Cayman
Showing 22951–23100 of 45550 results
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GSK2269557 is an inhibitor of PI3Kδ (pKi = 9.9) that is >1,000-fold selective for PI3Kδ over PI3Kα, β, and γ isoforms.{32991} It is reported to be active in a brown Norway rat acute ovalbumin-induced allergic asthma model of Th2-driven lung inflammation (ED50 = 67 µg/kg).{32991}
Brand:CaymanSKU:-Available on backorder
GSK2269557 is an inhibitor of PI3Kδ (pKi = 9.9) that is >1,000-fold selective for PI3Kδ over PI3Kα, β, and γ isoforms.{32991} It is reported to be active in a brown Norway rat acute ovalbumin-induced allergic asthma model of Th2-driven lung inflammation (ED50 = 67 µg/kg).{32991}
Brand:CaymanSKU:-Available on backorder
GSK2269557 is an inhibitor of PI3Kδ (pKi = 9.9) that is >1,000-fold selective for PI3Kδ over PI3Kα, β, and γ isoforms.{32991} It is reported to be active in a brown Norway rat acute ovalbumin-induced allergic asthma model of Th2-driven lung inflammation (ED50 = 67 µg/kg).{32991}
Brand:CaymanSKU:-Available on backorder
GSK2292767 is a potent and selective inhibitor of phosphatidylinositol 3-kinase δ (PI3Kδ; Ki = 79 pM).{32991} It has >1,000-fold selectivity for PI3Kδ over isoforms PI3Kα, PI3Kβ, and PI3Kγ with Ki values of 501, 630, and 501 nM, respectively. GSK2292767 is >100-fold selective for PI3Kδ over a panel of 250 kinases. It inhibits IFN-γ and IL-2 production (IC50s = 1.9 and 3.16 nM, respectively) in a human lung parenchyma assay. GSK2292767 also protects against eosinophil recruitment (ED50 = 35 μg/kg) in the brown Norway rat acute ovalbumin model of Th2-driven lung inflammation.
Brand:CaymanSKU:21757 -Out of stock
GSK2292767 is a potent and selective inhibitor of phosphatidylinositol 3-kinase δ (PI3Kδ; Ki = 79 pM).{32991} It has >1,000-fold selectivity for PI3Kδ over isoforms PI3Kα, PI3Kβ, and PI3Kγ with Ki values of 501, 630, and 501 nM, respectively. GSK2292767 is >100-fold selective for PI3Kδ over a panel of 250 kinases. It inhibits IFN-γ and IL-2 production (IC50s = 1.9 and 3.16 nM, respectively) in a human lung parenchyma assay. GSK2292767 also protects against eosinophil recruitment (ED50 = 35 μg/kg) in the brown Norway rat acute ovalbumin model of Th2-driven lung inflammation.
Brand:CaymanSKU:21757 -Out of stock
GSK2292767 is a potent and selective inhibitor of phosphatidylinositol 3-kinase δ (PI3Kδ; Ki = 79 pM).{32991} It has >1,000-fold selectivity for PI3Kδ over isoforms PI3Kα, PI3Kβ, and PI3Kγ with Ki values of 501, 630, and 501 nM, respectively. GSK2292767 is >100-fold selective for PI3Kδ over a panel of 250 kinases. It inhibits IFN-γ and IL-2 production (IC50s = 1.9 and 3.16 nM, respectively) in a human lung parenchyma assay. GSK2292767 also protects against eosinophil recruitment (ED50 = 35 μg/kg) in the brown Norway rat acute ovalbumin model of Th2-driven lung inflammation.
Brand:CaymanSKU:21757 -Out of stock
GSK2292767 is a potent and selective inhibitor of phosphatidylinositol 3-kinase δ (PI3Kδ; Ki = 79 pM).{32991} It has >1,000-fold selectivity for PI3Kδ over isoforms PI3Kα, PI3Kβ, and PI3Kγ with Ki values of 501, 630, and 501 nM, respectively. GSK2292767 is >100-fold selective for PI3Kδ over a panel of 250 kinases. It inhibits IFN-γ and IL-2 production (IC50s = 1.9 and 3.16 nM, respectively) in a human lung parenchyma assay. GSK2292767 also protects against eosinophil recruitment (ED50 = 35 μg/kg) in the brown Norway rat acute ovalbumin model of Th2-driven lung inflammation.
Brand:CaymanSKU:21757 -Out of stock
GSK2330672 is an inhibitor of the apical sodium-dependent bile acid transporter (ASBT; IC50s = 42, 2.1, and 1.9 nM for human, mouse, and rat ASBT, respectively).{42065} In vivo, GSK2330672 (0.05 mg/kg) stimulates fecal bile acid secretion, reduces hemoglobin A1c (HbA1c) and plasma glucose levels, and increases total GLP-1 (Item No. 24460) and plasma insulin in Zucker diabetic fatty (ZDF) rats.
Brand:CaymanSKU:23843 - 1 mgAvailable on backorder
GSK2330672 is an inhibitor of the apical sodium-dependent bile acid transporter (ASBT; IC50s = 42, 2.1, and 1.9 nM for human, mouse, and rat ASBT, respectively).{42065} In vivo, GSK2330672 (0.05 mg/kg) stimulates fecal bile acid secretion, reduces hemoglobin A1c (HbA1c) and plasma glucose levels, and increases total GLP-1 (Item No. 24460) and plasma insulin in Zucker diabetic fatty (ZDF) rats.
Brand:CaymanSKU:23843 - 10 mgAvailable on backorder
GSK2330672 is an inhibitor of the apical sodium-dependent bile acid transporter (ASBT; IC50s = 42, 2.1, and 1.9 nM for human, mouse, and rat ASBT, respectively).{42065} In vivo, GSK2330672 (0.05 mg/kg) stimulates fecal bile acid secretion, reduces hemoglobin A1c (HbA1c) and plasma glucose levels, and increases total GLP-1 (Item No. 24460) and plasma insulin in Zucker diabetic fatty (ZDF) rats.
Brand:CaymanSKU:23843 - 5 mgAvailable on backorder
3-Phosphoinositide-dependent protein kinase 1 (PDK1) is a serine-threonine kinase that plays an important role in growth factor signaling by phosphorylating and activating a group of kinases, including protein kinase (PK)B, PKA, and certain isoforms of PKC. GSK2334470 is an inhibitor of PDK1 (IC50 = ~10 nM) that even at 100-fold higher concentrations does not affect the activity of 93 other protein kinases, including that of 13 closely related AGC kinase family members.{29229} In HEK293 cells, 30 nM – 1 µM GSK2334470 suppresses T-loop phosphorylation and activation of SGK, S6K1, and RSK, as well as the activation of Akt.{29229}
Brand:CaymanSKU:-Available on backorder
3-Phosphoinositide-dependent protein kinase 1 (PDK1) is a serine-threonine kinase that plays an important role in growth factor signaling by phosphorylating and activating a group of kinases, including protein kinase (PK)B, PKA, and certain isoforms of PKC. GSK2334470 is an inhibitor of PDK1 (IC50 = ~10 nM) that even at 100-fold higher concentrations does not affect the activity of 93 other protein kinases, including that of 13 closely related AGC kinase family members.{29229} In HEK293 cells, 30 nM – 1 µM GSK2334470 suppresses T-loop phosphorylation and activation of SGK, S6K1, and RSK, as well as the activation of Akt.{29229}
Brand:CaymanSKU:-Available on backorder
3-Phosphoinositide-dependent protein kinase 1 (PDK1) is a serine-threonine kinase that plays an important role in growth factor signaling by phosphorylating and activating a group of kinases, including protein kinase (PK)B, PKA, and certain isoforms of PKC. GSK2334470 is an inhibitor of PDK1 (IC50 = ~10 nM) that even at 100-fold higher concentrations does not affect the activity of 93 other protein kinases, including that of 13 closely related AGC kinase family members.{29229} In HEK293 cells, 30 nM – 1 µM GSK2334470 suppresses T-loop phosphorylation and activation of SGK, S6K1, and RSK, as well as the activation of Akt.{29229}
Brand:CaymanSKU:-Available on backorder
3-Phosphoinositide-dependent protein kinase 1 (PDK1) is a serine-threonine kinase that plays an important role in growth factor signaling by phosphorylating and activating a group of kinases, including protein kinase (PK)B, PKA, and certain isoforms of PKC. GSK2334470 is an inhibitor of PDK1 (IC50 = ~10 nM) that even at 100-fold higher concentrations does not affect the activity of 93 other protein kinases, including that of 13 closely related AGC kinase family members.{29229} In HEK293 cells, 30 nM – 1 µM GSK2334470 suppresses T-loop phosphorylation and activation of SGK, S6K1, and RSK, as well as the activation of Akt.{29229}
Brand:CaymanSKU:-Available on backorder
GSK256066 is a potent phosphodiesterase 4 (PDE4) inhibitor (IC50s = 4.9, 3.2, 3.8, and 1.1 pM for PDE4A, PDE4B, PDE4C, and PDE4D, respectively).{47799} It is greater than 380,000-fold selective for PDE4 over PDE1-3, -5, and -6 and greater than 2,500-fold selective over PDE7. GSK256066 inhibits LPS-induced TNF-α production in human peripheral blood monocytes (IC50 = 0.01 nM) and human whole blood (IC50 = 126 pM). Intratracheal administration of GSK256066 inhibits LPS-induced pulmonary neutrophilia in rats (ED50 = 1.1 µg/kg). It inhibits ovalbumin-induced pulmonary eosinophilia in rats (ED50 = 0.4 µg/kg) and LPS-induced pulmonary neutrophilia in ferrets (ED50 = 18 µg/kg).{47800}
Brand:CaymanSKU:28012 - 1 mgAvailable on backorder
GSK256066 is a potent phosphodiesterase 4 (PDE4) inhibitor (IC50s = 4.9, 3.2, 3.8, and 1.1 pM for PDE4A, PDE4B, PDE4C, and PDE4D, respectively).{47799} It is greater than 380,000-fold selective for PDE4 over PDE1-3, -5, and -6 and greater than 2,500-fold selective over PDE7. GSK256066 inhibits LPS-induced TNF-α production in human peripheral blood monocytes (IC50 = 0.01 nM) and human whole blood (IC50 = 126 pM). Intratracheal administration of GSK256066 inhibits LPS-induced pulmonary neutrophilia in rats (ED50 = 1.1 µg/kg). It inhibits ovalbumin-induced pulmonary eosinophilia in rats (ED50 = 0.4 µg/kg) and LPS-induced pulmonary neutrophilia in ferrets (ED50 = 18 µg/kg).{47800}
Brand:CaymanSKU:28012 - 10 mgAvailable on backorder
GSK256066 is a potent phosphodiesterase 4 (PDE4) inhibitor (IC50s = 4.9, 3.2, 3.8, and 1.1 pM for PDE4A, PDE4B, PDE4C, and PDE4D, respectively).{47799} It is greater than 380,000-fold selective for PDE4 over PDE1-3, -5, and -6 and greater than 2,500-fold selective over PDE7. GSK256066 inhibits LPS-induced TNF-α production in human peripheral blood monocytes (IC50 = 0.01 nM) and human whole blood (IC50 = 126 pM). Intratracheal administration of GSK256066 inhibits LPS-induced pulmonary neutrophilia in rats (ED50 = 1.1 µg/kg). It inhibits ovalbumin-induced pulmonary eosinophilia in rats (ED50 = 0.4 µg/kg) and LPS-induced pulmonary neutrophilia in ferrets (ED50 = 18 µg/kg).{47800}
Brand:CaymanSKU:28012 - 25 mgAvailable on backorder
GSK256066 is a potent phosphodiesterase 4 (PDE4) inhibitor (IC50s = 4.9, 3.2, 3.8, and 1.1 pM for PDE4A, PDE4B, PDE4C, and PDE4D, respectively).{47799} It is greater than 380,000-fold selective for PDE4 over PDE1-3, -5, and -6 and greater than 2,500-fold selective over PDE7. GSK256066 inhibits LPS-induced TNF-α production in human peripheral blood monocytes (IC50 = 0.01 nM) and human whole blood (IC50 = 126 pM). Intratracheal administration of GSK256066 inhibits LPS-induced pulmonary neutrophilia in rats (ED50 = 1.1 µg/kg). It inhibits ovalbumin-induced pulmonary eosinophilia in rats (ED50 = 0.4 µg/kg) and LPS-induced pulmonary neutrophilia in ferrets (ED50 = 18 µg/kg).{47800}
Brand:CaymanSKU:28012 - 5 mgAvailable on backorder
GSK2578215A is a potent inhibitor of leucine-rich repeat kinase 2 (LRRK2; IC50 = 8.9 nM) that also inhibits the G2019S mutant of LRRK2 (IC50 = 10.1 nM).{32599} It displays selectivity for LRRK2 over a panel of 460 other kinases. GSK2578215A prevents phosphorylation of both wild-type and G2019S LRRK2 in mouse spleen and kidney, but not in brain, following intraperitoneal injection of 100 mg/kg.{32599} GSK2578215A induces protective autophagy in SH-SY5Y cells and blocks LRRK2-dependent Na+/Ca2+ exchanger activity in dendritic cells.{32600,32601}
Brand:CaymanSKU:- GSK2578215A is a potent inhibitor of leucine-rich repeat kinase 2 (LRRK2; IC50 = 8.9 nM) that also inhibits the G2019S mutant of LRRK2 (IC50 = 10.1 nM).{32599} It displays selectivity for LRRK2 over a panel of 460 other kinases. GSK2578215A prevents phosphorylation of both wild-type and G2019S LRRK2 in mouse spleen and kidney, but not in brain, following intraperitoneal injection of 100 mg/kg.{32599} GSK2578215A induces protective autophagy in SH-SY5Y cells and blocks LRRK2-dependent Na+/Ca2+ exchanger activity in dendritic cells.{32600,32601}
Brand:CaymanSKU:- GSK2578215A is a potent inhibitor of leucine-rich repeat kinase 2 (LRRK2; IC50 = 8.9 nM) that also inhibits the G2019S mutant of LRRK2 (IC50 = 10.1 nM).{32599} It displays selectivity for LRRK2 over a panel of 460 other kinases. GSK2578215A prevents phosphorylation of both wild-type and G2019S LRRK2 in mouse spleen and kidney, but not in brain, following intraperitoneal injection of 100 mg/kg.{32599} GSK2578215A induces protective autophagy in SH-SY5Y cells and blocks LRRK2-dependent Na+/Ca2+ exchanger activity in dendritic cells.{32600,32601}
Brand:CaymanSKU:- GSK2578215A is a potent inhibitor of leucine-rich repeat kinase 2 (LRRK2; IC50 = 8.9 nM) that also inhibits the G2019S mutant of LRRK2 (IC50 = 10.1 nM).{32599} It displays selectivity for LRRK2 over a panel of 460 other kinases. GSK2578215A prevents phosphorylation of both wild-type and G2019S LRRK2 in mouse spleen and kidney, but not in brain, following intraperitoneal injection of 100 mg/kg.{32599} GSK2578215A induces protective autophagy in SH-SY5Y cells and blocks LRRK2-dependent Na+/Ca2+ exchanger activity in dendritic cells.{32600,32601}
Brand:CaymanSKU:-
Brand:CaymanSKU:21360 -Out of stock
Brand:CaymanSKU:21360 -Out of stock
Brand:CaymanSKU:21360 -Out of stock
Brand:CaymanSKU:21360 -Out of stock
GSK2606414 is an orally available, selective protein kinase R-like ER kinase (PERK) inhibitor with an IC50 value of 0.4 nM.{28170} It can inhibit thapsigargin-induced PERK phosphorylation in lung carcinoma A549 cells and attenuates subcutaneous pancreatic human tumor xenograft growth in mice.{28170} Because PERK mediates the unfolded protein response pathway, which has roles in neurotoxicity and cancer, inhibition of PERK signaling has potential applications for the treatment of cancer and also cognitive degeneration.
Brand:CaymanSKU:-Available on backorder
GSK2606414 is an orally available, selective protein kinase R-like ER kinase (PERK) inhibitor with an IC50 value of 0.4 nM.{28170} It can inhibit thapsigargin-induced PERK phosphorylation in lung carcinoma A549 cells and attenuates subcutaneous pancreatic human tumor xenograft growth in mice.{28170} Because PERK mediates the unfolded protein response pathway, which has roles in neurotoxicity and cancer, inhibition of PERK signaling has potential applications for the treatment of cancer and also cognitive degeneration.
Brand:CaymanSKU:-Available on backorder
GSK2606414 is an orally available, selective protein kinase R-like ER kinase (PERK) inhibitor with an IC50 value of 0.4 nM.{28170} It can inhibit thapsigargin-induced PERK phosphorylation in lung carcinoma A549 cells and attenuates subcutaneous pancreatic human tumor xenograft growth in mice.{28170} Because PERK mediates the unfolded protein response pathway, which has roles in neurotoxicity and cancer, inhibition of PERK signaling has potential applications for the treatment of cancer and also cognitive degeneration.
Brand:CaymanSKU:-Available on backorder
GSK2606414 is an orally available, selective protein kinase R-like ER kinase (PERK) inhibitor with an IC50 value of 0.4 nM.{28170} It can inhibit thapsigargin-induced PERK phosphorylation in lung carcinoma A549 cells and attenuates subcutaneous pancreatic human tumor xenograft growth in mice.{28170} Because PERK mediates the unfolded protein response pathway, which has roles in neurotoxicity and cancer, inhibition of PERK signaling has potential applications for the treatment of cancer and also cognitive degeneration.
Brand:CaymanSKU:-Available on backorder
Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of phosphatidylinositol at the 3 position to produce the second messengers phosphatidylinositol-3,4-bisphosphate (PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3). Class 1 PI3Ks are composed of a p110 catalytic subunit, of which there are four isoforms (p110α, p110β, p110δ, and p100γ), and a p85 regulatory subunit. GSK2636771 is an orally bioavailable inhibitor of PI3K p110β.{30758} At 1-10 µM, it decreases cell viability and Akt phosphorylation in p100β-dependent PTEN-deficient PC-3 prostate and BT549 and HCC70 breast cancer cell lines.{29910}
Brand:CaymanSKU:-Available on backorder
Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of phosphatidylinositol at the 3 position to produce the second messengers phosphatidylinositol-3,4-bisphosphate (PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3). Class 1 PI3Ks are composed of a p110 catalytic subunit, of which there are four isoforms (p110α, p110β, p110δ, and p100γ), and a p85 regulatory subunit. GSK2636771 is an orally bioavailable inhibitor of PI3K p110β.{30758} At 1-10 µM, it decreases cell viability and Akt phosphorylation in p100β-dependent PTEN-deficient PC-3 prostate and BT549 and HCC70 breast cancer cell lines.{29910}
Brand:CaymanSKU:-Available on backorder
Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of phosphatidylinositol at the 3 position to produce the second messengers phosphatidylinositol-3,4-bisphosphate (PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3). Class 1 PI3Ks are composed of a p110 catalytic subunit, of which there are four isoforms (p110α, p110β, p110δ, and p100γ), and a p85 regulatory subunit. GSK2636771 is an orally bioavailable inhibitor of PI3K p110β.{30758} At 1-10 µM, it decreases cell viability and Akt phosphorylation in p100β-dependent PTEN-deficient PC-3 prostate and BT549 and HCC70 breast cancer cell lines.{29910}
Brand:CaymanSKU:-Available on backorder
Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of phosphatidylinositol at the 3 position to produce the second messengers phosphatidylinositol-3,4-bisphosphate (PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3). Class 1 PI3Ks are composed of a p110 catalytic subunit, of which there are four isoforms (p110α, p110β, p110δ, and p100γ), and a p85 regulatory subunit. GSK2636771 is an orally bioavailable inhibitor of PI3K p110β.{30758} At 1-10 µM, it decreases cell viability and Akt phosphorylation in p100β-dependent PTEN-deficient PC-3 prostate and BT549 and HCC70 breast cancer cell lines.{29910}
Brand:CaymanSKU:-Available on backorder
Endothelial lipase, a member of the triglyceride lipase gene family expressed in endothelial cells, prefers phospholipid-enriched high-density lipoprotein (HDL) over triglyceride as substrate. GSK264220A is a potent inhibitor of endothelial lipase (IC50 = 16 nM).{16431} Levels of HDL cholesterol are inversely correlated with endothelial lipase protein activity. Therefore, inhibition of endothelial lipase by compounds like GSK264220A may be expected to increase HDL levels and potentially decrease the risk of cardiovascular disease.
Brand:CaymanSKU:13009 - 1 mgAvailable on backorder
Endothelial lipase, a member of the triglyceride lipase gene family expressed in endothelial cells, prefers phospholipid-enriched high-density lipoprotein (HDL) over triglyceride as substrate. GSK264220A is a potent inhibitor of endothelial lipase (IC50 = 16 nM).{16431} Levels of HDL cholesterol are inversely correlated with endothelial lipase protein activity. Therefore, inhibition of endothelial lipase by compounds like GSK264220A may be expected to increase HDL levels and potentially decrease the risk of cardiovascular disease.
Brand:CaymanSKU:13009 - 10 mgAvailable on backorder
Endothelial lipase, a member of the triglyceride lipase gene family expressed in endothelial cells, prefers phospholipid-enriched high-density lipoprotein (HDL) over triglyceride as substrate. GSK264220A is a potent inhibitor of endothelial lipase (IC50 = 16 nM).{16431} Levels of HDL cholesterol are inversely correlated with endothelial lipase protein activity. Therefore, inhibition of endothelial lipase by compounds like GSK264220A may be expected to increase HDL levels and potentially decrease the risk of cardiovascular disease.
Brand:CaymanSKU:13009 - 25 mgAvailable on backorder
Endothelial lipase, a member of the triglyceride lipase gene family expressed in endothelial cells, prefers phospholipid-enriched high-density lipoprotein (HDL) over triglyceride as substrate. GSK264220A is a potent inhibitor of endothelial lipase (IC50 = 16 nM).{16431} Levels of HDL cholesterol are inversely correlated with endothelial lipase protein activity. Therefore, inhibition of endothelial lipase by compounds like GSK264220A may be expected to increase HDL levels and potentially decrease the risk of cardiovascular disease.
Brand:CaymanSKU:13009 - 5 mgAvailable on backorder
GSK2656157 is an inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK; IC50 = 0.9 nM).{32772,32773} It is selective for PERK over a panel of additional kinases.{32772} GSK2656157 blocks both stress-induced PERK autophosphorylation and eIF2α substrate phosphorylation and decreases levels of ATF4 and CHOP in multiple cell lines.{32772} It is orally bioavailable, suppressing PERK autophosphorylation in mouse pancreas and inhibiting the growth of multiple human tumor xenografts in mice.{32772,32773} GSK2656157 inhibits caspase 1 activation in macrophage-like J774.1 cells, preventing LPS-induced IL-1β production, through its effects on the PERK/eIF2α pathway.{32771}
Brand:CaymanSKU:-Available on backorder
GSK2656157 is an inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK; IC50 = 0.9 nM).{32772,32773} It is selective for PERK over a panel of additional kinases.{32772} GSK2656157 blocks both stress-induced PERK autophosphorylation and eIF2α substrate phosphorylation and decreases levels of ATF4 and CHOP in multiple cell lines.{32772} It is orally bioavailable, suppressing PERK autophosphorylation in mouse pancreas and inhibiting the growth of multiple human tumor xenografts in mice.{32772,32773} GSK2656157 inhibits caspase 1 activation in macrophage-like J774.1 cells, preventing LPS-induced IL-1β production, through its effects on the PERK/eIF2α pathway.{32771}
Brand:CaymanSKU:-Available on backorder
GSK2656157 is an inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK; IC50 = 0.9 nM).{32772,32773} It is selective for PERK over a panel of additional kinases.{32772} GSK2656157 blocks both stress-induced PERK autophosphorylation and eIF2α substrate phosphorylation and decreases levels of ATF4 and CHOP in multiple cell lines.{32772} It is orally bioavailable, suppressing PERK autophosphorylation in mouse pancreas and inhibiting the growth of multiple human tumor xenografts in mice.{32772,32773} GSK2656157 inhibits caspase 1 activation in macrophage-like J774.1 cells, preventing LPS-induced IL-1β production, through its effects on the PERK/eIF2α pathway.{32771}
Brand:CaymanSKU:-Available on backorder
GSK2656157 is an inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK; IC50 = 0.9 nM).{32772,32773} It is selective for PERK over a panel of additional kinases.{32772} GSK2656157 blocks both stress-induced PERK autophosphorylation and eIF2α substrate phosphorylation and decreases levels of ATF4 and CHOP in multiple cell lines.{32772} It is orally bioavailable, suppressing PERK autophosphorylation in mouse pancreas and inhibiting the growth of multiple human tumor xenografts in mice.{32772,32773} GSK2656157 inhibits caspase 1 activation in macrophage-like J774.1 cells, preventing LPS-induced IL-1β production, through its effects on the PERK/eIF2α pathway.{32771}
Brand:CaymanSKU:-Available on backorder
Two Rho-associated kinases (ROCKS), ROCK-I and ROCK-II, act downstream of the G protein Rho to regulate cytoskeletal stability. The ROCKs play important roles in diverse cellular functions including cell adhesion and proliferation, smooth muscle contraction, and stem cell renewal. GSK269962 is a selective ROCK inhibitor with IC50 values of 1.6 and 6 nM for ROCK-I and ROCK-II, respectively.{16599} It displays greater than 30-fold selectivity for ROCK against a panel of serine/threonine kinases.{16599} GSK269962 has been shown to block the generation of inflammatory cytokines in lipopolysaccharide-stimulated monocytes and to induce vasorelaxation in preconstricted rat aorta (IC50 = 35 nM).{16599} Oral administration of 1-30 mg/kg GSK269962 can dose-dependently lower blood pressure in spontaneously hypertensive rats.{16599}
Brand:CaymanSKU:-Available on backorder
Two Rho-associated kinases (ROCKS), ROCK-I and ROCK-II, act downstream of the G protein Rho to regulate cytoskeletal stability. The ROCKs play important roles in diverse cellular functions including cell adhesion and proliferation, smooth muscle contraction, and stem cell renewal. GSK269962 is a selective ROCK inhibitor with IC50 values of 1.6 and 6 nM for ROCK-I and ROCK-II, respectively.{16599} It displays greater than 30-fold selectivity for ROCK against a panel of serine/threonine kinases.{16599} GSK269962 has been shown to block the generation of inflammatory cytokines in lipopolysaccharide-stimulated monocytes and to induce vasorelaxation in preconstricted rat aorta (IC50 = 35 nM).{16599} Oral administration of 1-30 mg/kg GSK269962 can dose-dependently lower blood pressure in spontaneously hypertensive rats.{16599}
Brand:CaymanSKU:-Available on backorder
Two Rho-associated kinases (ROCKS), ROCK-I and ROCK-II, act downstream of the G protein Rho to regulate cytoskeletal stability. The ROCKs play important roles in diverse cellular functions including cell adhesion and proliferation, smooth muscle contraction, and stem cell renewal. GSK269962 is a selective ROCK inhibitor with IC50 values of 1.6 and 6 nM for ROCK-I and ROCK-II, respectively.{16599} It displays greater than 30-fold selectivity for ROCK against a panel of serine/threonine kinases.{16599} GSK269962 has been shown to block the generation of inflammatory cytokines in lipopolysaccharide-stimulated monocytes and to induce vasorelaxation in preconstricted rat aorta (IC50 = 35 nM).{16599} Oral administration of 1-30 mg/kg GSK269962 can dose-dependently lower blood pressure in spontaneously hypertensive rats.{16599}
Brand:CaymanSKU:-Available on backorder
Two Rho-associated kinases (ROCKS), ROCK-I and ROCK-II, act downstream of the G protein Rho to regulate cytoskeletal stability. The ROCKs play important roles in diverse cellular functions including cell adhesion and proliferation, smooth muscle contraction, and stem cell renewal. GSK269962 is a selective ROCK inhibitor with IC50 values of 1.6 and 6 nM for ROCK-I and ROCK-II, respectively.{16599} It displays greater than 30-fold selectivity for ROCK against a panel of serine/threonine kinases.{16599} GSK269962 has been shown to block the generation of inflammatory cytokines in lipopolysaccharide-stimulated monocytes and to induce vasorelaxation in preconstricted rat aorta (IC50 = 35 nM).{16599} Oral administration of 1-30 mg/kg GSK269962 can dose-dependently lower blood pressure in spontaneously hypertensive rats.{16599}
Brand:CaymanSKU:-Available on backorder
BAZ2A/B are bromodomain-containing proteins whose biological function is believed to function similarly to ACF1, the Drosophila BAZ2B ortholog. ACF complexes play roles in establishing regular nucleosome spacing during chromatin assembly and influencing different remodeling outcomes at target loci.{21672,21674} BAZ2A and BAZ2B constitute the central scaffolding protein of the nucleolar remodeling complex (NoRC) that regulates the expression of noncoding RNAs. GSK2801 is a selective, cell-permeable inhibitor of the BAZ2 family of bromodomain-containing proteins (IC50s = 9-350 nM in a BAZ2B AlphaScreen).{29090,26201} It binds to BAZ2A and BAZ2B with Kd values of 0.26 and 0.14 µM, respectively, and does not interact with the bromodomains of BRD4(BD1), CREBBP, TRIM24/TIF1α, PB1(BD5), PCAF, or ATAD2.{29090,26201} See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:- BAZ2A/B are bromodomain-containing proteins whose biological function is believed to function similarly to ACF1, the Drosophila BAZ2B ortholog. ACF complexes play roles in establishing regular nucleosome spacing during chromatin assembly and influencing different remodeling outcomes at target loci.{21672,21674} BAZ2A and BAZ2B constitute the central scaffolding protein of the nucleolar remodeling complex (NoRC) that regulates the expression of noncoding RNAs. GSK2801 is a selective, cell-permeable inhibitor of the BAZ2 family of bromodomain-containing proteins (IC50s = 9-350 nM in a BAZ2B AlphaScreen).{29090,26201} It binds to BAZ2A and BAZ2B with Kd values of 0.26 and 0.14 µM, respectively, and does not interact with the bromodomains of BRD4(BD1), CREBBP, TRIM24/TIF1α, PB1(BD5), PCAF, or ATAD2.{29090,26201} See the Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:-
The wild-type p53-induced phosphatase Wip1, also known as protein phosphatase magnesium-dependent 1 delta (PPM1D) or PP2Cδ, modulates cell cycling and may contribute to some forms of cancer.{27983,27982} GSK2830371 is a potent inhibitor of Wip1 (IC50 = 6 nM).{27981} It displays selectivity for Wip1 over 21 other phosphatases.{27981} GSK2830371 increases phosphorylation of Wip1 substrates and blocks cell cycling in hematopoietic cancer cells and in Wip1-amplified cancer cells with wild-type p53.{27981} This compound is orally bioavailable and causes inhibition of lymphoma xenograft growth in mice.{27981}
Brand:CaymanSKU:-Out of stock
The wild-type p53-induced phosphatase Wip1, also known as protein phosphatase magnesium-dependent 1 delta (PPM1D) or PP2Cδ, modulates cell cycling and may contribute to some forms of cancer.{27983,27982} GSK2830371 is a potent inhibitor of Wip1 (IC50 = 6 nM).{27981} It displays selectivity for Wip1 over 21 other phosphatases.{27981} GSK2830371 increases phosphorylation of Wip1 substrates and blocks cell cycling in hematopoietic cancer cells and in Wip1-amplified cancer cells with wild-type p53.{27981} This compound is orally bioavailable and causes inhibition of lymphoma xenograft growth in mice.{27981}
Brand:CaymanSKU:-Out of stock
The wild-type p53-induced phosphatase Wip1, also known as protein phosphatase magnesium-dependent 1 delta (PPM1D) or PP2Cδ, modulates cell cycling and may contribute to some forms of cancer.{27983,27982} GSK2830371 is a potent inhibitor of Wip1 (IC50 = 6 nM).{27981} It displays selectivity for Wip1 over 21 other phosphatases.{27981} GSK2830371 increases phosphorylation of Wip1 substrates and blocks cell cycling in hematopoietic cancer cells and in Wip1-amplified cancer cells with wild-type p53.{27981} This compound is orally bioavailable and causes inhibition of lymphoma xenograft growth in mice.{27981}
Brand:CaymanSKU:-Out of stock
The wild-type p53-induced phosphatase Wip1, also known as protein phosphatase magnesium-dependent 1 delta (PPM1D) or PP2Cδ, modulates cell cycling and may contribute to some forms of cancer.{27983,27982} GSK2830371 is a potent inhibitor of Wip1 (IC50 = 6 nM).{27981} It displays selectivity for Wip1 over 21 other phosphatases.{27981} GSK2830371 increases phosphorylation of Wip1 substrates and blocks cell cycling in hematopoietic cancer cells and in Wip1-amplified cancer cells with wild-type p53.{27981} This compound is orally bioavailable and causes inhibition of lymphoma xenograft growth in mice.{27981}
Brand:CaymanSKU:-Out of stock
GSK2837808A is a potent inhibitor of lactate dehydrogenase (LDH) A and B (IC50s = 2.6 and 0.43 nM, for human recombinant LDHA and LDHB, respectively).{35109} It inhibits lactate production in Snu398 hepatocellular carcinoma cells in which LDHB expression is undetectable (EC50 = 400 nM). GSK2837808A (10 µM) reduces glucose consumption in Snu398 but not HepG2 hepatocellular carcinoma cells. A panel of 30 cancer cell lines, with varying levels of LDHA and LDHB expression, shows differential sensitivities to GSK2837808A with EC50s ranging from 400 nM to 30 µM. The potency of GSK2837808A does not correlate with LDHA, LDHB, or total LDH expression levels.
Brand:CaymanSKU:20626 -Available on backorder
GSK2837808A is a potent inhibitor of lactate dehydrogenase (LDH) A and B (IC50s = 2.6 and 0.43 nM, for human recombinant LDHA and LDHB, respectively).{35109} It inhibits lactate production in Snu398 hepatocellular carcinoma cells in which LDHB expression is undetectable (EC50 = 400 nM). GSK2837808A (10 µM) reduces glucose consumption in Snu398 but not HepG2 hepatocellular carcinoma cells. A panel of 30 cancer cell lines, with varying levels of LDHA and LDHB expression, shows differential sensitivities to GSK2837808A with EC50s ranging from 400 nM to 30 µM. The potency of GSK2837808A does not correlate with LDHA, LDHB, or total LDH expression levels.
Brand:CaymanSKU:20626 -Available on backorder
GSK2837808A is a potent inhibitor of lactate dehydrogenase (LDH) A and B (IC50s = 2.6 and 0.43 nM, for human recombinant LDHA and LDHB, respectively).{35109} It inhibits lactate production in Snu398 hepatocellular carcinoma cells in which LDHB expression is undetectable (EC50 = 400 nM). GSK2837808A (10 µM) reduces glucose consumption in Snu398 but not HepG2 hepatocellular carcinoma cells. A panel of 30 cancer cell lines, with varying levels of LDHA and LDHB expression, shows differential sensitivities to GSK2837808A with EC50s ranging from 400 nM to 30 µM. The potency of GSK2837808A does not correlate with LDHA, LDHB, or total LDH expression levels.
Brand:CaymanSKU:20626 -Available on backorder
GSK2837808A is a potent inhibitor of lactate dehydrogenase (LDH) A and B (IC50s = 2.6 and 0.43 nM, for human recombinant LDHA and LDHB, respectively).{35109} It inhibits lactate production in Snu398 hepatocellular carcinoma cells in which LDHB expression is undetectable (EC50 = 400 nM). GSK2837808A (10 µM) reduces glucose consumption in Snu398 but not HepG2 hepatocellular carcinoma cells. A panel of 30 cancer cell lines, with varying levels of LDHA and LDHB expression, shows differential sensitivities to GSK2837808A with EC50s ranging from 400 nM to 30 µM. The potency of GSK2837808A does not correlate with LDHA, LDHB, or total LDH expression levels.
Brand:CaymanSKU:20626 -Available on backorder
GSK2838232 is a second generation inhibitor of HIV-1 maturation (IC90 = 6.4 nM).{42480} It is active against a variety of HIV isolates resistant to bevirimat (PA-457; Item No. 21339).{42481}
Brand:CaymanSKU:21390 -Out of stock
GSK2838232 is a second generation inhibitor of HIV-1 maturation (IC90 = 6.4 nM).{42480} It is active against a variety of HIV isolates resistant to bevirimat (PA-457; Item No. 21339).{42481}
Brand:CaymanSKU:21390 -Out of stock
GSK2838232 is a second generation inhibitor of HIV-1 maturation (IC90 = 6.4 nM).{42480} It is active against a variety of HIV isolates resistant to bevirimat (PA-457; Item No. 21339).{42481}
Brand:CaymanSKU:21390 -Out of stock
GSK2838232 is a second generation inhibitor of HIV-1 maturation (IC90 = 6.4 nM).{42480} It is active against a variety of HIV isolates resistant to bevirimat (PA-457; Item No. 21339).{42481}
Brand:CaymanSKU:21390 -Out of stock
GSK2879552 is a selective, orally bioavailable, mechanism-based inactivator of lysine-specific demethylase 1 (LSD1)/corepressor for element-1-silencing transcription factor (CoREST) activity.{31307} Inhibition of LSD1 via GSK2879552 has been shown to enhance H3K4 methylation and to increase the expression of tumor-suppressor genes.{31307,31138} GSK2879552 demonstrates anti-proliferative growth effects (EC50s = 2-240 nM) in AML cell lines and is currently under clinical evaluation for cancer treatment.{31307,31139}
Brand:CaymanSKU:-Available on backorder
GSK2879552 is a selective, orally bioavailable, mechanism-based inactivator of lysine-specific demethylase 1 (LSD1)/corepressor for element-1-silencing transcription factor (CoREST) activity.{31307} Inhibition of LSD1 via GSK2879552 has been shown to enhance H3K4 methylation and to increase the expression of tumor-suppressor genes.{31307,31138} GSK2879552 demonstrates anti-proliferative growth effects (EC50s = 2-240 nM) in AML cell lines and is currently under clinical evaluation for cancer treatment.{31307,31139}
Brand:CaymanSKU:-Available on backorder
GSK2879552 is a selective, orally bioavailable, mechanism-based inactivator of lysine-specific demethylase 1 (LSD1)/corepressor for element-1-silencing transcription factor (CoREST) activity.{31307} Inhibition of LSD1 via GSK2879552 has been shown to enhance H3K4 methylation and to increase the expression of tumor-suppressor genes.{31307,31138} GSK2879552 demonstrates anti-proliferative growth effects (EC50s = 2-240 nM) in AML cell lines and is currently under clinical evaluation for cancer treatment.{31307,31139}
Brand:CaymanSKU:-Available on backorder
GSK2879552 is a selective, orally bioavailable, mechanism-based inactivator of lysine-specific demethylase 1 (LSD1)/corepressor for element-1-silencing transcription factor (CoREST) activity.{31307} Inhibition of LSD1 via GSK2879552 has been shown to enhance H3K4 methylation and to increase the expression of tumor-suppressor genes.{31307,31138} GSK2879552 demonstrates anti-proliferative growth effects (EC50s = 2-240 nM) in AML cell lines and is currently under clinical evaluation for cancer treatment.{31307,31139}
Brand:CaymanSKU:-Available on backorder
GSK2881078 is a selective androgen receptor modulator (SARM) that is being evaluated for effects on muscle growth and strength in subjects with muscle wasting to improve their physical function. It is currently in phase I clinical trials.
Brand:CaymanSKU:20313 -Available on backorder
GSK2881078 is a selective androgen receptor modulator (SARM) that is being evaluated for effects on muscle growth and strength in subjects with muscle wasting to improve their physical function. It is currently in phase I clinical trials.
Brand:CaymanSKU:20313 -Available on backorder
GSK2881078 is a selective androgen receptor modulator (SARM) that is being evaluated for effects on muscle growth and strength in subjects with muscle wasting to improve their physical function. It is currently in phase I clinical trials.
Brand:CaymanSKU:20313 -Available on backorder
GSK2881078 is a selective androgen receptor modulator (SARM) that is being evaluated for effects on muscle growth and strength in subjects with muscle wasting to improve their physical function. It is currently in phase I clinical trials.
Brand:CaymanSKU:20313 -Available on backorder
GSK2981278 is a highly selective, potent small molecule inhibitor of the retinoic acid receptor-related orphan receptor γ (RORγ). This agent inhibits IL-17A and IL-22 protein secretion from human T cells grown under Th17 skewing conditions in a concentration-dependent manner, with an IC50 value of 3.2 nM.{34217} GSK2981278 also significantly inhibits RORγ transactivation in CHO and Jurkat cells at tested concentrations of 0.1-10 µM.{34217} Topical treatment with GSK2981278 (1% ointment) reduces dermal symptoms in an imiquimod mouse model of psoriasis.{34217} A formulation of this compound is currently in clinical trials to investigate its potential effectiveness against psoriasis.
Brand:CaymanSKU:20974 -Out of stock
GSK2981278 is a highly selective, potent small molecule inhibitor of the retinoic acid receptor-related orphan receptor γ (RORγ). This agent inhibits IL-17A and IL-22 protein secretion from human T cells grown under Th17 skewing conditions in a concentration-dependent manner, with an IC50 value of 3.2 nM.{34217} GSK2981278 also significantly inhibits RORγ transactivation in CHO and Jurkat cells at tested concentrations of 0.1-10 µM.{34217} Topical treatment with GSK2981278 (1% ointment) reduces dermal symptoms in an imiquimod mouse model of psoriasis.{34217} A formulation of this compound is currently in clinical trials to investigate its potential effectiveness against psoriasis.
Brand:CaymanSKU:20974 -Out of stock
GSK2981278 is a highly selective, potent small molecule inhibitor of the retinoic acid receptor-related orphan receptor γ (RORγ). This agent inhibits IL-17A and IL-22 protein secretion from human T cells grown under Th17 skewing conditions in a concentration-dependent manner, with an IC50 value of 3.2 nM.{34217} GSK2981278 also significantly inhibits RORγ transactivation in CHO and Jurkat cells at tested concentrations of 0.1-10 µM.{34217} Topical treatment with GSK2981278 (1% ointment) reduces dermal symptoms in an imiquimod mouse model of psoriasis.{34217} A formulation of this compound is currently in clinical trials to investigate its potential effectiveness against psoriasis.
Brand:CaymanSKU:20974 -Out of stock
GSK2981278 is a highly selective, potent small molecule inhibitor of the retinoic acid receptor-related orphan receptor γ (RORγ). This agent inhibits IL-17A and IL-22 protein secretion from human T cells grown under Th17 skewing conditions in a concentration-dependent manner, with an IC50 value of 3.2 nM.{34217} GSK2981278 also significantly inhibits RORγ transactivation in CHO and Jurkat cells at tested concentrations of 0.1-10 µM.{34217} Topical treatment with GSK2981278 (1% ointment) reduces dermal symptoms in an imiquimod mouse model of psoriasis.{34217} A formulation of this compound is currently in clinical trials to investigate its potential effectiveness against psoriasis.
Brand:CaymanSKU:20974 -Out of stock
GSK2982772 is an inhibitor of receptor interacting serine/threonine kinase 1 (RIPK1; IC50s = 16 and 2,500 nM for the human and mouse enzymes, respectively).{49425} It is greater than 10,000-fold selective for RIPK1 over a panel of 339 kinases at 10 µM. GSK2982772 inhibits necrotic cell death induced by a combination of TNF-α and the caspase inhibitor QVD-OPh in U937 human monocytic and L929 murine fibrosarcoma cells (IC50s = 6.3 and 1,300 nM, respectively). GSK2982772 (3-300 nM) decreases IL-1β and IL-6 levels in intestinal mucosa tissue isolated from patients with ulcerative colitis. It increases survival in a mouse model of TNF-α-induced lethal shock when administered at doses of 3, 10, and 50 mg/kg.
Brand:CaymanSKU:29230 - 1 mgAvailable on backorder
GSK2982772 is an inhibitor of receptor interacting serine/threonine kinase 1 (RIPK1; IC50s = 16 and 2,500 nM for the human and mouse enzymes, respectively).{49425} It is greater than 10,000-fold selective for RIPK1 over a panel of 339 kinases at 10 µM. GSK2982772 inhibits necrotic cell death induced by a combination of TNF-α and the caspase inhibitor QVD-OPh in U937 human monocytic and L929 murine fibrosarcoma cells (IC50s = 6.3 and 1,300 nM, respectively). GSK2982772 (3-300 nM) decreases IL-1β and IL-6 levels in intestinal mucosa tissue isolated from patients with ulcerative colitis. It increases survival in a mouse model of TNF-α-induced lethal shock when administered at doses of 3, 10, and 50 mg/kg.
Brand:CaymanSKU:29230 - 10 mgAvailable on backorder
GSK2982772 is an inhibitor of receptor interacting serine/threonine kinase 1 (RIPK1; IC50s = 16 and 2,500 nM for the human and mouse enzymes, respectively).{49425} It is greater than 10,000-fold selective for RIPK1 over a panel of 339 kinases at 10 µM. GSK2982772 inhibits necrotic cell death induced by a combination of TNF-α and the caspase inhibitor QVD-OPh in U937 human monocytic and L929 murine fibrosarcoma cells (IC50s = 6.3 and 1,300 nM, respectively). GSK2982772 (3-300 nM) decreases IL-1β and IL-6 levels in intestinal mucosa tissue isolated from patients with ulcerative colitis. It increases survival in a mouse model of TNF-α-induced lethal shock when administered at doses of 3, 10, and 50 mg/kg.
Brand:CaymanSKU:29230 - 5 mgAvailable on backorder
GSK2983559 is a receptor-interacting protein kinase 2 (RIPK2) inhibitor.{54446} It inhibits RIPK2 by 65% in a kinase assay when used at a concentration of 10 µM. GSK2983559 (10 µM) also inhibits VEGFR3 by greater than 90%, as well as 14 additional kinases by 60 to 89% in a panel of 344 kinases. In vivo, GSK2983559 (7.5 and 145 mg/kg twice per day) reduces colonic damage in a mouse model of TNBS-induced colitis. GSK2983559 is also a prodrug that is cleaved to an active metabolite in the gastrointestinal tract that inhibits RIPK2 more potently than GSK2983559.
Brand:CaymanSKU:31458 - 1 mgAvailable on backorder
GSK2983559 is a receptor-interacting protein kinase 2 (RIPK2) inhibitor.{54446} It inhibits RIPK2 by 65% in a kinase assay when used at a concentration of 10 µM. GSK2983559 (10 µM) also inhibits VEGFR3 by greater than 90%, as well as 14 additional kinases by 60 to 89% in a panel of 344 kinases. In vivo, GSK2983559 (7.5 and 145 mg/kg twice per day) reduces colonic damage in a mouse model of TNBS-induced colitis. GSK2983559 is also a prodrug that is cleaved to an active metabolite in the gastrointestinal tract that inhibits RIPK2 more potently than GSK2983559.
Brand:CaymanSKU:31458 - 10 mgAvailable on backorder
GSK2983559 is a receptor-interacting protein kinase 2 (RIPK2) inhibitor.{54446} It inhibits RIPK2 by 65% in a kinase assay when used at a concentration of 10 µM. GSK2983559 (10 µM) also inhibits VEGFR3 by greater than 90%, as well as 14 additional kinases by 60 to 89% in a panel of 344 kinases. In vivo, GSK2983559 (7.5 and 145 mg/kg twice per day) reduces colonic damage in a mouse model of TNBS-induced colitis. GSK2983559 is also a prodrug that is cleaved to an active metabolite in the gastrointestinal tract that inhibits RIPK2 more potently than GSK2983559.
Brand:CaymanSKU:31458 - 25 mgAvailable on backorder
GSK2983559 is a receptor-interacting protein kinase 2 (RIPK2) inhibitor.{54446} It inhibits RIPK2 by 65% in a kinase assay when used at a concentration of 10 µM. GSK2983559 (10 µM) also inhibits VEGFR3 by greater than 90%, as well as 14 additional kinases by 60 to 89% in a panel of 344 kinases. In vivo, GSK2983559 (7.5 and 145 mg/kg twice per day) reduces colonic damage in a mouse model of TNBS-induced colitis. GSK2983559 is also a prodrug that is cleaved to an active metabolite in the gastrointestinal tract that inhibits RIPK2 more potently than GSK2983559.
Brand:CaymanSKU:31458 - 5 mgAvailable on backorder
GSK3 Inhibitor XIII is an aminopyrazole ATP-competitive inhibitor of glycogen synthase kinase 3 (GSK3), with 34% inhibition when used at a concentration of 2.5 µM.{40152} It inhibits androgen receptor transactivation in 22Rv1, LNCaP, and LNCaP-SSR cell lines in a dose-dependent manner. It promotes nuclear export of the androgen receptor and decreases translocation to the nucleus in PC3 and PCa prostate cancer cells, respectively.{40152,40153} In HEK293 cells expressing the rat Nav1.2 channel, pretreatment with GSK3 inhibitor XIII dose-dependently potentiates peak current densities.{40151}
Brand:CaymanSKU:21190 -Out of stock
GSK3 Inhibitor XIII is an aminopyrazole ATP-competitive inhibitor of glycogen synthase kinase 3 (GSK3), with 34% inhibition when used at a concentration of 2.5 µM.{40152} It inhibits androgen receptor transactivation in 22Rv1, LNCaP, and LNCaP-SSR cell lines in a dose-dependent manner. It promotes nuclear export of the androgen receptor and decreases translocation to the nucleus in PC3 and PCa prostate cancer cells, respectively.{40152,40153} In HEK293 cells expressing the rat Nav1.2 channel, pretreatment with GSK3 inhibitor XIII dose-dependently potentiates peak current densities.{40151}
Brand:CaymanSKU:21190 -Out of stock