prevents tumor growth of SCLC cells harboring PIK3CA mutation in mice.{32573}
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PF-4989216 is an orally bioavailable broad-spectrum PI3K inhibitor (IC50s = 2, 142, 65, 1, and 110 nM for p110α, p110β, p110γ, p110δ, and VPS34, respectively).{32573} It inhibits the cell viability of small-cell lung cancer (SCLC) cells with a mutation in PIK3CA, blocking PI3K downstream signaling and inducing apoptosis.{32573} PF-4989216 prevents tumor growth of SCLC cells harboring PIK3CA mutation in mice.{32573}
Brand:CaymanSKU:-Available on backorder
PF-4989216 is an orally bioavailable broad-spectrum PI3K inhibitor (IC50s = 2, 142, 65, 1, and 110 nM for p110α, p110β, p110γ, p110δ, and VPS34, respectively).{32573} It inhibits the cell viability of small-cell lung cancer (SCLC) cells with a mutation in PIK3CA, blocking PI3K downstream signaling and inducing apoptosis.{32573} PF-4989216 prevents tumor growth of SCLC cells harboring PIK3CA mutation in mice.{32573}
Brand:CaymanSKU:-Available on backorder
PF-4989216 is an orally bioavailable broad-spectrum PI3K inhibitor (IC50s = 2, 142, 65, 1, and 110 nM for p110α, p110β, p110γ, p110δ, and VPS34, respectively).{32573} It inhibits the cell viability of small-cell lung cancer (SCLC) cells with a mutation in PIK3CA, blocking PI3K downstream signaling and inducing apoptosis.{32573} PF-4989216 prevents tumor growth of SCLC cells harboring PIK3CA mutation in mice.{32573}
Brand:CaymanSKU:-Available on backorder
PF-543 is a potent inhibitor of sphingosine kinase 1 (SPHK1; IC50 = 2 nM) that inhibits sphingosine-1-phosphate (S1P) binding to human recombinant SPHK1 (Ki = 3.6 nM).{27977} It is selective for SPHK1 over SPHK2 (IC50 = 356 nM) as well as a panel of protein and lipid kinases and S1P receptors at a concentration of 10 µM. PF-543 inhibits the formation of S1P in 1483 cells and human whole blood (EC50s = 8.4 and 26.7 nM, respectively). In vivo, PF-543 prevents sickling, hemolysis, and inflammation in a transgenic mouse model of sickle cell disease.{27978}
Brand:CaymanSKU:-Out of stock
PF-543 is a potent inhibitor of sphingosine kinase 1 (SPHK1; IC50 = 2 nM) that inhibits sphingosine-1-phosphate (S1P) binding to human recombinant SPHK1 (Ki = 3.6 nM).{27977} It is selective for SPHK1 over SPHK2 (IC50 = 356 nM) as well as a panel of protein and lipid kinases and S1P receptors at a concentration of 10 µM. PF-543 inhibits the formation of S1P in 1483 cells and human whole blood (EC50s = 8.4 and 26.7 nM, respectively). In vivo, PF-543 prevents sickling, hemolysis, and inflammation in a transgenic mouse model of sickle cell disease.{27978}
Brand:CaymanSKU:-Out of stock
PF-543 is a potent inhibitor of sphingosine kinase 1 (SPHK1; IC50 = 2 nM) that inhibits sphingosine-1-phosphate (S1P) binding to human recombinant SPHK1 (Ki = 3.6 nM).{27977} It is selective for SPHK1 over SPHK2 (IC50 = 356 nM) as well as a panel of protein and lipid kinases and S1P receptors at a concentration of 10 µM. PF-543 inhibits the formation of S1P in 1483 cells and human whole blood (EC50s = 8.4 and 26.7 nM, respectively). In vivo, PF-543 prevents sickling, hemolysis, and inflammation in a transgenic mouse model of sickle cell disease.{27978}
Brand:CaymanSKU:-Out of stock
PF-543 is a potent inhibitor of sphingosine kinase 1 (SPHK1; IC50 = 2 nM) that inhibits sphingosine-1-phosphate (S1P) binding to human recombinant SPHK1 (Ki = 3.6 nM).{27977} It is selective for SPHK1 over SPHK2 (IC50 = 356 nM) as well as a panel of protein and lipid kinases and S1P receptors at a concentration of 10 µM. PF-543 inhibits the formation of S1P in 1483 cells and human whole blood (EC50s = 8.4 and 26.7 nM, respectively). In vivo, PF-543 prevents sickling, hemolysis, and inflammation in a transgenic mouse model of sickle cell disease.{27978}
Brand:CaymanSKU:-Out of stock
Focal adhesion kinase (FAK) and proline-rich tyrosine kinase 2 (PYK2) are non-receptor tyrosine kinases that constitute the FAK subfamily and play a vital role in many oncogenic pathways.{15630} PF-562271 is an ATP-competitive, reversible inhibitor of FAK (IC50 = 1.5 nM) that demonstrates 10-fold reduced potency for PYK2 (IC50 = 14 nM) and >100-fold selectivity against other protein kinases.{29911} PF-562271 inhibits FAK phosphorylation with an EC50 value of 93 ng/ml in glioblastoma-bearing mice and has been shown to regress tumors in multiple xenograft models.{29911,29912}
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Focal adhesion kinase (FAK) and proline-rich tyrosine kinase 2 (PYK2) are non-receptor tyrosine kinases that constitute the FAK subfamily and play a vital role in many oncogenic pathways.{15630} PF-562271 is an ATP-competitive, reversible inhibitor of FAK (IC50 = 1.5 nM) that demonstrates 10-fold reduced potency for PYK2 (IC50 = 14 nM) and >100-fold selectivity against other protein kinases.{29911} PF-562271 inhibits FAK phosphorylation with an EC50 value of 93 ng/ml in glioblastoma-bearing mice and has been shown to regress tumors in multiple xenograft models.{29911,29912}
Brand:CaymanSKU:-Available on backorder
Focal adhesion kinase (FAK) and proline-rich tyrosine kinase 2 (PYK2) are non-receptor tyrosine kinases that constitute the FAK subfamily and play a vital role in many oncogenic pathways.{15630} PF-562271 is an ATP-competitive, reversible inhibitor of FAK (IC50 = 1.5 nM) that demonstrates 10-fold reduced potency for PYK2 (IC50 = 14 nM) and >100-fold selectivity against other protein kinases.{29911} PF-562271 inhibits FAK phosphorylation with an EC50 value of 93 ng/ml in glioblastoma-bearing mice and has been shown to regress tumors in multiple xenograft models.{29911,29912}
Brand:CaymanSKU:-Available on backorder
Focal adhesion kinase (FAK) and proline-rich tyrosine kinase 2 (PYK2) are non-receptor tyrosine kinases that constitute the FAK subfamily and play a vital role in many oncogenic pathways.{15630} PF-562271 is an ATP-competitive, reversible inhibitor of FAK (IC50 = 1.5 nM) that demonstrates 10-fold reduced potency for PYK2 (IC50 = 14 nM) and >100-fold selectivity against other protein kinases.{29911} PF-562271 inhibits FAK phosphorylation with an EC50 value of 93 ng/ml in glioblastoma-bearing mice and has been shown to regress tumors in multiple xenograft models.{29911,29912}
Brand:CaymanSKU:-Available on backorder
Focal adhesion kinases (FAKs) are non-receptor tyrosine kinases that play roles in regulating diverse processes, including cell adhesion, spreading, migration, proliferation, and apoptosis.{15630} They are overexpressed in many types of cancer. PF-573228 inhibits FAK with IC50 values of 4 and 30-100 nM for a purified recombinant catalytic fragment of FAK and in cultured cells, respectively.{14924} It is 50-250-fold selective for FAK over other protein kinases.{14924} PF-573228 can inhibit chemotactic and haptotactic migration of cells as well as prevent focal adhesion turnover.{28528}
Brand:CaymanSKU:-Focal adhesion kinases (FAKs) are non-receptor tyrosine kinases that play roles in regulating diverse processes, including cell adhesion, spreading, migration, proliferation, and apoptosis.{15630} They are overexpressed in many types of cancer. PF-573228 inhibits FAK with IC50 values of 4 and 30-100 nM for a purified recombinant catalytic fragment of FAK and in cultured cells, respectively.{14924} It is 50-250-fold selective for FAK over other protein kinases.{14924} PF-573228 can inhibit chemotactic and haptotactic migration of cells as well as prevent focal adhesion turnover.{28528}
Brand:CaymanSKU:-Focal adhesion kinases (FAKs) are non-receptor tyrosine kinases that play roles in regulating diverse processes, including cell adhesion, spreading, migration, proliferation, and apoptosis.{15630} They are overexpressed in many types of cancer. PF-573228 inhibits FAK with IC50 values of 4 and 30-100 nM for a purified recombinant catalytic fragment of FAK and in cultured cells, respectively.{14924} It is 50-250-fold selective for FAK over other protein kinases.{14924} PF-573228 can inhibit chemotactic and haptotactic migration of cells as well as prevent focal adhesion turnover.{28528}
Brand:CaymanSKU:-Focal adhesion kinases (FAKs) are non-receptor tyrosine kinases that play roles in regulating diverse processes, including cell adhesion, spreading, migration, proliferation, and apoptosis.{15630} They are overexpressed in many types of cancer. PF-573228 inhibits FAK with IC50 values of 4 and 30-100 nM for a purified recombinant catalytic fragment of FAK and in cultured cells, respectively.{14924} It is 50-250-fold selective for FAK over other protein kinases.{14924} PF-573228 can inhibit chemotactic and haptotactic migration of cells as well as prevent focal adhesion turnover.{28528}
Brand:CaymanSKU:-Fatty acid amide hydrolase (FAAH) is the enzyme responsible for hydrolysis and inactivation of fatty acid amides including anandamide and oleamide. PF-622 is a potent, time-dependent, irreversible FAAH inhibitor with IC50 values of 0.99 and 0.033 µM when preincubated with human recombinant FAAH for 5 and 60 minutes, respectively.{15092} Activity-based profiling of various human and murine tissue proteome samples revealed that PF-622 is highly selective for FAAH relative to other serine hydrolases, showing no discernable off-site activity up to 500 µM.{15092}
Brand:CaymanSKU:10010907 - 1 mgAvailable on backorder
Fatty acid amide hydrolase (FAAH) is the enzyme responsible for hydrolysis and inactivation of fatty acid amides including anandamide and oleamide. PF-622 is a potent, time-dependent, irreversible FAAH inhibitor with IC50 values of 0.99 and 0.033 µM when preincubated with human recombinant FAAH for 5 and 60 minutes, respectively.{15092} Activity-based profiling of various human and murine tissue proteome samples revealed that PF-622 is highly selective for FAAH relative to other serine hydrolases, showing no discernable off-site activity up to 500 µM.{15092}
Brand:CaymanSKU:10010907 - 10 mgAvailable on backorder
Fatty acid amide hydrolase (FAAH) is the enzyme responsible for hydrolysis and inactivation of fatty acid amides including anandamide and oleamide. PF-622 is a potent, time-dependent, irreversible FAAH inhibitor with IC50 values of 0.99 and 0.033 µM when preincubated with human recombinant FAAH for 5 and 60 minutes, respectively.{15092} Activity-based profiling of various human and murine tissue proteome samples revealed that PF-622 is highly selective for FAAH relative to other serine hydrolases, showing no discernable off-site activity up to 500 µM.{15092}
Brand:CaymanSKU:10010907 - 5 mgAvailable on backorder
Fatty acid amide hydrolase (FAAH) is the enzyme responsible for hydrolysis and inactivation of fatty acid amides including anandamide and oleamide. PF-622 is a potent, time-dependent, irreversible FAAH inhibitor with IC50 values of 0.99 and 0.033 µM when preincubated with human recombinant FAAH for 5 and 60 minutes, respectively.{15092} Activity-based profiling of various human and murine tissue proteome samples revealed that PF-622 is highly selective for FAAH relative to other serine hydrolases, showing no discernable off-site activity up to 500 µM.{15092}
Brand:CaymanSKU:10010907 - 50 mgAvailable on backorder
PF-6274484 is an inhibitor of the EGF receptor (EGFR; IC50s = 0.18 and 0.14 nM for wild-type EGFR and inhibitor-resistant EGFRL858R/T790M, respectively).{36569} It inhibits the autophosphorylation of wild-type EGFR in A549 cells and EGFRL858R/T790M in H1975 cells (IC50s = 5.8 and 6.6 nM, respectively).
Brand:CaymanSKU:22698 -Out of stock
PF-6274484 is an inhibitor of the EGF receptor (EGFR; IC50s = 0.18 and 0.14 nM for wild-type EGFR and inhibitor-resistant EGFRL858R/T790M, respectively).{36569} It inhibits the autophosphorylation of wild-type EGFR in A549 cells and EGFRL858R/T790M in H1975 cells (IC50s = 5.8 and 6.6 nM, respectively).
Brand:CaymanSKU:22698 -Out of stock
PF-6274484 is an inhibitor of the EGF receptor (EGFR; IC50s = 0.18 and 0.14 nM for wild-type EGFR and inhibitor-resistant EGFRL858R/T790M, respectively).{36569} It inhibits the autophosphorylation of wild-type EGFR in A549 cells and EGFRL858R/T790M in H1975 cells (IC50s = 5.8 and 6.6 nM, respectively).
Brand:CaymanSKU:22698 -Out of stock
The casein kinase 1 (CK1) family of kinases regulate diverse processes, particularly related to circadian rhythms and sensitivity to amphetamines.{23082,23080} PF-670462 is a potent inhibitor of the CK1 isoforms CK1ε and CK1δ (IC50 = 7.7 and 14 nM, respectively).{23083} It less effectively inhibits a wide variety of related or common kinases.{23083} Through its effects on CK1, PF-670462 disrupts circadian rhythms in cells and animals.{23083,23081} It also blocks the locomotor response to amphetamines in mice.{23080}
Brand:CaymanSKU:-The casein kinase 1 (CK1) family of kinases regulate diverse processes, particularly related to circadian rhythms and sensitivity to amphetamines.{23082,23080} PF-670462 is a potent inhibitor of the CK1 isoforms CK1ε and CK1δ (IC50 = 7.7 and 14 nM, respectively).{23083} It less effectively inhibits a wide variety of related or common kinases.{23083} Through its effects on CK1, PF-670462 disrupts circadian rhythms in cells and animals.{23083,23081} It also blocks the locomotor response to amphetamines in mice.{23080}
Brand:CaymanSKU:-Fatty acid amide hydrolase (FAAH) is the enzyme responsible for hydrolysis and inactivation of fatty acid amides including anandamide and oleamide. PF-750 is a potent, time-dependent, irreversible FAAH inhibitor with IC50 values of 0.6 and 0.016 µM when preincubated with recombinant human FAAH for 5 and 60 minutes, respectively.{15092} Activity-based profiling of various human and murine tissue proteome samples revealed that PF-750 is highly selective for FAAH relative to other serine hydrolases, showing no discernable off-site activity up to 500 µM.{15092}
Brand:CaymanSKU:10010908 - 1 mgAvailable on backorder
Fatty acid amide hydrolase (FAAH) is the enzyme responsible for hydrolysis and inactivation of fatty acid amides including anandamide and oleamide. PF-750 is a potent, time-dependent, irreversible FAAH inhibitor with IC50 values of 0.6 and 0.016 µM when preincubated with recombinant human FAAH for 5 and 60 minutes, respectively.{15092} Activity-based profiling of various human and murine tissue proteome samples revealed that PF-750 is highly selective for FAAH relative to other serine hydrolases, showing no discernable off-site activity up to 500 µM.{15092}
Brand:CaymanSKU:10010908 - 10 mgAvailable on backorder
Fatty acid amide hydrolase (FAAH) is the enzyme responsible for hydrolysis and inactivation of fatty acid amides including anandamide and oleamide. PF-750 is a potent, time-dependent, irreversible FAAH inhibitor with IC50 values of 0.6 and 0.016 µM when preincubated with recombinant human FAAH for 5 and 60 minutes, respectively.{15092} Activity-based profiling of various human and murine tissue proteome samples revealed that PF-750 is highly selective for FAAH relative to other serine hydrolases, showing no discernable off-site activity up to 500 µM.{15092}
Brand:CaymanSKU:10010908 - 5 mgAvailable on backorder
Fatty acid amide hydrolase (FAAH) is the enzyme responsible for hydrolysis and inactivation of fatty acid amides including anandamide and oleamide. PF-750 is a potent, time-dependent, irreversible FAAH inhibitor with IC50 values of 0.6 and 0.016 µM when preincubated with recombinant human FAAH for 5 and 60 minutes, respectively.{15092} Activity-based profiling of various human and murine tissue proteome samples revealed that PF-750 is highly selective for FAAH relative to other serine hydrolases, showing no discernable off-site activity up to 500 µM.{15092}
Brand:CaymanSKU:10010908 - 50 mgAvailable on backorder
Autotaxin converts lysophosphatidylcholine to lysophosphatidic acid (LPA), which can mediate changes in cell proliferation, angiogenesis, and cytokine secretion.{21340} PF-8380 is a potent inhibitor of autotaxin (IC50 = 2.8 nM in an enzyme assay), the enzyme that converts lysophosphatidylcholine to lysophosphatidic acid (LPA).{21340} It reverses MMP-13 expression induced by leptin in human OA chondrocytes when used at a concentration of 10 µM.{35249} PF-8380 (30 mg/kg) reduces LPA production by >95% following carrageenan-induced inflammation in rats and inhibits autotaxin activity in human whole blood (IC50 = 101 nM).{21340}
Brand:CaymanSKU:12018 - 1 mgAvailable on backorder
Autotaxin converts lysophosphatidylcholine to lysophosphatidic acid (LPA), which can mediate changes in cell proliferation, angiogenesis, and cytokine secretion.{21340} PF-8380 is a potent inhibitor of autotaxin (IC50 = 2.8 nM in an enzyme assay), the enzyme that converts lysophosphatidylcholine to lysophosphatidic acid (LPA).{21340} It reverses MMP-13 expression induced by leptin in human OA chondrocytes when used at a concentration of 10 µM.{35249} PF-8380 (30 mg/kg) reduces LPA production by >95% following carrageenan-induced inflammation in rats and inhibits autotaxin activity in human whole blood (IC50 = 101 nM).{21340}
Brand:CaymanSKU:12018 - 10 mgAvailable on backorder
Autotaxin converts lysophosphatidylcholine to lysophosphatidic acid (LPA), which can mediate changes in cell proliferation, angiogenesis, and cytokine secretion.{21340} PF-8380 is a potent inhibitor of autotaxin (IC50 = 2.8 nM in an enzyme assay), the enzyme that converts lysophosphatidylcholine to lysophosphatidic acid (LPA).{21340} It reverses MMP-13 expression induced by leptin in human OA chondrocytes when used at a concentration of 10 µM.{35249} PF-8380 (30 mg/kg) reduces LPA production by >95% following carrageenan-induced inflammation in rats and inhibits autotaxin activity in human whole blood (IC50 = 101 nM).{21340}
Brand:CaymanSKU:12018 - 25 mgAvailable on backorder
Autotaxin converts lysophosphatidylcholine to lysophosphatidic acid (LPA), which can mediate changes in cell proliferation, angiogenesis, and cytokine secretion.{21340} PF-8380 is a potent inhibitor of autotaxin (IC50 = 2.8 nM in an enzyme assay), the enzyme that converts lysophosphatidylcholine to lysophosphatidic acid (LPA).{21340} It reverses MMP-13 expression induced by leptin in human OA chondrocytes when used at a concentration of 10 µM.{35249} PF-8380 (30 mg/kg) reduces LPA production by >95% following carrageenan-induced inflammation in rats and inhibits autotaxin activity in human whole blood (IC50 = 101 nM).{21340}
Brand:CaymanSKU:12018 - 5 mgAvailable on backorder
Microsomal prostaglandin E synthase-1 (mPGES-1) converts the COX product prostaglandin H2 (PGH2; Item No. 17020) into the biologically active PGE2 (Item No. 14010).{7229} Like COX-2, the expression of mPGES-1 is induced in response to pro-inflammatory mediators, including LPS, IL-1β, and TNF-α.{11537} PF-9184 is a potent inhibitor of mPGES-1 (IC50 = 16.5 nM for recombinant human enzyme).{30680} It displays at least 6,500-fold selectivity for mPGES-1 over COX-1 and COX-2. PF-9184 blocks the synthesis of PGE2 in LPS-treated human whole blood and in IL-1β-stimulated fibroblasts (IC50s = 0.4-5 µM).{30723,30679}
Brand:CaymanSKU:-Available on backorder
Microsomal prostaglandin E synthase-1 (mPGES-1) converts the COX product prostaglandin H2 (PGH2; Item No. 17020) into the biologically active PGE2 (Item No. 14010).{7229} Like COX-2, the expression of mPGES-1 is induced in response to pro-inflammatory mediators, including LPS, IL-1β, and TNF-α.{11537} PF-9184 is a potent inhibitor of mPGES-1 (IC50 = 16.5 nM for recombinant human enzyme).{30680} It displays at least 6,500-fold selectivity for mPGES-1 over COX-1 and COX-2. PF-9184 blocks the synthesis of PGE2 in LPS-treated human whole blood and in IL-1β-stimulated fibroblasts (IC50s = 0.4-5 µM).{30723,30679}
Brand:CaymanSKU:-Available on backorder
Microsomal prostaglandin E synthase-1 (mPGES-1) converts the COX product prostaglandin H2 (PGH2; Item No. 17020) into the biologically active PGE2 (Item No. 14010).{7229} Like COX-2, the expression of mPGES-1 is induced in response to pro-inflammatory mediators, including LPS, IL-1β, and TNF-α.{11537} PF-9184 is a potent inhibitor of mPGES-1 (IC50 = 16.5 nM for recombinant human enzyme).{30680} It displays at least 6,500-fold selectivity for mPGES-1 over COX-1 and COX-2. PF-9184 blocks the synthesis of PGE2 in LPS-treated human whole blood and in IL-1β-stimulated fibroblasts (IC50s = 0.4-5 µM).{30723,30679}
Brand:CaymanSKU:-Available on backorder
Microsomal prostaglandin E synthase-1 (mPGES-1) converts the COX product prostaglandin H2 (PGH2; Item No. 17020) into the biologically active PGE2 (Item No. 14010).{7229} Like COX-2, the expression of mPGES-1 is induced in response to pro-inflammatory mediators, including LPS, IL-1β, and TNF-α.{11537} PF-9184 is a potent inhibitor of mPGES-1 (IC50 = 16.5 nM for recombinant human enzyme).{30680} It displays at least 6,500-fold selectivity for mPGES-1 over COX-1 and COX-2. PF-9184 blocks the synthesis of PGE2 in LPS-treated human whole blood and in IL-1β-stimulated fibroblasts (IC50s = 0.4-5 µM).{30723,30679}
Brand:CaymanSKU:-Available on backorder
PF-9366 is an inhibitor of methionine adenosyltransferase 2A (Mat2A; IC50 = 420 nM for S-adenosyl-L-methionine (SAM) production in an enzyme assay).{54128} It is selective for Mat2A over a panel of neurotransmitter transporters, phosphodiesterases, ion channels, and G protein-coupled receptors, as well as a panel of 39 kinases at 10 µM. PF-9366 inhibits SAM production in H520 lung carcinoma cells (IC50 = 1.2 µM) and Huh7 hepatocellular carcinoma cells (IC50 = 225 nM).
Brand:CaymanSKU:30782 - 10 mgAvailable on backorder
PF-9366 is an inhibitor of methionine adenosyltransferase 2A (Mat2A; IC50 = 420 nM for S-adenosyl-L-methionine (SAM) production in an enzyme assay).{54128} It is selective for Mat2A over a panel of neurotransmitter transporters, phosphodiesterases, ion channels, and G protein-coupled receptors, as well as a panel of 39 kinases at 10 µM. PF-9366 inhibits SAM production in H520 lung carcinoma cells (IC50 = 1.2 µM) and Huh7 hepatocellular carcinoma cells (IC50 = 225 nM).
Brand:CaymanSKU:30782 - 25 mgAvailable on backorder
PF-9366 is an inhibitor of methionine adenosyltransferase 2A (Mat2A; IC50 = 420 nM for S-adenosyl-L-methionine (SAM) production in an enzyme assay).{54128} It is selective for Mat2A over a panel of neurotransmitter transporters, phosphodiesterases, ion channels, and G protein-coupled receptors, as well as a panel of 39 kinases at 10 µM. PF-9366 inhibits SAM production in H520 lung carcinoma cells (IC50 = 1.2 µM) and Huh7 hepatocellular carcinoma cells (IC50 = 225 nM).
Brand:CaymanSKU:30782 - 5 mgAvailable on backorder
PF-998425 is a non-steroidal androgen receptor antagonist (IC50 = 43 nM in a cell-based assay).{57126} It binds to the androgen receptor (IC50 = 37 nM in a radioligand binding assay) and is selective for the androgen receptor over the progesterone receptor (IC50 = >10,000 nM). Topical administration of PF-998425 (3% twice per day) increases hair growth in a mouse model of hair growth, as well as reduces ear sebum in male Syrian golden hamsters (ED50 = 0.4% twice per day).
Brand:CaymanSKU:31442 - 1 mgAvailable on backorder
PF-998425 is a non-steroidal androgen receptor antagonist (IC50 = 43 nM in a cell-based assay).{57126} It binds to the androgen receptor (IC50 = 37 nM in a radioligand binding assay) and is selective for the androgen receptor over the progesterone receptor (IC50 = >10,000 nM). Topical administration of PF-998425 (3% twice per day) increases hair growth in a mouse model of hair growth, as well as reduces ear sebum in male Syrian golden hamsters (ED50 = 0.4% twice per day).
Brand:CaymanSKU:31442 - 10 mgAvailable on backorder
PF-998425 is a non-steroidal androgen receptor antagonist (IC50 = 43 nM in a cell-based assay).{57126} It binds to the androgen receptor (IC50 = 37 nM in a radioligand binding assay) and is selective for the androgen receptor over the progesterone receptor (IC50 = >10,000 nM). Topical administration of PF-998425 (3% twice per day) increases hair growth in a mouse model of hair growth, as well as reduces ear sebum in male Syrian golden hamsters (ED50 = 0.4% twice per day).
Brand:CaymanSKU:31442 - 5 mgAvailable on backorder