About 11 results found for searched term "GSK-J1" (0.119 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M2730 | GSK-J1 | Histone demethylase |
| GSK-J1 is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with IC50 of 60 nM towards KDM6B. GSK J1 is selective for the H3K27 demethylases JMJD3 and UTX. | ||
| M1759 | GSK1120212 (Trametinib) | MEK |
| JTP-74057, GSK212 | ||
| Trametinib (GSK1120212; Jtp-74057) is an orally effective MEK inhibitor with IC50 of 2 nM against MEK1 and MEK2, respectively. Trametinib can activate autophagy and induce apoptosis. | ||
| M2731 | GSK-J4 hydrochloride | Histone demethylase |
| GSK-J4 hydrochloride is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively. GSK-J4 hydrochloride inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK J4 hydrochloride is a cell permeable procompound of GSK J1, which is the first selective inhibitor of the H3K27 histone demethylase JMJD3 and UTX with IC50 of 60 nM and inactive against a panel of demethylases of the JMJ family. | ||
| M5149 | GSK-J4 | Histone demethylase |
| GSK-J4 is a cell permeable procompound rapidly hydrolyzed by macrophage esterases to GSK-J1, a potent selective jumonji H3K27 demethylase inhibitor. | ||
| M10879 | RGB-286638 | CDK |
| RGB-286638 is a potent CDK inhibitor that inhibits cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 activity,IC50 1, 2, 3, 4, 5 and 5 nM, respectively, and can inhibit GSK-3β, TAK1, Jak2 and MEK1.IC50 The values are 3, 5, 50, and 54 nM, respectively. | ||
| M13611 | RGB-286638 free base | CDK |
| RGB-286638 is a CDK inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM. | ||
| M13832 | GSK467 | Histone demethylase |
| GSK467 is a cell penetrant and selective KDM5B (JARID1B or PLU1) inhibitor with a Ki of 10 nM, shows 180-fold selectivity for KDM4C and no measurable inhibitory effects toward KDM6 or other Jumonji family members. | ||
| M14172 | Trametinib (DMSO solvate) | MEK |
| GSK-1120212 (DMSO solvate); JTP-74057 (DMSO solvate) | ||
| Trametinib (DMSO solvate) (GSK-1120212 (DMSO solvate);JTP-74057 (DMSO solvate)) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. | ||
| M14713 | GSK-J2 | Others |
| GSK-J2 is an isomer of GSK-J1 that does not have any specific activity. GSK-J1 is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A. | ||
| M20836 | Indirubin-3′-oxime | GSK-3 |
| IDR3O, I3O | ||
| Indirubin-3′-oxime (IDR3O, I3O) is an indirubin analogue that shows favorable inhibitory activity targeting GSK-3β and CDKs. Indirubin-3′-oxime also inhibits JNKs with IC50s of 0.8 μM, 1.4 μM, and 1.0 μM for JNK1, JNK2, and JNK3, respectively. Indirubin-3′-oxime activates Wnt/β-catenin signaling and inhibits adipocyte differentiation and obesity. | ||
| M31419 | JNJ-28583113 | TRP Channel |
| JNJ-28583113 is a brain-permeable TRPM2 antagonist and blocks phosphorylation of GSK3α and β subunits by inhibiting TRPM2. In addition, JNJ-28583113 inhibits cytokine release from microglia in response to pro-inflammatory stimuli. It has the function of protecting cells from oxidative stress-induced cell death. | ||
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