Glycogen synthase kinase 3 (GSK-3) is a multifunctional serine/threonine kinase found in all eukaryotes. GSK-3 is one of the few signaling mediators that play central roles in a diverse range of signaling pathways, including those activated by Wnts, hedgehog, growth factors, cytokines, and G protein-coupled ligands. GSK-3 targets transcription factors, regulates the activity of metabolic and signaling enzymes, and controls the half-life of proteins by earmarking them for degradation. GSK-3 exists as two isoforms, GSK-3a (51 kDa) and GSK3b (47 kDa), which are encoded by distinct genes. These isoforms often have overlapping functions, but they do not always compensate for each other.
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SB 216763 is a potent, selective, ATP competitive and cell permeable inhibitor GSK-3 with Ki of 9 nM (GSK-3α), equally potent for GSK-3β; displays no significant activity against a panel of 24 other protein kinases; stimulates glycogen synthesis in human liver cells and induces expression of a beta-catenin-LEF/TCF regulated reporter gene in HEK293 cells, protects both central and peripheral nervous system neurones in culture from death, activates beta-catenin-mediated transcription, and enhances the survival of CLL lymphocytes; displays therapeutic properties in a mouse model of pulmonary inflammation and fibrosis.
A potent, specific GSK-3 inhibitor with IC50 of 5 nM and 10 nM for GSK3β and GSK3α, respectively; mimics Wnt signaling in preadipocytes, stabilizes free cytosolic beta-catenin and inhibits adipogenesis by blocking induction of C/EBPα and PPARγ; potentiates insulin activation of glucose transport and utilization in vitro and in vivo; also widely used for stem cell differentiation and naive stem cell generation.
A potent GSK3β inhibitor with IC50 of 22 nM; prevents tau phosphorylation both in vitro and in vivo; also inhibits CDKs at higher concentrations, including Cdk1/cyclin B (IC50=180 nM), Cdk2/cyclin A (IC50~500 nM), Cdk2/cyclin E (IC50=250nM), Cdk4/cyclin D1 (IC50=3.3 uM) and Cdk5/p35 (IC50=100 nM); reversibly inhibits the proliferation of many cells types, arresting cycling in the G2/M phase.
A high-affinity, selective GSK3β inhibitor that activates canonical Wnt signaling; promotes rapid and efficient differentiation of human pluripotent stem cells (hPSCs) into vascular endothelial and smooth muscle cells.
A GSK-3β inhibitor with IC50 of 30 nM in a cell-free assay; can induce neurogenesis in murine ESCs; reduces Cdon levels and aberrant Cx43 activitiesin rat cardiomyocytes; attenuates rtPA-induced hemorrhagic transformation and activates the Wnt/β-catenin signaling pathway after acute ischemic stroke in rats.
Bikinin (Abrasin) is a plant GSK-3/Shaggy-like kinases inhibitor that activates brassinosteroid (BR) signaling downstream of the BR receptor, binds and inhibits Arabidopsis thaliana GSK3-like kinases; interferes directly with BIN2 kinase activity, also strongly inhibited the activity of the group I Arabidopsis GSK3 subfamilies, but not the ASKβ, ASKδ, and other Arabidopsis Ser/Thr kinases (AtMPK4, AtMPK6, and AtAURORA1); inhibits the SnRK2.3 kinase activity and its T180 phosphorylation in vivo.
GSK 3 Inhibitor IX
A cell-permeable derivative of 6-bromoindirubin that displays selective inhibition of GSK-3 with IC50 of 5 nM; also inhibit CDK1/Cyclin B and CDK5/p25 (IC50, 320 nM and 83 nM); maintains the undifferentiated phenotype in HESCs and MESCs, sustains the expression of Oct-3/4, Rex-1 and Nanog; promotes proliferation in mammalian cardiomyocytes.
CHIR-98014 is a potent, selective glycogen synthase kinase 3 (GSK-3) withIC50 of 0.65 and 0.58 nM for GSK-3α and GSK-3β, respectively; shows less potent activities against 20 other protein kinases including Cdc2 and Erk2; causes GS stimulation in CHO-IR cells and rat hepatocytes, with EC50s of 106 nM and 107 nM, respectively; reduces the viability of ES-CCE cells with IC50 of 1.1 uM, results in a significant activation of the Wnt/beta-catenin pathway in ES-D3 cells combined with CHIR-99021; significantly reduces fasting hyperglycemia within and shows improved glucose disposal in diabetic and insulin-resistant db/db mice.
AR-A014418 is a potent, specific ATP-competitive inhibitor of GSK-3β with Ki/IC50 of 38/104 nM; shows no significantly inhibition on CDK2, CDK5 (IC50>100 uM) or 26 other kinases; inhibits tau phosphorylation at a GSK3-specific site (Ser-396) in cells and protects N2A neuroblastoma cells against cell death mediated by inhibition of PI3K/Akt pathway.
IM-12 is a novel potent GSK-3β inhibitor with IC50 of 53 nM, significantly increases the β-catenin level and activates canonical Wnt signalling; attenuates cell proliferation of ReNcell VM cells, induces nuclear accumulation of beta-catenin.
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