Chemicals
Showing 21301–21450 of 41137 results
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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
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
Brand:CaymanSKU:23846 - 10 mgAvailable on backorder
Brand:CaymanSKU:23846 - 25 mgAvailable on backorder
Brand:CaymanSKU:23846 - 5 mgAvailable on backorder
Brand:CaymanSKU:23846 - 50 mgAvailable on backorder
GSK3326595 is an inhibitor of protein arginine methyltransferase 5 (PRMT5).{47250} It inhibits methylation of peptides derived from the PRMT5 substrates histone H4 and H2A, SmD3, FUBP1, and HNRNPH1 by the PRMT5/MEP50 complex with IC50 values ranging from 5.9 to 19.7 nM and is more than 4,000-fold selective for PRMT5/MEP50 over a panel of 20 methyltransferases. GSK3326595 (200 nM) induces alternative splicing of MDM4 in Z-138, MCF-7, JM1, and DOHH-2 cells and increases p53 and p21 protein levels in Z-138 cells in a concentration-dependent manner. GSK3326595 inhibits growth and symmetric dimethyl arginine (SDMA) methylation in several lymphoma and breast cancer cell lines. It also reduces tumor growth in a Z-138 mouse xenograft model when administered at doses of 25, 50, and 100 mg/kg twice per day.
Brand:CaymanSKU:27305 - 1 mgAvailable on backorder
GSK3326595 is an inhibitor of protein arginine methyltransferase 5 (PRMT5).{47250} It inhibits methylation of peptides derived from the PRMT5 substrates histone H4 and H2A, SmD3, FUBP1, and HNRNPH1 by the PRMT5/MEP50 complex with IC50 values ranging from 5.9 to 19.7 nM and is more than 4,000-fold selective for PRMT5/MEP50 over a panel of 20 methyltransferases. GSK3326595 (200 nM) induces alternative splicing of MDM4 in Z-138, MCF-7, JM1, and DOHH-2 cells and increases p53 and p21 protein levels in Z-138 cells in a concentration-dependent manner. GSK3326595 inhibits growth and symmetric dimethyl arginine (SDMA) methylation in several lymphoma and breast cancer cell lines. It also reduces tumor growth in a Z-138 mouse xenograft model when administered at doses of 25, 50, and 100 mg/kg twice per day.
Brand:CaymanSKU:27305 - 10 mgAvailable on backorder
GSK3326595 is an inhibitor of protein arginine methyltransferase 5 (PRMT5).{47250} It inhibits methylation of peptides derived from the PRMT5 substrates histone H4 and H2A, SmD3, FUBP1, and HNRNPH1 by the PRMT5/MEP50 complex with IC50 values ranging from 5.9 to 19.7 nM and is more than 4,000-fold selective for PRMT5/MEP50 over a panel of 20 methyltransferases. GSK3326595 (200 nM) induces alternative splicing of MDM4 in Z-138, MCF-7, JM1, and DOHH-2 cells and increases p53 and p21 protein levels in Z-138 cells in a concentration-dependent manner. GSK3326595 inhibits growth and symmetric dimethyl arginine (SDMA) methylation in several lymphoma and breast cancer cell lines. It also reduces tumor growth in a Z-138 mouse xenograft model when administered at doses of 25, 50, and 100 mg/kg twice per day.
Brand:CaymanSKU:27305 - 25 mgAvailable on backorder
GSK3326595 is an inhibitor of protein arginine methyltransferase 5 (PRMT5).{47250} It inhibits methylation of peptides derived from the PRMT5 substrates histone H4 and H2A, SmD3, FUBP1, and HNRNPH1 by the PRMT5/MEP50 complex with IC50 values ranging from 5.9 to 19.7 nM and is more than 4,000-fold selective for PRMT5/MEP50 over a panel of 20 methyltransferases. GSK3326595 (200 nM) induces alternative splicing of MDM4 in Z-138, MCF-7, JM1, and DOHH-2 cells and increases p53 and p21 protein levels in Z-138 cells in a concentration-dependent manner. GSK3326595 inhibits growth and symmetric dimethyl arginine (SDMA) methylation in several lymphoma and breast cancer cell lines. It also reduces tumor growth in a Z-138 mouse xenograft model when administered at doses of 25, 50, and 100 mg/kg twice per day.
Brand:CaymanSKU:27305 - 5 mgAvailable on backorder
The histone H3 lysine 27 (H3K27) methyltransferase EZH2 plays an important role in regulating gene expression, and its aberrant activity is linked to the onset and progression of cancer.{18930} GSK343 is a cell-permeable EZH2 inhibitor (IC50 = 4 nM) that is 60-fold selective over EZH1 and >1,000-fold selective over other histone methytranferases.{24979} GSK343 has been shown to inhibit the trimethylation of H3K27 in HCC1806 cells with an IC50 value of 174 nM.{24979} See Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:- The histone H3 lysine 27 (H3K27) methyltransferase EZH2 plays an important role in regulating gene expression, and its aberrant activity is linked to the onset and progression of cancer.{18930} GSK343 is a cell-permeable EZH2 inhibitor (IC50 = 4 nM) that is 60-fold selective over EZH1 and >1,000-fold selective over other histone methytranferases.{24979} GSK343 has been shown to inhibit the trimethylation of H3K27 in HCC1806 cells with an IC50 value of 174 nM.{24979} See Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:- The histone H3 lysine 27 (H3K27) methyltransferase EZH2 plays an important role in regulating gene expression, and its aberrant activity is linked to the onset and progression of cancer.{18930} GSK343 is a cell-permeable EZH2 inhibitor (IC50 = 4 nM) that is 60-fold selective over EZH1 and >1,000-fold selective over other histone methytranferases.{24979} GSK343 has been shown to inhibit the trimethylation of H3K27 in HCC1806 cells with an IC50 value of 174 nM.{24979} See Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:- The histone H3 lysine 27 (H3K27) methyltransferase EZH2 plays an important role in regulating gene expression, and its aberrant activity is linked to the onset and progression of cancer.{18930} GSK343 is a cell-permeable EZH2 inhibitor (IC50 = 4 nM) that is 60-fold selective over EZH1 and >1,000-fold selective over other histone methytranferases.{24979} GSK343 has been shown to inhibit the trimethylation of H3K27 in HCC1806 cells with an IC50 value of 174 nM.{24979} See Structural Genomics Consortium (SGC) website for more information.
Brand:CaymanSKU:-
GSK356278 is a potent, selective, and orally bioavailable phosphodiesterase 4 (PDE4) inhibitor with anxiolytic and cognition-improving effects.{55071} It is greater than 100-fold selective for PDE4A, -B, and -D (IC50s = 2.51, 1.58, and 2 nM for PDE4A, PDE4B, and PDE4D, respectively) over 10 other members of the PDE family, as well as over a panel of 154 diverse receptors, ion channels, and enzymes. It inhibits LPS-induced release of TNF-α in isolated human whole blood (IC50 = 23.1 nM) and reduces LPS-induced neutrophilia in rats (ED50 = 0.09 mg/kg). GSK356278 (0.01-1 mg/kg) induces anxiolytic behavior in marmosets, and improves performance of non-human primates in an object retrieval test when administered at a dose of 1 mg/kg.
Brand:CaymanSKU:30412 - 10 mgAvailable on backorder
GSK356278 is a potent, selective, and orally bioavailable phosphodiesterase 4 (PDE4) inhibitor with anxiolytic and cognition-improving effects.{55071} It is greater than 100-fold selective for PDE4A, -B, and -D (IC50s = 2.51, 1.58, and 2 nM for PDE4A, PDE4B, and PDE4D, respectively) over 10 other members of the PDE family, as well as over a panel of 154 diverse receptors, ion channels, and enzymes. It inhibits LPS-induced release of TNF-α in isolated human whole blood (IC50 = 23.1 nM) and reduces LPS-induced neutrophilia in rats (ED50 = 0.09 mg/kg). GSK356278 (0.01-1 mg/kg) induces anxiolytic behavior in marmosets, and improves performance of non-human primates in an object retrieval test when administered at a dose of 1 mg/kg.
Brand:CaymanSKU:30412 - 25 mgAvailable on backorder
GSK356278 is a potent, selective, and orally bioavailable phosphodiesterase 4 (PDE4) inhibitor with anxiolytic and cognition-improving effects.{55071} It is greater than 100-fold selective for PDE4A, -B, and -D (IC50s = 2.51, 1.58, and 2 nM for PDE4A, PDE4B, and PDE4D, respectively) over 10 other members of the PDE family, as well as over a panel of 154 diverse receptors, ion channels, and enzymes. It inhibits LPS-induced release of TNF-α in isolated human whole blood (IC50 = 23.1 nM) and reduces LPS-induced neutrophilia in rats (ED50 = 0.09 mg/kg). GSK356278 (0.01-1 mg/kg) induces anxiolytic behavior in marmosets, and improves performance of non-human primates in an object retrieval test when administered at a dose of 1 mg/kg.
Brand:CaymanSKU:30412 - 5 mgAvailable on backorder
GSK356278 is a potent, selective, and orally bioavailable phosphodiesterase 4 (PDE4) inhibitor with anxiolytic and cognition-improving effects.{55071} It is greater than 100-fold selective for PDE4A, -B, and -D (IC50s = 2.51, 1.58, and 2 nM for PDE4A, PDE4B, and PDE4D, respectively) over 10 other members of the PDE family, as well as over a panel of 154 diverse receptors, ion channels, and enzymes. It inhibits LPS-induced release of TNF-α in isolated human whole blood (IC50 = 23.1 nM) and reduces LPS-induced neutrophilia in rats (ED50 = 0.09 mg/kg). GSK356278 (0.01-1 mg/kg) induces anxiolytic behavior in marmosets, and improves performance of non-human primates in an object retrieval test when administered at a dose of 1 mg/kg.
Brand:CaymanSKU:30412 - 50 mgAvailable on backorder
PPARβ/δ is thought to play a role in lipid homeostasis and glucose disposal by regulating genes involved in fatty acid oxidation, reverse cholesterol transport, and carbon substrate utilization in skeletal muscle. It has also been implicated in the progression of certain cancers.{14613,15911,20406,20389} GSK3787 is an irreversible antagonist of PPARβ/δ (pIC50 = 6.6) with no measurable affinity for PPARα or PPARγ (pIC50 >5).{20391} At 1μM, it inhibits the expression of PPARβ/δ-regulated target genes, pyruvate dehydrogenase kinase 4 and carnitine palmitoyl transferase 1a, which are important for energy homeostasis in human skeletal muscle cells.{20391} GSK3787 (at 1 μM) also antagonizes agonist-induced expression of angiopoietin-like protein 4 in mouse fibroblasts, mouse keratinocytes, and human MCF-7, Huh7, and HepG2 cancer cell lines.{24665}
Brand:CaymanSKU:- PPARβ/δ is thought to play a role in lipid homeostasis and glucose disposal by regulating genes involved in fatty acid oxidation, reverse cholesterol transport, and carbon substrate utilization in skeletal muscle. It has also been implicated in the progression of certain cancers.{14613,15911,20406,20389} GSK3787 is an irreversible antagonist of PPARβ/δ (pIC50 = 6.6) with no measurable affinity for PPARα or PPARγ (pIC50 >5).{20391} At 1μM, it inhibits the expression of PPARβ/δ-regulated target genes, pyruvate dehydrogenase kinase 4 and carnitine palmitoyl transferase 1a, which are important for energy homeostasis in human skeletal muscle cells.{20391} GSK3787 (at 1 μM) also antagonizes agonist-induced expression of angiopoietin-like protein 4 in mouse fibroblasts, mouse keratinocytes, and human MCF-7, Huh7, and HepG2 cancer cell lines.{24665}
Brand:CaymanSKU:- PPARβ/δ is thought to play a role in lipid homeostasis and glucose disposal by regulating genes involved in fatty acid oxidation, reverse cholesterol transport, and carbon substrate utilization in skeletal muscle. It has also been implicated in the progression of certain cancers.{14613,15911,20406,20389} GSK3787 is an irreversible antagonist of PPARβ/δ (pIC50 = 6.6) with no measurable affinity for PPARα or PPARγ (pIC50 >5).{20391} At 1μM, it inhibits the expression of PPARβ/δ-regulated target genes, pyruvate dehydrogenase kinase 4 and carnitine palmitoyl transferase 1a, which are important for energy homeostasis in human skeletal muscle cells.{20391} GSK3787 (at 1 μM) also antagonizes agonist-induced expression of angiopoietin-like protein 4 in mouse fibroblasts, mouse keratinocytes, and human MCF-7, Huh7, and HepG2 cancer cell lines.{24665}
Brand:CaymanSKU:- PPARβ/δ is thought to play a role in lipid homeostasis and glucose disposal by regulating genes involved in fatty acid oxidation, reverse cholesterol transport, and carbon substrate utilization in skeletal muscle. It has also been implicated in the progression of certain cancers.{14613,15911,20406,20389} GSK3787 is an irreversible antagonist of PPARβ/δ (pIC50 = 6.6) with no measurable affinity for PPARα or PPARγ (pIC50 >5).{20391} At 1μM, it inhibits the expression of PPARβ/δ-regulated target genes, pyruvate dehydrogenase kinase 4 and carnitine palmitoyl transferase 1a, which are important for energy homeostasis in human skeletal muscle cells.{20391} GSK3787 (at 1 μM) also antagonizes agonist-induced expression of angiopoietin-like protein 4 in mouse fibroblasts, mouse keratinocytes, and human MCF-7, Huh7, and HepG2 cancer cell lines.{24665}
Brand:CaymanSKU:-
GSK3β Inhibitor II is a potent inhibitor of glycogen synthase kinase-3β (GSK3β; IC50 = 390 nM) that does not inhibit GSK-3α.{32116} Also referred to as tip-oxadiazole, this compound blocks the functional regulation of p53 by GSK3β, decreasing levels of MDM2, p21, and Bax and modulating mitochondrial p53 apoptotic signaling.{32117} GSK3β Inhibitor II also blocks GSK3β-mediated Tau phosphorylation and Aβ25-35-induced memory impairment in mouse hippocampus.{32115}
Brand:CaymanSKU:-Available on backorder
GSK3β Inhibitor II is a potent inhibitor of glycogen synthase kinase-3β (GSK3β; IC50 = 390 nM) that does not inhibit GSK-3α.{32116} Also referred to as tip-oxadiazole, this compound blocks the functional regulation of p53 by GSK3β, decreasing levels of MDM2, p21, and Bax and modulating mitochondrial p53 apoptotic signaling.{32117} GSK3β Inhibitor II also blocks GSK3β-mediated Tau phosphorylation and Aβ25-35-induced memory impairment in mouse hippocampus.{32115}
Brand:CaymanSKU:-Available on backorder
GSK3β Inhibitor VIII is an ATP-competitive inhibitor of the serine/threonine kinase, glycogen synthase kinase 3β (Ki = 38 nM; IC50 = 104 nM).{24857} It does not significantly inhibit the closely related cyclin-dependent kinase (Cdk)2 or Cdk5 (Kis = > 100 μM).{24857} GSK3β Inhibitor VIII demonstrates neuroprotective effects by inhibiting tau phosphorylation (IC50 = 2.7 μM) at a GSK3-specific site (Ser396) in cells stably expressing human four-repeat tau protein and also by protecting β-amyloid-exposed N2A neuroblastoma cells against cell death.{24857}
Brand:CaymanSKU:- GSK3β Inhibitor VIII is an ATP-competitive inhibitor of the serine/threonine kinase, glycogen synthase kinase 3β (Ki = 38 nM; IC50 = 104 nM).{24857} It does not significantly inhibit the closely related cyclin-dependent kinase (Cdk)2 or Cdk5 (Kis = > 100 μM).{24857} GSK3β Inhibitor VIII demonstrates neuroprotective effects by inhibiting tau phosphorylation (IC50 = 2.7 μM) at a GSK3-specific site (Ser396) in cells stably expressing human four-repeat tau protein and also by protecting β-amyloid-exposed N2A neuroblastoma cells against cell death.{24857}
Brand:CaymanSKU:- GSK3β Inhibitor VIII is an ATP-competitive inhibitor of the serine/threonine kinase, glycogen synthase kinase 3β (Ki = 38 nM; IC50 = 104 nM).{24857} It does not significantly inhibit the closely related cyclin-dependent kinase (Cdk)2 or Cdk5 (Kis = > 100 μM).{24857} GSK3β Inhibitor VIII demonstrates neuroprotective effects by inhibiting tau phosphorylation (IC50 = 2.7 μM) at a GSK3-specific site (Ser396) in cells stably expressing human four-repeat tau protein and also by protecting β-amyloid-exposed N2A neuroblastoma cells against cell death.{24857}
Brand:CaymanSKU:-
GSK3β inhibitor XI is a potent inhibitor of glycogen synthase kinase 3β (GSK3β; Ki = 25 nM).{36403} It is selective for GSK3β over a panel of 79 kinases at a concentration of 10 μM. GSK3β inhibitor XI inhibits GSK3β in HEK293 cells (EC50 = 32 nM).
Brand:CaymanSKU:23940 - 1 mgAvailable on backorder
GSK3β inhibitor XVIII is an inhibitor of glycogen synthase kinase 3β (GSK3β; IC50 = 64 nM).{47416} It induces expression of a luciferase reporter in HEK293 cells expressing wild-type Wnt (EC50 = ~1.25 µM) but not in cells expressing a β-catenin/TCF binding site-mutant Wnt. GSK3β inhibitor XVIII increases β-catenin accumulation in the nucleus of HEK293 cells. It induces proliferation of R7T1 β-cells (EC50 = 1,143 nM), an effect that can be blocked by the COX and Wnt signaling inhibitor sulindac (Item No. 10004386), and rat primary β-cells.
Brand:CaymanSKU:21198 -Out of stock
GSK3β inhibitor XVIII is an inhibitor of glycogen synthase kinase 3β (GSK3β; IC50 = 64 nM).{47416} It induces expression of a luciferase reporter in HEK293 cells expressing wild-type Wnt (EC50 = ~1.25 µM) but not in cells expressing a β-catenin/TCF binding site-mutant Wnt. GSK3β inhibitor XVIII increases β-catenin accumulation in the nucleus of HEK293 cells. It induces proliferation of R7T1 β-cells (EC50 = 1,143 nM), an effect that can be blocked by the COX and Wnt signaling inhibitor sulindac (Item No. 10004386), and rat primary β-cells.
Brand:CaymanSKU:21198 -Out of stock
GSK3β inhibitor XVIII is an inhibitor of glycogen synthase kinase 3β (GSK3β; IC50 = 64 nM).{47416} It induces expression of a luciferase reporter in HEK293 cells expressing wild-type Wnt (EC50 = ~1.25 µM) but not in cells expressing a β-catenin/TCF binding site-mutant Wnt. GSK3β inhibitor XVIII increases β-catenin accumulation in the nucleus of HEK293 cells. It induces proliferation of R7T1 β-cells (EC50 = 1,143 nM), an effect that can be blocked by the COX and Wnt signaling inhibitor sulindac (Item No. 10004386), and rat primary β-cells.
Brand:CaymanSKU:21198 -Out of stock
GSK3β inhibitor XVIII is an inhibitor of glycogen synthase kinase 3β (GSK3β; IC50 = 64 nM).{47416} It induces expression of a luciferase reporter in HEK293 cells expressing wild-type Wnt (EC50 = ~1.25 µM) but not in cells expressing a β-catenin/TCF binding site-mutant Wnt. GSK3β inhibitor XVIII increases β-catenin accumulation in the nucleus of HEK293 cells. It induces proliferation of R7T1 β-cells (EC50 = 1,143 nM), an effect that can be blocked by the COX and Wnt signaling inhibitor sulindac (Item No. 10004386), and rat primary β-cells.
Brand:CaymanSKU:21198 -Out of stock
GSK4027 is a p300/CBP-associated factor (PCAF)/general control nonderepressible 5 (GCN5) bromodomain inhibitor (Ki = 1.4 nM; IC50 = 60 nM in a chromatin engagement assay).{42858} It is greater than 18,000-fold selective for PCAF and GCN5 over BET family bromodomains and greater than 70-fold selective over other bromodomain families in a BROMOscan assay.
Brand:CaymanSKU:23421 - 1 mgAvailable on backorder
GSK4027 is a p300/CBP-associated factor (PCAF)/general control nonderepressible 5 (GCN5) bromodomain inhibitor (Ki = 1.4 nM; IC50 = 60 nM in a chromatin engagement assay).{42858} It is greater than 18,000-fold selective for PCAF and GCN5 over BET family bromodomains and greater than 70-fold selective over other bromodomain families in a BROMOscan assay.
Brand:CaymanSKU:23421 - 10 mgAvailable on backorder
GSK4027 is a p300/CBP-associated factor (PCAF)/general control nonderepressible 5 (GCN5) bromodomain inhibitor (Ki = 1.4 nM; IC50 = 60 nM in a chromatin engagement assay).{42858} It is greater than 18,000-fold selective for PCAF and GCN5 over BET family bromodomains and greater than 70-fold selective over other bromodomain families in a BROMOscan assay.
Brand:CaymanSKU:23421 - 5 mgAvailable on backorder
REV-ERBα is a nuclear hormone receptor with roles in circadian rhythm, adipogenesis, lipid metabolism, and inflammation. It binds porphoryin heme and in response to fluctuations in heme levels in cells it recruits corepressors such as NCoR and HDAC3 to repress the transcription of key genes involved in metabolic and circadian pathways.{21478,21474} GSK4112 is a synthetic agonist for REV-ERBα (EC50 = 0.4 μM) that was designed to mimic the action of heme.{21476,21477} At 10 μM, GSK4112 can reset the circadian rhythm in a phasic manner by inhibiting expression of the circadian target gene bmal1 and reduce glucose output by 30% in mouse primary hepatocytes by repressing the expression of several gluconeogenic genes.{21476} GSK4112 has been used to investigate the function of REV-ERBα in the coordination of circadian rhythm and metabolism in rat ovaries.{21475}
Brand:CaymanSKU:11931 - 10 mgAvailable on backorder
REV-ERBα is a nuclear hormone receptor with roles in circadian rhythm, adipogenesis, lipid metabolism, and inflammation. It binds porphoryin heme and in response to fluctuations in heme levels in cells it recruits corepressors such as NCoR and HDAC3 to repress the transcription of key genes involved in metabolic and circadian pathways.{21478,21474} GSK4112 is a synthetic agonist for REV-ERBα (EC50 = 0.4 μM) that was designed to mimic the action of heme.{21476,21477} At 10 μM, GSK4112 can reset the circadian rhythm in a phasic manner by inhibiting expression of the circadian target gene bmal1 and reduce glucose output by 30% in mouse primary hepatocytes by repressing the expression of several gluconeogenic genes.{21476} GSK4112 has been used to investigate the function of REV-ERBα in the coordination of circadian rhythm and metabolism in rat ovaries.{21475}
Brand:CaymanSKU:11931 - 25 mgAvailable on backorder
REV-ERBα is a nuclear hormone receptor with roles in circadian rhythm, adipogenesis, lipid metabolism, and inflammation. It binds porphoryin heme and in response to fluctuations in heme levels in cells it recruits corepressors such as NCoR and HDAC3 to repress the transcription of key genes involved in metabolic and circadian pathways.{21478,21474} GSK4112 is a synthetic agonist for REV-ERBα (EC50 = 0.4 μM) that was designed to mimic the action of heme.{21476,21477} At 10 μM, GSK4112 can reset the circadian rhythm in a phasic manner by inhibiting expression of the circadian target gene bmal1 and reduce glucose output by 30% in mouse primary hepatocytes by repressing the expression of several gluconeogenic genes.{21476} GSK4112 has been used to investigate the function of REV-ERBα in the coordination of circadian rhythm and metabolism in rat ovaries.{21475}
Brand:CaymanSKU:11931 - 5 mgAvailable on backorder
REV-ERBα is a nuclear hormone receptor with roles in circadian rhythm, adipogenesis, lipid metabolism, and inflammation. It binds porphoryin heme and in response to fluctuations in heme levels in cells it recruits corepressors such as NCoR and HDAC3 to repress the transcription of key genes involved in metabolic and circadian pathways.{21478,21474} GSK4112 is a synthetic agonist for REV-ERBα (EC50 = 0.4 μM) that was designed to mimic the action of heme.{21476,21477} At 10 μM, GSK4112 can reset the circadian rhythm in a phasic manner by inhibiting expression of the circadian target gene bmal1 and reduce glucose output by 30% in mouse primary hepatocytes by repressing the expression of several gluconeogenic genes.{21476} GSK4112 has been used to investigate the function of REV-ERBα in the coordination of circadian rhythm and metabolism in rat ovaries.{21475}
Brand:CaymanSKU:11931 - 50 mgAvailable on backorder
GSK429286A is a cell-permeable inhibitor of Rho-associated kinase (IC50 = 14 nM).{26327} It less potently inhibits p90 and p70 ribosomal S6 kinases (IC50s = 780 and 1,940 nM, respectively) and is ineffective against leucine-rich repeat protein kinase-2.{26327,26328} GSK429286A reverses adrenalin-induced contraction of rat aortic rings (IC50 = 190 nM) and produces a dose-dependent decrease in mean arterial pressure in spontaneously-hypertensive rats.{26327}
Brand:CaymanSKU:- GSK429286A is a cell-permeable inhibitor of Rho-associated kinase (IC50 = 14 nM).{26327} It less potently inhibits p90 and p70 ribosomal S6 kinases (IC50s = 780 and 1,940 nM, respectively) and is ineffective against leucine-rich repeat protein kinase-2.{26327,26328} GSK429286A reverses adrenalin-induced contraction of rat aortic rings (IC50 = 190 nM) and produces a dose-dependent decrease in mean arterial pressure in spontaneously-hypertensive rats.{26327}
Brand:CaymanSKU:- GSK429286A is a cell-permeable inhibitor of Rho-associated kinase (IC50 = 14 nM).{26327} It less potently inhibits p90 and p70 ribosomal S6 kinases (IC50s = 780 and 1,940 nM, respectively) and is ineffective against leucine-rich repeat protein kinase-2.{26327,26328} GSK429286A reverses adrenalin-induced contraction of rat aortic rings (IC50 = 190 nM) and produces a dose-dependent decrease in mean arterial pressure in spontaneously-hypertensive rats.{26327}
Brand:CaymanSKU:-
Polo-like kinases (Plks) are serine/threonine kinases with key roles in cell cycling.{29228} GSK461364 is a potent, reversible inhibitor of Plk1 (Ki = 2.2 nM).{29227} It is less effective against Plk2 and Plk3 (Kis = 860 and 1,000 nM, respectively) and at least 1,000-fold selective for Plk1 over a panel of 48 other kinases.{29227} GSK461364 dose-dependently halts cell cycling in diverse proliferating cancer cell lines and, at higher doses, triggers apoptosis.{29227} It appears to be more effective against p53-deficient tumors and is able to cross the blood-brain barrier.{29226,29225} GSK461364 is effective in vivo, inducing tumor growth inhibition or growth delay in xenograft models in mice.{29228,29227}
Brand:CaymanSKU:-Available on backorder
Polo-like kinases (Plks) are serine/threonine kinases with key roles in cell cycling.{29228} GSK461364 is a potent, reversible inhibitor of Plk1 (Ki = 2.2 nM).{29227} It is less effective against Plk2 and Plk3 (Kis = 860 and 1,000 nM, respectively) and at least 1,000-fold selective for Plk1 over a panel of 48 other kinases.{29227} GSK461364 dose-dependently halts cell cycling in diverse proliferating cancer cell lines and, at higher doses, triggers apoptosis.{29227} It appears to be more effective against p53-deficient tumors and is able to cross the blood-brain barrier.{29226,29225} GSK461364 is effective in vivo, inducing tumor growth inhibition or growth delay in xenograft models in mice.{29228,29227}
Brand:CaymanSKU:-Available on backorder
Polo-like kinases (Plks) are serine/threonine kinases with key roles in cell cycling.{29228} GSK461364 is a potent, reversible inhibitor of Plk1 (Ki = 2.2 nM).{29227} It is less effective against Plk2 and Plk3 (Kis = 860 and 1,000 nM, respectively) and at least 1,000-fold selective for Plk1 over a panel of 48 other kinases.{29227} GSK461364 dose-dependently halts cell cycling in diverse proliferating cancer cell lines and, at higher doses, triggers apoptosis.{29227} It appears to be more effective against p53-deficient tumors and is able to cross the blood-brain barrier.{29226,29225} GSK461364 is effective in vivo, inducing tumor growth inhibition or growth delay in xenograft models in mice.{29228,29227}
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Polo-like kinases (Plks) are serine/threonine kinases with key roles in cell cycling.{29228} GSK461364 is a potent, reversible inhibitor of Plk1 (Ki = 2.2 nM).{29227} It is less effective against Plk2 and Plk3 (Kis = 860 and 1,000 nM, respectively) and at least 1,000-fold selective for Plk1 over a panel of 48 other kinases.{29227} GSK461364 dose-dependently halts cell cycling in diverse proliferating cancer cell lines and, at higher doses, triggers apoptosis.{29227} It appears to be more effective against p53-deficient tumors and is able to cross the blood-brain barrier.{29226,29225} GSK461364 is effective in vivo, inducing tumor growth inhibition or growth delay in xenograft models in mice.{29228,29227}
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The estrogen-related receptors (ERRs) are orphan nuclear receptors with homology to the estrogen receptor family and are expressed in tissues with high metabolic demand. Binding of peroxisome proliferator-activated receptor γ-coactivator 1α (PGC-1α) to this class of receptors is known to potentiate ERR activity.{12071} GSK4716 is an ERRβ/γ agonist (IC50 = 2 µM) that can activate the receptor with similar potency as the protein ligand, PGC-1α.{28181} It is more than 50-fold selective for binding to ERRβ/γ compared with the estrogen receptors.{28181} This compound has been used to demonstrate the contribution of ERR receptor activity to the regulation of mitochondrial activity in skeletal muscle during exercise.{28182}
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The estrogen-related receptors (ERRs) are orphan nuclear receptors with homology to the estrogen receptor family and are expressed in tissues with high metabolic demand. Binding of peroxisome proliferator-activated receptor γ-coactivator 1α (PGC-1α) to this class of receptors is known to potentiate ERR activity.{12071} GSK4716 is an ERRβ/γ agonist (IC50 = 2 µM) that can activate the receptor with similar potency as the protein ligand, PGC-1α.{28181} It is more than 50-fold selective for binding to ERRβ/γ compared with the estrogen receptors.{28181} This compound has been used to demonstrate the contribution of ERR receptor activity to the regulation of mitochondrial activity in skeletal muscle during exercise.{28182}
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The estrogen-related receptors (ERRs) are orphan nuclear receptors with homology to the estrogen receptor family and are expressed in tissues with high metabolic demand. Binding of peroxisome proliferator-activated receptor γ-coactivator 1α (PGC-1α) to this class of receptors is known to potentiate ERR activity.{12071} GSK4716 is an ERRβ/γ agonist (IC50 = 2 µM) that can activate the receptor with similar potency as the protein ligand, PGC-1α.{28181} It is more than 50-fold selective for binding to ERRβ/γ compared with the estrogen receptors.{28181} This compound has been used to demonstrate the contribution of ERR receptor activity to the regulation of mitochondrial activity in skeletal muscle during exercise.{28182}
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GSK481 is an inhibitor of receptor-interacting serine/threonine protein kinase 1 (RIP1 or RIPK1) that blocks autophosphorylation of Ser166 on wild-type human RIP1 with an IC50 value of 2.8 nM.{33779} It is selective for RIP1 over a panel of over 450 other kinases, including RIP3.{33778,33779} GSK481 inhibits RIP1 from human and cynomolgus monkey but is at least 100-fold less potent against non-primate RIP1.{33779}
Brand:CaymanSKU:20308 -Available on backorder
GSK481 is an inhibitor of receptor-interacting serine/threonine protein kinase 1 (RIP1 or RIPK1) that blocks autophosphorylation of Ser166 on wild-type human RIP1 with an IC50 value of 2.8 nM.{33779} It is selective for RIP1 over a panel of over 450 other kinases, including RIP3.{33778,33779} GSK481 inhibits RIP1 from human and cynomolgus monkey but is at least 100-fold less potent against non-primate RIP1.{33779}
Brand:CaymanSKU:20308 -Available on backorder
GSK481 is an inhibitor of receptor-interacting serine/threonine protein kinase 1 (RIP1 or RIPK1) that blocks autophosphorylation of Ser166 on wild-type human RIP1 with an IC50 value of 2.8 nM.{33779} It is selective for RIP1 over a panel of over 450 other kinases, including RIP3.{33778,33779} GSK481 inhibits RIP1 from human and cynomolgus monkey but is at least 100-fold less potent against non-primate RIP1.{33779}
Brand:CaymanSKU:20308 -Available on backorder
GSK481 is an inhibitor of receptor-interacting serine/threonine protein kinase 1 (RIP1 or RIPK1) that blocks autophosphorylation of Ser166 on wild-type human RIP1 with an IC50 value of 2.8 nM.{33779} It is selective for RIP1 over a panel of over 450 other kinases, including RIP3.{33778,33779} GSK481 inhibits RIP1 from human and cynomolgus monkey but is at least 100-fold less potent against non-primate RIP1.{33779}
Brand:CaymanSKU:20308 -Available on backorder
GSK484 is a reversible inhibitor of PAD4 (IC50 = 50 nM) that binds to the low-calcium form of the enzyme.{28376} It is selective for PAD4 over PAD1-3. GSK484 blocks the citrullination of PAD4 target proteins in human neutrophils and inhibits the formation of neutrophil extracellular traps in both mouse and human neutrophils.{28376} It exhibits favorable pharmacokinetic profiles in mouse and rat. See the Structural Genomics Consortium (SGC) website for more information.
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GSK484 is a reversible inhibitor of PAD4 (IC50 = 50 nM) that binds to the low-calcium form of the enzyme.{28376} It is selective for PAD4 over PAD1-3. GSK484 blocks the citrullination of PAD4 target proteins in human neutrophils and inhibits the formation of neutrophil extracellular traps in both mouse and human neutrophils.{28376} It exhibits favorable pharmacokinetic profiles in mouse and rat. See the Structural Genomics Consortium (SGC) website for more information.
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GSK484 is a reversible inhibitor of PAD4 (IC50 = 50 nM) that binds to the low-calcium form of the enzyme.{28376} It is selective for PAD4 over PAD1-3. GSK484 blocks the citrullination of PAD4 target proteins in human neutrophils and inhibits the formation of neutrophil extracellular traps in both mouse and human neutrophils.{28376} It exhibits favorable pharmacokinetic profiles in mouse and rat. See the Structural Genomics Consortium (SGC) website for more information.
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GSK484 is a reversible inhibitor of PAD4 (IC50 = 50 nM) that binds to the low-calcium form of the enzyme.{28376} It is selective for PAD4 over PAD1-3. GSK484 blocks the citrullination of PAD4 target proteins in human neutrophils and inhibits the formation of neutrophil extracellular traps in both mouse and human neutrophils.{28376} It exhibits favorable pharmacokinetic profiles in mouse and rat. See the Structural Genomics Consortium (SGC) website for more information.
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The lysine methyltransferase EZH2 (KMT6), part of the polycomb repressive complex 2, catalyzes trimethylation of lysine 27 on histone H3 (H3K27me3) and is involved in proliferation and aggressive cell growth associated with neoplastic cells. GSK503 is an inhibitor of EZH2 that prevents the methyltransferase activity of wild-type and mutant EZH2 with similar potency (Kiapp = 3-27 nM).{29988} It is more than 200-fold selective for EZH2 over EZH1 and more than 4,000-fold selective over other histone methyltransferases. GSK503 displays favorable pharmacokinetics in mice. It prevents germinal center formation and hyperplasia that is relevant to lymphoma generation and inhibits growth and metastasis of cutaneous melanomas in mice.{29988,29989}
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The lysine methyltransferase EZH2 (KMT6), part of the polycomb repressive complex 2, catalyzes trimethylation of lysine 27 on histone H3 (H3K27me3) and is involved in proliferation and aggressive cell growth associated with neoplastic cells. GSK503 is an inhibitor of EZH2 that prevents the methyltransferase activity of wild-type and mutant EZH2 with similar potency (Kiapp = 3-27 nM).{29988} It is more than 200-fold selective for EZH2 over EZH1 and more than 4,000-fold selective over other histone methyltransferases. GSK503 displays favorable pharmacokinetics in mice. It prevents germinal center formation and hyperplasia that is relevant to lymphoma generation and inhibits growth and metastasis of cutaneous melanomas in mice.{29988,29989}
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The lysine methyltransferase EZH2 (KMT6), part of the polycomb repressive complex 2, catalyzes trimethylation of lysine 27 on histone H3 (H3K27me3) and is involved in proliferation and aggressive cell growth associated with neoplastic cells. GSK503 is an inhibitor of EZH2 that prevents the methyltransferase activity of wild-type and mutant EZH2 with similar potency (Kiapp = 3-27 nM).{29988} It is more than 200-fold selective for EZH2 over EZH1 and more than 4,000-fold selective over other histone methyltransferases. GSK503 displays favorable pharmacokinetics in mice. It prevents germinal center formation and hyperplasia that is relevant to lymphoma generation and inhibits growth and metastasis of cutaneous melanomas in mice.{29988,29989}
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The lysine methyltransferase EZH2 (KMT6), part of the polycomb repressive complex 2, catalyzes trimethylation of lysine 27 on histone H3 (H3K27me3) and is involved in proliferation and aggressive cell growth associated with neoplastic cells. GSK503 is an inhibitor of EZH2 that prevents the methyltransferase activity of wild-type and mutant EZH2 with similar potency (Kiapp = 3-27 nM).{29988} It is more than 200-fold selective for EZH2 over EZH1 and more than 4,000-fold selective over other histone methyltransferases. GSK503 displays favorable pharmacokinetics in mice. It prevents germinal center formation and hyperplasia that is relevant to lymphoma generation and inhibits growth and metastasis of cutaneous melanomas in mice.{29988,29989}
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GSK583 is a selective inhibitor of RIP-like interacting CLARP kinase (RICK also known as RIP2 kinase; IC50 = 5 nM).{31440} RIP2 Kinase is a central component of the innate immune system and enables downstream signaling following activation of the pattern recognition receptors NOD1 and NOD2, leading to the production of inflammatory cytokines. In an ex vivo human translational model using intestinal mucosal tissue from inflammatory bowel disease patients, GSK583 inhibited both TNF-α and IL-6 production with an IC50 value of 200 nM.{31440}
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GSK583 is a selective inhibitor of RIP-like interacting CLARP kinase (RICK also known as RIP2 kinase; IC50 = 5 nM).{31440} RIP2 Kinase is a central component of the innate immune system and enables downstream signaling following activation of the pattern recognition receptors NOD1 and NOD2, leading to the production of inflammatory cytokines. In an ex vivo human translational model using intestinal mucosal tissue from inflammatory bowel disease patients, GSK583 inhibited both TNF-α and IL-6 production with an IC50 value of 200 nM.{31440}
Brand:CaymanSKU:19739 -Available on backorder
GSK583 is a selective inhibitor of RIP-like interacting CLARP kinase (RICK also known as RIP2 kinase; IC50 = 5 nM).{31440} RIP2 Kinase is a central component of the innate immune system and enables downstream signaling following activation of the pattern recognition receptors NOD1 and NOD2, leading to the production of inflammatory cytokines. In an ex vivo human translational model using intestinal mucosal tissue from inflammatory bowel disease patients, GSK583 inhibited both TNF-α and IL-6 production with an IC50 value of 200 nM.{31440}
Brand:CaymanSKU:19739 -Available on backorder
GSK583 is a selective inhibitor of RIP-like interacting CLARP kinase (RICK also known as RIP2 kinase; IC50 = 5 nM).{31440} RIP2 Kinase is a central component of the innate immune system and enables downstream signaling following activation of the pattern recognition receptors NOD1 and NOD2, leading to the production of inflammatory cytokines. In an ex vivo human translational model using intestinal mucosal tissue from inflammatory bowel disease patients, GSK583 inhibited both TNF-α and IL-6 production with an IC50 value of 200 nM.{31440}
Brand:CaymanSKU:19739 -Available on backorder
GSK591 is a chemical probe for protein arginine methyltransferase 5 (PRMT5) that potently inhibits the PRMT5/MEP50 complex from methylating histone H4 (IC50 = 11 nM) in vitro. GSK591 is selective for PRMT5 (up to 50 µM) relative to a panel of other methyltransferases. In Z-138 cells, GSK591 inhibits the symmetric arginine methylation of SmD3 with an EC50 value of 56 nM. For more information on GSK591 please visit the Structural Genomics Consortium (SGC). The negative control, SGC2096, for GSK591 is also available exclusively through the SGC. You can submit a request to receive the negative control here.
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GSK591 is a chemical probe for protein arginine methyltransferase 5 (PRMT5) that potently inhibits the PRMT5/MEP50 complex from methylating histone H4 (IC50 = 11 nM) in vitro. GSK591 is selective for PRMT5 (up to 50 µM) relative to a panel of other methyltransferases. In Z-138 cells, GSK591 inhibits the symmetric arginine methylation of SmD3 with an EC50 value of 56 nM. For more information on GSK591 please visit the Structural Genomics Consortium (SGC). The negative control, SGC2096, for GSK591 is also available exclusively through the SGC. You can submit a request to receive the negative control here.
Brand:CaymanSKU:-Available on backorder
GSK591 is a chemical probe for protein arginine methyltransferase 5 (PRMT5) that potently inhibits the PRMT5/MEP50 complex from methylating histone H4 (IC50 = 11 nM) in vitro. GSK591 is selective for PRMT5 (up to 50 µM) relative to a panel of other methyltransferases. In Z-138 cells, GSK591 inhibits the symmetric arginine methylation of SmD3 with an EC50 value of 56 nM. For more information on GSK591 please visit the Structural Genomics Consortium (SGC). The negative control, SGC2096, for GSK591 is also available exclusively through the SGC. You can submit a request to receive the negative control here.
Brand:CaymanSKU:-Available on backorder
GSK591 is a chemical probe for protein arginine methyltransferase 5 (PRMT5) that potently inhibits the PRMT5/MEP50 complex from methylating histone H4 (IC50 = 11 nM) in vitro. GSK591 is selective for PRMT5 (up to 50 µM) relative to a panel of other methyltransferases. In Z-138 cells, GSK591 inhibits the symmetric arginine methylation of SmD3 with an EC50 value of 56 nM. For more information on GSK591 please visit the Structural Genomics Consortium (SGC). The negative control, SGC2096, for GSK591 is also available exclusively through the SGC. You can submit a request to receive the negative control here.
Brand:CaymanSKU:-Available on backorder
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 (BR140 or Peregrin) is important for maintaining Hox gene expression and the development of multiple tissues, axial skeleton, and the hematopoietic system.{29177} GSK5959 is a potent, cell-permeable inhibitor of the BRPF1 bromodomain (IC50 = 80 nM).{29176} It exhibits greater than 100-fold selectivity for the BRPF1 bromodomain over a panel of 35 other bromodomains. GSK5959 disrupts chromatin binding of BRPF1 in a cellular assay by blocking the interaction of BRPF1 with histone H3.3.{29176}
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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 (BR140 or Peregrin) is important for maintaining Hox gene expression and the development of multiple tissues, axial skeleton, and the hematopoietic system.{29177} GSK5959 is a potent, cell-permeable inhibitor of the BRPF1 bromodomain (IC50 = 80 nM).{29176} It exhibits greater than 100-fold selectivity for the BRPF1 bromodomain over a panel of 35 other bromodomains. GSK5959 disrupts chromatin binding of BRPF1 in a cellular assay by blocking the interaction of BRPF1 with histone H3.3.{29176}
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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 (BR140 or Peregrin) is important for maintaining Hox gene expression and the development of multiple tissues, axial skeleton, and the hematopoietic system.{29177} GSK5959 is a potent, cell-permeable inhibitor of the BRPF1 bromodomain (IC50 = 80 nM).{29176} It exhibits greater than 100-fold selectivity for the BRPF1 bromodomain over a panel of 35 other bromodomains. GSK5959 disrupts chromatin binding of BRPF1 in a cellular assay by blocking the interaction of BRPF1 with histone H3.3.{29176}
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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 (BR140 or Peregrin) is important for maintaining Hox gene expression and the development of multiple tissues, axial skeleton, and the hematopoietic system.{29177} GSK5959 is a potent, cell-permeable inhibitor of the BRPF1 bromodomain (IC50 = 80 nM).{29176} It exhibits greater than 100-fold selectivity for the BRPF1 bromodomain over a panel of 35 other bromodomains. GSK5959 disrupts chromatin binding of BRPF1 in a cellular assay by blocking the interaction of BRPF1 with histone H3.3.{29176}
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GSK621 is an activator of AMP-activated protein kinase (AMPK). It has been shown to increase phosphorylation at AMPKα T172, a marker of AMPK activation, in both acute myeloid leukemia (AML) cell lines and primary AML samples.{31816} GSK621 is reported to reduce the proliferation of AML cell lines (IC50s = 13-30 μM), triggering autophagy via the eIF2α/ATF4 signaling pathway.{31816}
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GSK621 is an activator of AMP-activated protein kinase (AMPK). It has been shown to increase phosphorylation at AMPKα T172, a marker of AMPK activation, in both acute myeloid leukemia (AML) cell lines and primary AML samples.{31816} GSK621 is reported to reduce the proliferation of AML cell lines (IC50s = 13-30 μM), triggering autophagy via the eIF2α/ATF4 signaling pathway.{31816}
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GSK621 is an activator of AMP-activated protein kinase (AMPK). It has been shown to increase phosphorylation at AMPKα T172, a marker of AMPK activation, in both acute myeloid leukemia (AML) cell lines and primary AML samples.{31816} GSK621 is reported to reduce the proliferation of AML cell lines (IC50s = 13-30 μM), triggering autophagy via the eIF2α/ATF4 signaling pathway.{31816}
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GSK621 is an activator of AMP-activated protein kinase (AMPK). It has been shown to increase phosphorylation at AMPKα T172, a marker of AMPK activation, in both acute myeloid leukemia (AML) cell lines and primary AML samples.{31816} GSK621 is reported to reduce the proliferation of AML cell lines (IC50s = 13-30 μM), triggering autophagy via the eIF2α/ATF4 signaling pathway.{31816}
Brand:CaymanSKU:-Available on backorder