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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.

Cat. No. Product Name CAS No. Information

SB 216763


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.


CHIR-99021 trihydrochloride


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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