Chemicals

Showing 31651–31800 of 41137 results

  • 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.  

     

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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.  

     

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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.  

     

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    Cayman
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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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  • 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}  

     

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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}  

     

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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}  

     

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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}  

     

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  • 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.  

     

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    SKU:21965 -

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  • 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.  

     

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    Cayman
    SKU:21965 -

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  • 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.  

     

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    Cayman
    SKU:21965 -

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  • 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.  

     

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    Cayman
    SKU:21965 -

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  • 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}  

     

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  • 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}  

     

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  • 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}  

     

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    Cayman
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  • 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}  

     

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  • 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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  • 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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  • 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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    Cayman
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  • 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.  

     

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    SKU:22768 -

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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.  

     

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    Cayman
    SKU:22768 -

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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.  

     

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    Cayman
    SKU:22768 -

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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.  

     

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    Cayman
    SKU:22768 -

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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}  

     

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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}  

     

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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}  

     

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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}  

     

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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}  

     

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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-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.  

     

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    SKU:28915 - 1 mg

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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.  

     

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    SKU:28915 - 10 mg

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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.  

     

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    SKU:28915 - 25 mg

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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.  

     

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    SKU:28915 - 5 mg

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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}  

     

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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}  

     

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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}  

     

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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}  

     

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  • 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}  

     

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  • 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}  

     

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  • 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}  

     

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  • 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}  

     

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    SKU:-

    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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    Cayman
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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}  

     

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    Cayman
    SKU:-

    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}  

     

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    Cayman
    SKU:-

    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}  

     

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    Cayman
    SKU:-

    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}  

     

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    Cayman
    SKU:-
  • 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:
    Cayman
    SKU:-
  • 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:
    Cayman
    SKU:-
  • 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:
    Cayman
    SKU:-
  • 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}  

     

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    Cayman
    SKU:10010907 - 1 mg

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  • 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:
    Cayman
    SKU:10010907 - 10 mg

    Available 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:
    Cayman
    SKU:10010907 - 5 mg

    Available 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:
    Cayman
    SKU:10010907 - 50 mg

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  • 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:
    Cayman
    SKU: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:
    Cayman
    SKU: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:
    Cayman
    SKU: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}  

     

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    Cayman
    SKU:-
  • 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}  

     

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    Cayman
    SKU:-
  • 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:
    Cayman
    SKU:10010908 - 1 mg

    Available 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:
    Cayman
    SKU:10010908 - 10 mg

    Available 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:
    Cayman
    SKU:10010908 - 5 mg

    Available 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:
    Cayman
    SKU:10010908 - 50 mg

    Available 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:
    Cayman
    SKU:12018 - 1 mg

    Available 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:
    Cayman
    SKU:12018 - 10 mg

    Available 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:
    Cayman
    SKU:12018 - 25 mg

    Available 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:
    Cayman
    SKU:12018 - 5 mg

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  • 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}  

     

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    Cayman
    SKU:-

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  • 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}  

     

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    Cayman
    SKU:-

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  • 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}  

     

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    Cayman
    SKU:-

    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}  

     

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    Cayman
    SKU:-

    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:
    Cayman
    SKU:30782 - 10 mg

    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:
    Cayman
    SKU:30782 - 25 mg

    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:
    Cayman
    SKU:30782 - 5 mg

    Available 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:
    Cayman
    SKU:31442 - 1 mg

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  • 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:
    Cayman
    SKU:31442 - 10 mg

    Available 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:
    Cayman
    SKU:31442 - 5 mg

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  • CREB-binding protein (CBP) and E1A-associated protein p300 are transcriptional co-activators that modulate DNA replication, DNA repair, cell growth, transformation, and development.{22609,22611} Both CBP and p300 contain bromodomains, which mediate their binding to acetylated lysine residues on histones and other proteins.{21581} PF-CBP1 is an inhibitor of the CBP and p300 bromodomains (IC50s = 125 and 363 nM, respectively).{30310} It displays greater than 100-fold selectivity for the bromodomain of CBP over those of BRD4 and a panel of other proteins.{30310} PF-CBP1 reduces the expression of inflammatory cytokines by LPS-stimulated primary macrophages.{30310} It also suppresses the expression of RGS4 (regulator of G protein signaling 4) in primary cortical neurons.{30310}  

     

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    Cayman
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  • CREB-binding protein (CBP) and E1A-associated protein p300 are transcriptional co-activators that modulate DNA replication, DNA repair, cell growth, transformation, and development.{22609,22611} Both CBP and p300 contain bromodomains, which mediate their binding to acetylated lysine residues on histones and other proteins.{21581} PF-CBP1 is an inhibitor of the CBP and p300 bromodomains (IC50s = 125 and 363 nM, respectively).{30310} It displays greater than 100-fold selectivity for the bromodomain of CBP over those of BRD4 and a panel of other proteins.{30310} PF-CBP1 reduces the expression of inflammatory cytokines by LPS-stimulated primary macrophages.{30310} It also suppresses the expression of RGS4 (regulator of G protein signaling 4) in primary cortical neurons.{30310}  

     

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    Cayman
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  • CREB-binding protein (CBP) and E1A-associated protein p300 are transcriptional co-activators that modulate DNA replication, DNA repair, cell growth, transformation, and development.{22609,22611} Both CBP and p300 contain bromodomains, which mediate their binding to acetylated lysine residues on histones and other proteins.{21581} PF-CBP1 is an inhibitor of the CBP and p300 bromodomains (IC50s = 125 and 363 nM, respectively).{30310} It displays greater than 100-fold selectivity for the bromodomain of CBP over those of BRD4 and a panel of other proteins.{30310} PF-CBP1 reduces the expression of inflammatory cytokines by LPS-stimulated primary macrophages.{30310} It also suppresses the expression of RGS4 (regulator of G protein signaling 4) in primary cortical neurons.{30310}  

     

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    Cayman
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  • Bromodomains recognize acetylated lysine residues and recruit regulatory complexes to acetylated nucleosomes, thereby controlling chromatin structure and gene expression. The isolated individual or tandem bromodomains of bromodomain-containing protein (BRD) 2 and BRD4 bind acetylated histone tails, which couples histone acetylation marks to the transcriptional regulation of target promoters. Small molecule inhibitors of bromodomain interactions hold promise as useful therapeutics for human disease.{19044,19929,19950} PFI-1 is a BET bromodomain inhibitor that exhibits inhibitory activity at BRD2 and BRD4. In an AlphaScreen assay it has been shown to inhibit BRD2 bromodomain 2 and BRD4 bromodomain 1 with IC50 values of 98 nM and 0.22 μM, respectively. See the Structural Genomics Consortium (SGC) website for more information.  

     

    Brand:
    Cayman
    SKU:11155 - 1 mg

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  • Bromodomains recognize acetylated lysine residues and recruit regulatory complexes to acetylated nucleosomes, thereby controlling chromatin structure and gene expression. The isolated individual or tandem bromodomains of bromodomain-containing protein (BRD) 2 and BRD4 bind acetylated histone tails, which couples histone acetylation marks to the transcriptional regulation of target promoters. Small molecule inhibitors of bromodomain interactions hold promise as useful therapeutics for human disease.{19044,19929,19950} PFI-1 is a BET bromodomain inhibitor that exhibits inhibitory activity at BRD2 and BRD4. In an AlphaScreen assay it has been shown to inhibit BRD2 bromodomain 2 and BRD4 bromodomain 1 with IC50 values of 98 nM and 0.22 μM, respectively. See the Structural Genomics Consortium (SGC) website for more information.  

     

    Brand:
    Cayman
    SKU:11155 - 10 mg

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  • Bromodomains recognize acetylated lysine residues and recruit regulatory complexes to acetylated nucleosomes, thereby controlling chromatin structure and gene expression. The isolated individual or tandem bromodomains of bromodomain-containing protein (BRD) 2 and BRD4 bind acetylated histone tails, which couples histone acetylation marks to the transcriptional regulation of target promoters. Small molecule inhibitors of bromodomain interactions hold promise as useful therapeutics for human disease.{19044,19929,19950} PFI-1 is a BET bromodomain inhibitor that exhibits inhibitory activity at BRD2 and BRD4. In an AlphaScreen assay it has been shown to inhibit BRD2 bromodomain 2 and BRD4 bromodomain 1 with IC50 values of 98 nM and 0.22 μM, respectively. See the Structural Genomics Consortium (SGC) website for more information.  

     

    Brand:
    Cayman
    SKU:11155 - 25 mg

    Available on backorder

  • Bromodomains recognize acetylated lysine residues and recruit regulatory complexes to acetylated nucleosomes, thereby controlling chromatin structure and gene expression. The isolated individual or tandem bromodomains of bromodomain-containing protein (BRD) 2 and BRD4 bind acetylated histone tails, which couples histone acetylation marks to the transcriptional regulation of target promoters. Small molecule inhibitors of bromodomain interactions hold promise as useful therapeutics for human disease.{19044,19929,19950} PFI-1 is a BET bromodomain inhibitor that exhibits inhibitory activity at BRD2 and BRD4. In an AlphaScreen assay it has been shown to inhibit BRD2 bromodomain 2 and BRD4 bromodomain 1 with IC50 values of 98 nM and 0.22 μM, respectively. See the Structural Genomics Consortium (SGC) website for more information.  

     

    Brand:
    Cayman
    SKU:11155 - 5 mg

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  • The SWI/SNF-related, Matrix-associated, Actin-dependent Regulator of Chromatin (SMARC) proteins integrate into complexes that remodel chromatin.{25296} The SMARC family A (SMARCA) members SMARCA2 (also known as BRM) and SMARCA4 (BRG1) are helicases that contain structurally-related bromodomains for binding acetylated lysine residues on target proteins.{25295,25294} The protein polybromo-1 (PB1, BRG1-associated factor) contains six bromodomains, but only the fifth (PB1(5)) shares the same structural signature as those of SMARCA2 and SMARCA4.{25295} PFI-3 is a probe that binds avidly to the structurally-similar SMARCA4 bromodomain and PB1(bromodomain 5) with Kd values of 89 and 48 nM, respectively. Evaluation of interactions of PFI-3 with different classes of bromodomains using thermal stability assay indicates that PFI-3 interacts selectively with bromodomains from SMARCA2 and SMARCA4 as well as the fifth domain of PB1. Similarly, PFI-1 (Item No. 11155) does not interact with a panel of kinases. See the Structural Genomics Consortium (SGC) website for more information.  

     

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    Cayman
    SKU:-
  • The SWI/SNF-related, Matrix-associated, Actin-dependent Regulator of Chromatin (SMARC) proteins integrate into complexes that remodel chromatin.{25296} The SMARC family A (SMARCA) members SMARCA2 (also known as BRM) and SMARCA4 (BRG1) are helicases that contain structurally-related bromodomains for binding acetylated lysine residues on target proteins.{25295,25294} The protein polybromo-1 (PB1, BRG1-associated factor) contains six bromodomains, but only the fifth (PB1(5)) shares the same structural signature as those of SMARCA2 and SMARCA4.{25295} PFI-3 is a probe that binds avidly to the structurally-similar SMARCA4 bromodomain and PB1(bromodomain 5) with Kd values of 89 and 48 nM, respectively. Evaluation of interactions of PFI-3 with different classes of bromodomains using thermal stability assay indicates that PFI-3 interacts selectively with bromodomains from SMARCA2 and SMARCA4 as well as the fifth domain of PB1. Similarly, PFI-1 (Item No. 11155) does not interact with a panel of kinases. See the Structural Genomics Consortium (SGC) website for more information.  

     

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  • The SWI/SNF-related, Matrix-associated, Actin-dependent Regulator of Chromatin (SMARC) proteins integrate into complexes that remodel chromatin.{25296} The SMARC family A (SMARCA) members SMARCA2 (also known as BRM) and SMARCA4 (BRG1) are helicases that contain structurally-related bromodomains for binding acetylated lysine residues on target proteins.{25295,25294} The protein polybromo-1 (PB1, BRG1-associated factor) contains six bromodomains, but only the fifth (PB1(5)) shares the same structural signature as those of SMARCA2 and SMARCA4.{25295} PFI-3 is a probe that binds avidly to the structurally-similar SMARCA4 bromodomain and PB1(bromodomain 5) with Kd values of 89 and 48 nM, respectively. Evaluation of interactions of PFI-3 with different classes of bromodomains using thermal stability assay indicates that PFI-3 interacts selectively with bromodomains from SMARCA2 and SMARCA4 as well as the fifth domain of PB1. Similarly, PFI-1 (Item No. 11155) does not interact with a panel of kinases. See the Structural Genomics Consortium (SGC) website for more information.  

     

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    Cayman
    SKU:-
  • The SWI/SNF-related, Matrix-associated, Actin-dependent Regulator of Chromatin (SMARC) proteins integrate into complexes that remodel chromatin.{25296} The SMARC family A (SMARCA) members SMARCA2 (also known as BRM) and SMARCA4 (BRG1) are helicases that contain structurally-related bromodomains for binding acetylated lysine residues on target proteins.{25295,25294} The protein polybromo-1 (PB1, BRG1-associated factor) contains six bromodomains, but only the fifth (PB1(5)) shares the same structural signature as those of SMARCA2 and SMARCA4.{25295} PFI-3 is a probe that binds avidly to the structurally-similar SMARCA4 bromodomain and PB1(bromodomain 5) with Kd values of 89 and 48 nM, respectively. Evaluation of interactions of PFI-3 with different classes of bromodomains using thermal stability assay indicates that PFI-3 interacts selectively with bromodomains from SMARCA2 and SMARCA4 as well as the fifth domain of PB1. Similarly, PFI-1 (Item No. 11155) does not interact with a panel of kinases. See the Structural Genomics Consortium (SGC) website for more information.  

     

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  • The bromodomain and PHD finger-containing (BRPF) proteins are scaffolding components of chromatin-binding MOZ/MORF histone acetyltransferase complexes, which have activity as transcriptional regulators.{21051,29177} BRPF1, aka BR140 or Peregrin, is important for maintaining Hox gene expression and the development of multiple tissues, axial skeleton, and the hematopoietic system.{29177} PFI-4 is a chemical probe that specifically binds to the bromodomain of BRPF1 (Kd = 13 nM), inhibiting binding to tri-acetylated histone 4 (residues 1-21).{29176} It has much lower affinity for bromodomain 1 of BRD4 (Kd = >50 µM) and is selective for BRPF1 over BRPF2 and BRPF3.{29176} PFI-4 is potent in cells, with an IC50 value of 250 nM. See the Structural Genomics Consortium (SGC) website for more information.  

     

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  • The bromodomain and PHD finger-containing (BRPF) proteins are scaffolding components of chromatin-binding MOZ/MORF histone acetyltransferase complexes, which have activity as transcriptional regulators.{21051,29177} BRPF1, aka BR140 or Peregrin, is important for maintaining Hox gene expression and the development of multiple tissues, axial skeleton, and the hematopoietic system.{29177} PFI-4 is a chemical probe that specifically binds to the bromodomain of BRPF1 (Kd = 13 nM), inhibiting binding to tri-acetylated histone 4 (residues 1-21).{29176} It has much lower affinity for bromodomain 1 of BRD4 (Kd = >50 µM) and is selective for BRPF1 over BRPF2 and BRPF3.{29176} PFI-4 is potent in cells, with an IC50 value of 250 nM. See the Structural Genomics Consortium (SGC) website for more information.  

     

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  • The bromodomain and PHD finger-containing (BRPF) proteins are scaffolding components of chromatin-binding MOZ/MORF histone acetyltransferase complexes, which have activity as transcriptional regulators.{21051,29177} BRPF1, aka BR140 or Peregrin, is important for maintaining Hox gene expression and the development of multiple tissues, axial skeleton, and the hematopoietic system.{29177} PFI-4 is a chemical probe that specifically binds to the bromodomain of BRPF1 (Kd = 13 nM), inhibiting binding to tri-acetylated histone 4 (residues 1-21).{29176} It has much lower affinity for bromodomain 1 of BRD4 (Kd = >50 µM) and is selective for BRPF1 over BRPF2 and BRPF3.{29176} PFI-4 is potent in cells, with an IC50 value of 250 nM. See the Structural Genomics Consortium (SGC) website for more information.  

     

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    Cayman
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  • The bromodomain and PHD finger-containing (BRPF) proteins are scaffolding components of chromatin-binding MOZ/MORF histone acetyltransferase complexes, which have activity as transcriptional regulators.{21051,29177} BRPF1, aka BR140 or Peregrin, is important for maintaining Hox gene expression and the development of multiple tissues, axial skeleton, and the hematopoietic system.{29177} PFI-4 is a chemical probe that specifically binds to the bromodomain of BRPF1 (Kd = 13 nM), inhibiting binding to tri-acetylated histone 4 (residues 1-21).{29176} It has much lower affinity for bromodomain 1 of BRD4 (Kd = >50 µM) and is selective for BRPF1 over BRPF2 and BRPF3.{29176} PFI-4 is potent in cells, with an IC50 value of 250 nM. See the Structural Genomics Consortium (SGC) website for more information.  

     

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  • 6-Phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 (PFKFB3) is a bifunctional enzyme that contains distinct domains for the phosphorylation of fructose 6-phosphate and the dephosphorylation of fructose 2,6-bisphosphate. PFKFB3 protein expression is elevated in most tumor types.{30751,27006} PFK15 is a selective inhibitor of PFKFB3 (IC50 = 207 nM).{30752} It has no significant inhibitory effect on any member of a panel of 96 other kinases, and does not inhibit purified 6-phosphofructo-1-kinase, hexokinase, phosphoglucose isomerase, or PFKFB4. PFK15 rapidly induces apoptosis in transformed cells, suppresses glucose uptake and growth of Lewis lung carcinomas in syngeneic mice, and yields antitumor effects in human xenograft models of cancer in athymic mice.{30752}  

     

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  • 6-Phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 (PFKFB3) is a bifunctional enzyme that contains distinct domains for the phosphorylation of fructose 6-phosphate and the dephosphorylation of fructose 2,6-bisphosphate. PFKFB3 protein expression is elevated in most tumor types.{30751,27006} PFK15 is a selective inhibitor of PFKFB3 (IC50 = 207 nM).{30752} It has no significant inhibitory effect on any member of a panel of 96 other kinases, and does not inhibit purified 6-phosphofructo-1-kinase, hexokinase, phosphoglucose isomerase, or PFKFB4. PFK15 rapidly induces apoptosis in transformed cells, suppresses glucose uptake and growth of Lewis lung carcinomas in syngeneic mice, and yields antitumor effects in human xenograft models of cancer in athymic mice.{30752}  

     

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  • 6-Phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 (PFKFB3) is a bifunctional enzyme that contains distinct domains for the phosphorylation of fructose 6-phosphate and the dephosphorylation of fructose 2,6-bisphosphate. PFKFB3 protein expression is elevated in most tumor types.{30751,27006} PFK15 is a selective inhibitor of PFKFB3 (IC50 = 207 nM).{30752} It has no significant inhibitory effect on any member of a panel of 96 other kinases, and does not inhibit purified 6-phosphofructo-1-kinase, hexokinase, phosphoglucose isomerase, or PFKFB4. PFK15 rapidly induces apoptosis in transformed cells, suppresses glucose uptake and growth of Lewis lung carcinomas in syngeneic mice, and yields antitumor effects in human xenograft models of cancer in athymic mice.{30752}  

     

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    Cayman
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  • 6-Phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 (PFKFB3) is a bifunctional enzyme that contains distinct domains for the phosphorylation of fructose 6-phosphate and the dephosphorylation of fructose 2,6-bisphosphate. PFKFB3 protein expression is elevated in most tumor types.{30751,27006} PFK15 is a selective inhibitor of PFKFB3 (IC50 = 207 nM).{30752} It has no significant inhibitory effect on any member of a panel of 96 other kinases, and does not inhibit purified 6-phosphofructo-1-kinase, hexokinase, phosphoglucose isomerase, or PFKFB4. PFK15 rapidly induces apoptosis in transformed cells, suppresses glucose uptake and growth of Lewis lung carcinomas in syngeneic mice, and yields antitumor effects in human xenograft models of cancer in athymic mice.{30752}  

     

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  • PFK158 is an inhibitor of 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 (PFKFB3; IC50 = 137 nM for human recombinant PFKFB3).{37211} It inhibits PFKFB3 and glycolysis in Jurkat cells (IC50s = 1.6 and 0.847 μM, respectively). PFK158 inhibits the growth of leukemia cells in vitro (IC50 = 0.33 μM for Jurkat cells) and reduces tumor volume in CT-26 murine colon carcinoma syngeneic model and a BxPC-3 pancreatic cancer mouse xenograft model. PFK158 also enhances activity of the anti-CTLA-4 antibody in the B16/F10 mouse model of melanoma.{37212}  

     

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    Cayman
    SKU:22987 - 10 mg

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  • PFK158 is an inhibitor of 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 (PFKFB3; IC50 = 137 nM for human recombinant PFKFB3).{37211} It inhibits PFKFB3 and glycolysis in Jurkat cells (IC50s = 1.6 and 0.847 μM, respectively). PFK158 inhibits the growth of leukemia cells in vitro (IC50 = 0.33 μM for Jurkat cells) and reduces tumor volume in CT-26 murine colon carcinoma syngeneic model and a BxPC-3 pancreatic cancer mouse xenograft model. PFK158 also enhances activity of the anti-CTLA-4 antibody in the B16/F10 mouse model of melanoma.{37212}  

     

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    Cayman
    SKU:22987 - 25 mg

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  • PFK158 is an inhibitor of 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 (PFKFB3; IC50 = 137 nM for human recombinant PFKFB3).{37211} It inhibits PFKFB3 and glycolysis in Jurkat cells (IC50s = 1.6 and 0.847 μM, respectively). PFK158 inhibits the growth of leukemia cells in vitro (IC50 = 0.33 μM for Jurkat cells) and reduces tumor volume in CT-26 murine colon carcinoma syngeneic model and a BxPC-3 pancreatic cancer mouse xenograft model. PFK158 also enhances activity of the anti-CTLA-4 antibody in the B16/F10 mouse model of melanoma.{37212}  

     

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    Cayman
    SKU:22987 - 5 mg

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  • PG-01037 is a selective dopamine D3 receptor antagonist (Kis = 0.7, 93, and 375 nM for HEK293 cells expressing human D3, D2, and D4 receptors, respectively).{34174} It inhibits quinpirole-induced stimulation of mitogenesis in CHO cells expressing human dopamine D3 receptors (EC50 = 3 nM). PG-01037 (32 mg/kg) reduces progressive-ratio methamphetamine self-administration in rats allowed extended access.{36955} It reduces loss of dopaminergic neurons in the substantia nigra pars compacta and improves motor performance in the coat-hanger test in a mouse model of Parkinson’s disease induced by MPTP.{36956}  

     

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    Cayman
    SKU:22079 -

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  • PG-01037 is a selective dopamine D3 receptor antagonist (Kis = 0.7, 93, and 375 nM for HEK293 cells expressing human D3, D2, and D4 receptors, respectively).{34174} It inhibits quinpirole-induced stimulation of mitogenesis in CHO cells expressing human dopamine D3 receptors (EC50 = 3 nM). PG-01037 (32 mg/kg) reduces progressive-ratio methamphetamine self-administration in rats allowed extended access.{36955} It reduces loss of dopaminergic neurons in the substantia nigra pars compacta and improves motor performance in the coat-hanger test in a mouse model of Parkinson’s disease induced by MPTP.{36956}  

     

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    Cayman
    SKU:22079 -

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  • PG-01037 is a selective dopamine D3 receptor antagonist (Kis = 0.7, 93, and 375 nM for HEK293 cells expressing human D3, D2, and D4 receptors, respectively).{34174} It inhibits quinpirole-induced stimulation of mitogenesis in CHO cells expressing human dopamine D3 receptors (EC50 = 3 nM). PG-01037 (32 mg/kg) reduces progressive-ratio methamphetamine self-administration in rats allowed extended access.{36955} It reduces loss of dopaminergic neurons in the substantia nigra pars compacta and improves motor performance in the coat-hanger test in a mouse model of Parkinson’s disease induced by MPTP.{36956}  

     

    Brand:
    Cayman
    SKU:22079 -

    Out of stock

  • PG-01037 is a selective dopamine D3 receptor antagonist (Kis = 0.7, 93, and 375 nM for HEK293 cells expressing human D3, D2, and D4 receptors, respectively).{34174} It inhibits quinpirole-induced stimulation of mitogenesis in CHO cells expressing human dopamine D3 receptors (EC50 = 3 nM). PG-01037 (32 mg/kg) reduces progressive-ratio methamphetamine self-administration in rats allowed extended access.{36955} It reduces loss of dopaminergic neurons in the substantia nigra pars compacta and improves motor performance in the coat-hanger test in a mouse model of Parkinson’s disease induced by MPTP.{36956}  

     

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    Cayman
    SKU:22079 -

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  • Prostaglandin D2 (PGD2) plays a pharmacological role in allergic and asthmatic anaphylaxis, normal physiological sleep and lowering of body temperature, as well as inhibits platelet aggregation and relaxes vascular smooth muscle.{580} PGDM is a major urinary metabolite of PGD2 with a unique lower sidechain that readily undergoes reversible cyclization.{35} It is used as a biomarker to assess endogenous production of PGD2.  

     

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    Cayman
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  • Prostaglandin D2 (PGD2) plays a pharmacological role in allergic and asthmatic anaphylaxis, normal physiological sleep and lowering of body temperature, as well as inhibits platelet aggregation and relaxes vascular smooth muscle.{580} PGDM is a major urinary metabolite of PGD2 with a unique lower sidechain that readily undergoes reversible cyclization.{35} It is used as a biomarker to assess endogenous production of PGD2.  

     

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    Cayman
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  • Prostaglandin D2 (PGD2) plays a pharmacological role in allergic and asthmatic anaphylaxis, normal physiological sleep and lowering of body temperature, as well as inhibits platelet aggregation and relaxes vascular smooth muscle.{580} PGDM is a major urinary metabolite of PGD2 with a unique lower sidechain that readily undergoes reversible cyclization.{35} It is used as a biomarker to assess endogenous production of PGD2.  

     

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    Cayman
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  • PGP-4008 is a selective inhibitor of P-glycoprotein (P-gp) that does not affect the activity of multidrug resistance-related protein 1 (MRP1).{32706,32707} It is effective in vitro and, when delivered intraperitoneally, in vivo, inhibiting tumor growth when given with doxorubicin (Item No. 15007).{32706,32707} PGP-4008 also enhances the ability of docetaxel (Item No. 11637) to inhibit growth and drive apoptosis in ovarian cancer cells.{32708}  

     

    Brand:
    Cayman
    SKU:20901 -

    Out of stock

  • PGP-4008 is a selective inhibitor of P-glycoprotein (P-gp) that does not affect the activity of multidrug resistance-related protein 1 (MRP1).{32706,32707} It is effective in vitro and, when delivered intraperitoneally, in vivo, inhibiting tumor growth when given with doxorubicin (Item No. 15007).{32706,32707} PGP-4008 also enhances the ability of docetaxel (Item No. 11637) to inhibit growth and drive apoptosis in ovarian cancer cells.{32708}  

     

    Brand:
    Cayman
    SKU:20901 -

    Out of stock

  • PGPC is an oxidized phospholipid that can be formed under conditions of oxidative stress.{15289} It is found as a component in mildly oxidized LDL (MM-LDL) and in products formed from the oxidation of 1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine (Ox-PAPC).{10395} PGPC activates peroxisome proliferator-activated receptor (PPARα) in a concentration-dependent manner in a cell-based ligand-binding assay.{37721} It increases VCAM1 and E-selectin expression in human aortic endothelial cells (HAECs), as well as HAEC binding by monocytes and polymorphonuclear neutrophils (PMNs), in a concentration-dependent manner.{10396} PGPC (37.5 μM) also increases total 5-lipoxygenase metabolites in murine resident peritoneal macrophages (RPMs) and induces apoptosis in A7r5 rat aortic smooth muscle cells in vitro when used at a concentration of 50 μM.{37717,37718} PGPC levels are increased in the serum, LDL, and peripheral blood mononuclear cells (PBMCs) of patients with coronary artery disease.{37719} UVA irradiation increases PGPC levels in cultured human skin fibroblasts.{37720}  

     

    Brand:
    Cayman
    SKU:10044 - 1 mg

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  • PGPC is an oxidized phospholipid that can be formed under conditions of oxidative stress.{15289} It is found as a component in mildly oxidized LDL (MM-LDL) and in products formed from the oxidation of 1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine (Ox-PAPC).{10395} PGPC activates peroxisome proliferator-activated receptor (PPARα) in a concentration-dependent manner in a cell-based ligand-binding assay.{37721} It increases VCAM1 and E-selectin expression in human aortic endothelial cells (HAECs), as well as HAEC binding by monocytes and polymorphonuclear neutrophils (PMNs), in a concentration-dependent manner.{10396} PGPC (37.5 μM) also increases total 5-lipoxygenase metabolites in murine resident peritoneal macrophages (RPMs) and induces apoptosis in A7r5 rat aortic smooth muscle cells in vitro when used at a concentration of 50 μM.{37717,37718} PGPC levels are increased in the serum, LDL, and peripheral blood mononuclear cells (PBMCs) of patients with coronary artery disease.{37719} UVA irradiation increases PGPC levels in cultured human skin fibroblasts.{37720}  

     

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    Cayman
    SKU:10044 - 10 mg

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  • PGPC is an oxidized phospholipid that can be formed under conditions of oxidative stress.{15289} It is found as a component in mildly oxidized LDL (MM-LDL) and in products formed from the oxidation of 1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine (Ox-PAPC).{10395} PGPC activates peroxisome proliferator-activated receptor (PPARα) in a concentration-dependent manner in a cell-based ligand-binding assay.{37721} It increases VCAM1 and E-selectin expression in human aortic endothelial cells (HAECs), as well as HAEC binding by monocytes and polymorphonuclear neutrophils (PMNs), in a concentration-dependent manner.{10396} PGPC (37.5 μM) also increases total 5-lipoxygenase metabolites in murine resident peritoneal macrophages (RPMs) and induces apoptosis in A7r5 rat aortic smooth muscle cells in vitro when used at a concentration of 50 μM.{37717,37718} PGPC levels are increased in the serum, LDL, and peripheral blood mononuclear cells (PBMCs) of patients with coronary artery disease.{37719} UVA irradiation increases PGPC levels in cultured human skin fibroblasts.{37720}  

     

    Brand:
    Cayman
    SKU:10044 - 5 mg

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  • PGPC is an oxidized phospholipid that can be formed under conditions of oxidative stress.{15289} It is found as a component in mildly oxidized LDL (MM-LDL) and in products formed from the oxidation of 1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine (Ox-PAPC).{10395} PGPC activates peroxisome proliferator-activated receptor (PPARα) in a concentration-dependent manner in a cell-based ligand-binding assay.{37721} It increases VCAM1 and E-selectin expression in human aortic endothelial cells (HAECs), as well as HAEC binding by monocytes and polymorphonuclear neutrophils (PMNs), in a concentration-dependent manner.{10396} PGPC (37.5 μM) also increases total 5-lipoxygenase metabolites in murine resident peritoneal macrophages (RPMs) and induces apoptosis in A7r5 rat aortic smooth muscle cells in vitro when used at a concentration of 50 μM.{37717,37718} PGPC levels are increased in the serum, LDL, and peripheral blood mononuclear cells (PBMCs) of patients with coronary artery disease.{37719} UVA irradiation increases PGPC levels in cultured human skin fibroblasts.{37720}  

     

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    Cayman
    SKU:10044 - 500 µg

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  • PH-002 is an inhibitor of the interaction between the amino- and carboxy-terminal domains of apolipoprotein E4 (ApoE4; IC50 = 116 nM in a FRET reporter assay for domain interaction).{43809,51125} It restores intracellular trafficking of ApoE4 to the endoplasmic reticulum and Golgi apparatus in Neuro-2a cells expressing EGFP-ApoE4 or EGFP-ApoE4-R61T, a mutation that impairs ApoE4 domain interactions, when used at a concentration of 100 nM. PH-002 also prevents impairments in neurite outgrowth and dendritic spine development induced by expression of ApoE4 in Neuro-2a cells. It restores levels of mitochondrial complex IV subunit 1 in Neuro-2a cells expressing ApoE4 (EC50 = 39 nM) and increases mitochondrial motility in PC12 cells expressing ApoE4 (EC50 = <1 nM).{43809}  

     

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    Cayman
    SKU:27739 - 1 mg

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  • PH-002 is an inhibitor of the interaction between the amino- and carboxy-terminal domains of apolipoprotein E4 (ApoE4; IC50 = 116 nM in a FRET reporter assay for domain interaction).{43809,51125} It restores intracellular trafficking of ApoE4 to the endoplasmic reticulum and Golgi apparatus in Neuro-2a cells expressing EGFP-ApoE4 or EGFP-ApoE4-R61T, a mutation that impairs ApoE4 domain interactions, when used at a concentration of 100 nM. PH-002 also prevents impairments in neurite outgrowth and dendritic spine development induced by expression of ApoE4 in Neuro-2a cells. It restores levels of mitochondrial complex IV subunit 1 in Neuro-2a cells expressing ApoE4 (EC50 = 39 nM) and increases mitochondrial motility in PC12 cells expressing ApoE4 (EC50 = <1 nM).{43809}  

     

    Brand:
    Cayman
    SKU:27739 - 10 mg

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  • PH-002 is an inhibitor of the interaction between the amino- and carboxy-terminal domains of apolipoprotein E4 (ApoE4; IC50 = 116 nM in a FRET reporter assay for domain interaction).{43809,51125} It restores intracellular trafficking of ApoE4 to the endoplasmic reticulum and Golgi apparatus in Neuro-2a cells expressing EGFP-ApoE4 or EGFP-ApoE4-R61T, a mutation that impairs ApoE4 domain interactions, when used at a concentration of 100 nM. PH-002 also prevents impairments in neurite outgrowth and dendritic spine development induced by expression of ApoE4 in Neuro-2a cells. It restores levels of mitochondrial complex IV subunit 1 in Neuro-2a cells expressing ApoE4 (EC50 = 39 nM) and increases mitochondrial motility in PC12 cells expressing ApoE4 (EC50 = <1 nM).{43809}  

     

    Brand:
    Cayman
    SKU:27739 - 25 mg

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  • PH-002 is an inhibitor of the interaction between the amino- and carboxy-terminal domains of apolipoprotein E4 (ApoE4; IC50 = 116 nM in a FRET reporter assay for domain interaction).{43809,51125} It restores intracellular trafficking of ApoE4 to the endoplasmic reticulum and Golgi apparatus in Neuro-2a cells expressing EGFP-ApoE4 or EGFP-ApoE4-R61T, a mutation that impairs ApoE4 domain interactions, when used at a concentration of 100 nM. PH-002 also prevents impairments in neurite outgrowth and dendritic spine development induced by expression of ApoE4 in Neuro-2a cells. It restores levels of mitochondrial complex IV subunit 1 in Neuro-2a cells expressing ApoE4 (EC50 = 39 nM) and increases mitochondrial motility in PC12 cells expressing ApoE4 (EC50 = <1 nM).{43809}  

     

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    Cayman
    SKU:27739 - 5 mg

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  • PH-797804 is an inhibitor of p38α MAPK with an IC50 value of 26 nM in a cell-free assay.{31975,21533} It is 4-fold more selective for p38α compared to p38β and does not inhibit JNK2 or ERK at concentrations up to 1 µM.{31975} PH-797804 treatment for 10 days in vivo demonstrates anti-inflammatory activity in chronic inflammatory disease models, significantly reducing both joint inflammation and associated bone loss in streptococcal cell wall-induced arthritis in rats and collagen-induced arthritis in mice.{31975}  

     

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    Cayman
    SKU:20244 -

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  • PH-797804 is an inhibitor of p38α MAPK with an IC50 value of 26 nM in a cell-free assay.{31975,21533} It is 4-fold more selective for p38α compared to p38β and does not inhibit JNK2 or ERK at concentrations up to 1 µM.{31975} PH-797804 treatment for 10 days in vivo demonstrates anti-inflammatory activity in chronic inflammatory disease models, significantly reducing both joint inflammation and associated bone loss in streptococcal cell wall-induced arthritis in rats and collagen-induced arthritis in mice.{31975}  

     

    Brand:
    Cayman
    SKU:20244 -

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  • PH-797804 is an inhibitor of p38α MAPK with an IC50 value of 26 nM in a cell-free assay.{31975,21533} It is 4-fold more selective for p38α compared to p38β and does not inhibit JNK2 or ERK at concentrations up to 1 µM.{31975} PH-797804 treatment for 10 days in vivo demonstrates anti-inflammatory activity in chronic inflammatory disease models, significantly reducing both joint inflammation and associated bone loss in streptococcal cell wall-induced arthritis in rats and collagen-induced arthritis in mice.{31975}  

     

    Brand:
    Cayman
    SKU:20244 -

    Available on backorder

  • PH-797804 is an inhibitor of p38α MAPK with an IC50 value of 26 nM in a cell-free assay.{31975,21533} It is 4-fold more selective for p38α compared to p38β and does not inhibit JNK2 or ERK at concentrations up to 1 µM.{31975} PH-797804 treatment for 10 days in vivo demonstrates anti-inflammatory activity in chronic inflammatory disease models, significantly reducing both joint inflammation and associated bone loss in streptococcal cell wall-induced arthritis in rats and collagen-induced arthritis in mice.{31975}  

     

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    Cayman
    SKU:20244 -

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  • The c-Met receptor tyrosine kinase and its ligand, hepatocyte growth factor, have been implicated in the development and progression of several human cancers.{23657} PHA-665752 is an ATP-competitive, active-site inhibitor of the catalytic activity of c-Met kinase (Ki = 4 nM; IC50 = 9 nM).{24836} It exhibits >50-fold selectivity for c-Met over a panel of tyrosine and serine/threonine kinases. PHA-665752 can inhibit c-Met phosphorylation, as well as cell proliferation and cell motility, of various tumor cells (IC50s = 18-50 nM).{24836} It also inhibits signal transduction downstream of c-Met, interfering with the activation of Gab-1 adaptor protein, ERK1/2, Akt, STAT3, PLC-γ, and focal adhesion kinase in multiple tumor cell lines.{24836} In a gastric carcinoma xenograft model, 25 mg/kg PHA-665752 was shown to reduce tumor growth in mice by inhibiting c-Met activation.{24836}  

     

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    Cayman
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  • The c-Met receptor tyrosine kinase and its ligand, hepatocyte growth factor, have been implicated in the development and progression of several human cancers.{23657} PHA-665752 is an ATP-competitive, active-site inhibitor of the catalytic activity of c-Met kinase (Ki = 4 nM; IC50 = 9 nM).{24836} It exhibits >50-fold selectivity for c-Met over a panel of tyrosine and serine/threonine kinases. PHA-665752 can inhibit c-Met phosphorylation, as well as cell proliferation and cell motility, of various tumor cells (IC50s = 18-50 nM).{24836} It also inhibits signal transduction downstream of c-Met, interfering with the activation of Gab-1 adaptor protein, ERK1/2, Akt, STAT3, PLC-γ, and focal adhesion kinase in multiple tumor cell lines.{24836} In a gastric carcinoma xenograft model, 25 mg/kg PHA-665752 was shown to reduce tumor growth in mice by inhibiting c-Met activation.{24836}  

     

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    Cayman
    SKU:-
  • The c-Met receptor tyrosine kinase and its ligand, hepatocyte growth factor, have been implicated in the development and progression of several human cancers.{23657} PHA-665752 is an ATP-competitive, active-site inhibitor of the catalytic activity of c-Met kinase (Ki = 4 nM; IC50 = 9 nM).{24836} It exhibits >50-fold selectivity for c-Met over a panel of tyrosine and serine/threonine kinases. PHA-665752 can inhibit c-Met phosphorylation, as well as cell proliferation and cell motility, of various tumor cells (IC50s = 18-50 nM).{24836} It also inhibits signal transduction downstream of c-Met, interfering with the activation of Gab-1 adaptor protein, ERK1/2, Akt, STAT3, PLC-γ, and focal adhesion kinase in multiple tumor cell lines.{24836} In a gastric carcinoma xenograft model, 25 mg/kg PHA-665752 was shown to reduce tumor growth in mice by inhibiting c-Met activation.{24836}  

     

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    Cayman
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  • The c-Met receptor tyrosine kinase and its ligand, hepatocyte growth factor, have been implicated in the development and progression of several human cancers.{23657} PHA-665752 is an ATP-competitive, active-site inhibitor of the catalytic activity of c-Met kinase (Ki = 4 nM; IC50 = 9 nM).{24836} It exhibits >50-fold selectivity for c-Met over a panel of tyrosine and serine/threonine kinases. PHA-665752 can inhibit c-Met phosphorylation, as well as cell proliferation and cell motility, of various tumor cells (IC50s = 18-50 nM).{24836} It also inhibits signal transduction downstream of c-Met, interfering with the activation of Gab-1 adaptor protein, ERK1/2, Akt, STAT3, PLC-γ, and focal adhesion kinase in multiple tumor cell lines.{24836} In a gastric carcinoma xenograft model, 25 mg/kg PHA-665752 was shown to reduce tumor growth in mice by inhibiting c-Met activation.{24836}  

     

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    Cayman
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  • PHA-680632 is an inhibitor of Aurora A, B, and C kinases (IC50s = 27, 135, and 120 nM, respectively).{48527} It has greater than 15-fold selectivity for Aurora A kinase in a panel of 31 kinases. PHA-680632 inhibits phosphorylation of serine 10 on histone H3 in U2OS cells (IC50 = 0.39 µM). It inhibits proliferation of U2OS, HeLa, A549, HCT116, U937, and HL-60 cells (IC50s = 1.6, 0.4, 0.6, 0.1, 0.1, and 0.1 µM, respectively). PHA-680632 reduces the size of established tumors in transgenic v-Ha-ras mice and in an HL-60 human leukemia mouse xenograft model when administered at a dose of 45 mg/kg.  

     

    Brand:
    Cayman
    SKU:28381 - 10 mg

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  • PHA-680632 is an inhibitor of Aurora A, B, and C kinases (IC50s = 27, 135, and 120 nM, respectively).{48527} It has greater than 15-fold selectivity for Aurora A kinase in a panel of 31 kinases. PHA-680632 inhibits phosphorylation of serine 10 on histone H3 in U2OS cells (IC50 = 0.39 µM). It inhibits proliferation of U2OS, HeLa, A549, HCT116, U937, and HL-60 cells (IC50s = 1.6, 0.4, 0.6, 0.1, 0.1, and 0.1 µM, respectively). PHA-680632 reduces the size of established tumors in transgenic v-Ha-ras mice and in an HL-60 human leukemia mouse xenograft model when administered at a dose of 45 mg/kg.  

     

    Brand:
    Cayman
    SKU:28381 - 25 mg

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  • PHA-680632 is an inhibitor of Aurora A, B, and C kinases (IC50s = 27, 135, and 120 nM, respectively).{48527} It has greater than 15-fold selectivity for Aurora A kinase in a panel of 31 kinases. PHA-680632 inhibits phosphorylation of serine 10 on histone H3 in U2OS cells (IC50 = 0.39 µM). It inhibits proliferation of U2OS, HeLa, A549, HCT116, U937, and HL-60 cells (IC50s = 1.6, 0.4, 0.6, 0.1, 0.1, and 0.1 µM, respectively). PHA-680632 reduces the size of established tumors in transgenic v-Ha-ras mice and in an HL-60 human leukemia mouse xenograft model when administered at a dose of 45 mg/kg.  

     

    Brand:
    Cayman
    SKU:28381 - 5 mg

    Available on backorder

  • PHA-680632 is an inhibitor of Aurora A, B, and C kinases (IC50s = 27, 135, and 120 nM, respectively).{48527} It has greater than 15-fold selectivity for Aurora A kinase in a panel of 31 kinases. PHA-680632 inhibits phosphorylation of serine 10 on histone H3 in U2OS cells (IC50 = 0.39 µM). It inhibits proliferation of U2OS, HeLa, A549, HCT116, U937, and HL-60 cells (IC50s = 1.6, 0.4, 0.6, 0.1, 0.1, and 0.1 µM, respectively). PHA-680632 reduces the size of established tumors in transgenic v-Ha-ras mice and in an HL-60 human leukemia mouse xenograft model when administered at a dose of 45 mg/kg.  

     

    Brand:
    Cayman
    SKU:28381 - 50 mg

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  • Cdc7 kinase is a key regulator of the S-phase of the cell cycle. It is known to promote the activity of DNA replication origins in eukaryotic organisms. Inhibition of Cdc7 kinase causes blockade of DNA synthesis in human cell lines. Tumor cells are then funneled into the apoptotic pathway in a p53-independent manner. Pharmacological inhibition of Cdc7 kinase can be an effective strategy for the development of oncologic therapeutics useful for treatment of cancers. PHA-767491 is a potent inhibitor of Cdc7 kinase with an IC50 value of 10 nM in the presence of 1.5 µM ATP.{16775} At 10 µM, PHA-767491 induces apoptotic cell death in multiple cancer cell types.{16775} PHA-767491 also inhibits Cdk9, a kinase involved in the phosphorylation of RNA polymerase II and in transcriptional regulation of gene expression, with an IC50 value of 34 nM.{16774}  

     

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    Cayman
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  • Cdc7 kinase is a key regulator of the S-phase of the cell cycle. It is known to promote the activity of DNA replication origins in eukaryotic organisms. Inhibition of Cdc7 kinase causes blockade of DNA synthesis in human cell lines. Tumor cells are then funneled into the apoptotic pathway in a p53-independent manner. Pharmacological inhibition of Cdc7 kinase can be an effective strategy for the development of oncologic therapeutics useful for treatment of cancers. PHA-767491 is a potent inhibitor of Cdc7 kinase with an IC50 value of 10 nM in the presence of 1.5 µM ATP.{16775} At 10 µM, PHA-767491 induces apoptotic cell death in multiple cancer cell types.{16775} PHA-767491 also inhibits Cdk9, a kinase involved in the phosphorylation of RNA polymerase II and in transcriptional regulation of gene expression, with an IC50 value of 34 nM.{16774}  

     

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    Cayman
    SKU:-

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  • Cdc7 kinase is a key regulator of the S-phase of the cell cycle. It is known to promote the activity of DNA replication origins in eukaryotic organisms. Inhibition of Cdc7 kinase causes blockade of DNA synthesis in human cell lines. Tumor cells are then funneled into the apoptotic pathway in a p53-independent manner. Pharmacological inhibition of Cdc7 kinase can be an effective strategy for the development of oncologic therapeutics useful for treatment of cancers. PHA-767491 is a potent inhibitor of Cdc7 kinase with an IC50 value of 10 nM in the presence of 1.5 µM ATP.{16775} At 10 µM, PHA-767491 induces apoptotic cell death in multiple cancer cell types.{16775} PHA-767491 also inhibits Cdk9, a kinase involved in the phosphorylation of RNA polymerase II and in transcriptional regulation of gene expression, with an IC50 value of 34 nM.{16774}  

     

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    Cayman
    SKU:-

    Available on backorder

  • Cdc7 kinase is a key regulator of the S-phase of the cell cycle. It is known to promote the activity of DNA replication origins in eukaryotic organisms. Inhibition of Cdc7 kinase causes blockade of DNA synthesis in human cell lines. Tumor cells are then funneled into the apoptotic pathway in a p53-independent manner. Pharmacological inhibition of Cdc7 kinase can be an effective strategy for the development of oncologic therapeutics useful for treatment of cancers. PHA-767491 is a potent inhibitor of Cdc7 kinase with an IC50 value of 10 nM in the presence of 1.5 µM ATP.{16775} At 10 µM, PHA-767491 induces apoptotic cell death in multiple cancer cell types.{16775} PHA-767491 also inhibits Cdk9, a kinase involved in the phosphorylation of RNA polymerase II and in transcriptional regulation of gene expression, with an IC50 value of 34 nM.{16774}  

     

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    Cayman
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  • PHA-793887 is a pyrrolo[3,4-c]pyrazole that inhibits cyclin-dependent kinases Cdk2/cyclin A, Cdk2/cyclin E, Cdk5/p25, and Cdk7/cyclin H with IC50 values of 8, 8, 5, and 10 nM, respectively.{30703} It is more than 6-fold selective for these kinases over Cdk1/cyclin B, Cdk4/cyclin D1, Cdk9/cyclin T, and GSK3β (IC50s = 60, 62, 138, and 79 nM, respectively).{30703} PHA-793887 is cytotoxic to human ovarian A2780, colon HCT116, pancreatic BX-PC3, and leukemic K562, KU812, KCL22, and TOM1 cells both in vitro and in xenograft models.{30703,30704} This compound has been examined in patients with solid tumors in phase 1 clinical trials.{30702}  

     

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    Cayman
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  • PHA-793887 is a pyrrolo[3,4-c]pyrazole that inhibits cyclin-dependent kinases Cdk2/cyclin A, Cdk2/cyclin E, Cdk5/p25, and Cdk7/cyclin H with IC50 values of 8, 8, 5, and 10 nM, respectively.{30703} It is more than 6-fold selective for these kinases over Cdk1/cyclin B, Cdk4/cyclin D1, Cdk9/cyclin T, and GSK3β (IC50s = 60, 62, 138, and 79 nM, respectively).{30703} PHA-793887 is cytotoxic to human ovarian A2780, colon HCT116, pancreatic BX-PC3, and leukemic K562, KU812, KCL22, and TOM1 cells both in vitro and in xenograft models.{30703,30704} This compound has been examined in patients with solid tumors in phase 1 clinical trials.{30702}  

     

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    Cayman
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  • PHA-793887 is a pyrrolo[3,4-c]pyrazole that inhibits cyclin-dependent kinases Cdk2/cyclin A, Cdk2/cyclin E, Cdk5/p25, and Cdk7/cyclin H with IC50 values of 8, 8, 5, and 10 nM, respectively.{30703} It is more than 6-fold selective for these kinases over Cdk1/cyclin B, Cdk4/cyclin D1, Cdk9/cyclin T, and GSK3β (IC50s = 60, 62, 138, and 79 nM, respectively).{30703} PHA-793887 is cytotoxic to human ovarian A2780, colon HCT116, pancreatic BX-PC3, and leukemic K562, KU812, KCL22, and TOM1 cells both in vitro and in xenograft models.{30703,30704} This compound has been examined in patients with solid tumors in phase 1 clinical trials.{30702}  

     

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    Cayman
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  • PHA-793887 is a pyrrolo[3,4-c]pyrazole that inhibits cyclin-dependent kinases Cdk2/cyclin A, Cdk2/cyclin E, Cdk5/p25, and Cdk7/cyclin H with IC50 values of 8, 8, 5, and 10 nM, respectively.{30703} It is more than 6-fold selective for these kinases over Cdk1/cyclin B, Cdk4/cyclin D1, Cdk9/cyclin T, and GSK3β (IC50s = 60, 62, 138, and 79 nM, respectively).{30703} PHA-793887 is cytotoxic to human ovarian A2780, colon HCT116, pancreatic BX-PC3, and leukemic K562, KU812, KCL22, and TOM1 cells both in vitro and in xenograft models.{30703,30704} This compound has been examined in patients with solid tumors in phase 1 clinical trials.{30702}  

     

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    Cayman
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  • PHA-848125 is an ATP-competitive inhibitor of cyclin-dependent kinases (Cdks) that potently inhibits Cdk2/cyclin A (IC50 = 45 nM).{34455} It is at least 3-fold less potent at Cdks 1, 3, 4, 5, and 7.{34455} PHA-848125 is orally available and displays efficacy in suppressing the growth of cancer cells or tumor xenografts in animals.{34455,34456,34457}  

     

    Brand:
    Cayman
    SKU:21474 -

    Out of stock

  • PHA-848125 is an ATP-competitive inhibitor of cyclin-dependent kinases (Cdks) that potently inhibits Cdk2/cyclin A (IC50 = 45 nM).{34455} It is at least 3-fold less potent at Cdks 1, 3, 4, 5, and 7.{34455} PHA-848125 is orally available and displays efficacy in suppressing the growth of cancer cells or tumor xenografts in animals.{34455,34456,34457}  

     

    Brand:
    Cayman
    SKU:21474 -

    Out of stock

  • PHA-848125 is an ATP-competitive inhibitor of cyclin-dependent kinases (Cdks) that potently inhibits Cdk2/cyclin A (IC50 = 45 nM).{34455} It is at least 3-fold less potent at Cdks 1, 3, 4, 5, and 7.{34455} PHA-848125 is orally available and displays efficacy in suppressing the growth of cancer cells or tumor xenografts in animals.{34455,34456,34457}  

     

    Brand:
    Cayman
    SKU:21474 -

    Out of stock

  • Phallacidin is a natural mycotoxin first isolated from the death cap mushroom, A. phalloides. It binds filamentous actin (F-actin) like phalloidin (Item No. 18039), but contains a carboxyl group for coupling reactions.{29213,29214}  

     

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    Cayman
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  • Phalloidin is a natural mycotoxin first isolated from the death cap mushroom, A. phalloides. It binds F-actin and stabilizes actin fibers.{29147,29148} Fluorescently labeled phalloidin is commonly used to stain F-actin in cells.{29149,29146}  

     

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    Cayman
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  • Phanerosporic acid is a fungal secondary metabolite originally isolated from P. chrysosporum that has antibacterial activity against B. cereus, B. subtilis, and E. coli and antifungal activity against S. cerevisiae, A. niger, O. ulmi, U. maydis, C. cucmerinum, C. cladosporioides, and B. cinerea.{35189} It has been used in the synthesis of macrolide derivatives.  

     

    Brand:
    Cayman
    SKU:23879 - 25 mg

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  • Phanerosporic acid is a fungal secondary metabolite originally isolated from P. chrysosporum that has antibacterial activity against B. cereus, B. subtilis, and E. coli and antifungal activity against S. cerevisiae, A. niger, O. ulmi, U. maydis, C. cucmerinum, C. cladosporioides, and B. cinerea.{35189} It has been used in the synthesis of macrolide derivatives.  

     

    Brand:
    Cayman
    SKU:23879 - 5 mg

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  • Phe-Arg-βNA is a peptide broad-spectrum bacterial efflux pump inhibitor.{53463} It potentiates the activity of the fluoroquinolone antibiotic levofloxacin (Item No. 20382) against P. aeruginosa strains overexpressing the MexAB-OprM, MexCD-OprJ, or MexEF-OprN multidrug resistance efflux pumps (EC50s = 10 µg/ml for all) but is inactive against these strains when used alone (MICs = >512 µg/ml for all). Phe-Arg-βNA also increases the susceptibility of quinolone-resistant E. coli isolates to nalidixic acid (Item No. 19807).{53464}  

     

    Brand:
    Cayman
    SKU:29511 - 100 mg

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  • Phe-Arg-βNA is a peptide broad-spectrum bacterial efflux pump inhibitor.{53463} It potentiates the activity of the fluoroquinolone antibiotic levofloxacin (Item No. 20382) against P. aeruginosa strains overexpressing the MexAB-OprM, MexCD-OprJ, or MexEF-OprN multidrug resistance efflux pumps (EC50s = 10 µg/ml for all) but is inactive against these strains when used alone (MICs = >512 µg/ml for all). Phe-Arg-βNA also increases the susceptibility of quinolone-resistant E. coli isolates to nalidixic acid (Item No. 19807).{53464}  

     

    Brand:
    Cayman
    SKU:29511 - 25 mg

    Available on backorder

  • Phe-Arg-βNA is a peptide broad-spectrum bacterial efflux pump inhibitor.{53463} It potentiates the activity of the fluoroquinolone antibiotic levofloxacin (Item No. 20382) against P. aeruginosa strains overexpressing the MexAB-OprM, MexCD-OprJ, or MexEF-OprN multidrug resistance efflux pumps (EC50s = 10 µg/ml for all) but is inactive against these strains when used alone (MICs = >512 µg/ml for all). Phe-Arg-βNA also increases the susceptibility of quinolone-resistant E. coli isolates to nalidixic acid (Item No. 19807).{53464}  

     

    Brand:
    Cayman
    SKU:29511 - 250 mg

    Available on backorder