Cat. No. 1616
Chemical Name: 3-(2,4-Dichlorophenyl)-4-(1-methyl-
Biological ActivityPotent and selective, ATP-competitive glycogen synthase kinase-3 (GSK-3) inhibitor (IC50 = 34.3 nM for GSK-3α). Equally effective at inhibiting human GSK-3α and GSK-3β. Exhibits minimal activity against 24 other protein kinases (IC50 >10 μM). Stimulates glycogen synthesis in liver cells, and induces β-catenin-dependent gene transcription. Neuroprotective; also reduces pulmonary inflammation and fibrosis in a mouse model. Shown to maintain mouse embryonic stem cells in a pluripotent state.
Licensing InformationSold for research purposes under agreement from GlaxoSmithKline
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Certificate of Analysis / Safety Data Sheet
Coghlan et al (2000) Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription. Chem.Biol. 7 793. PMID: 11033082.
Cross et al (2001) Selective small-molecule inhibitors of glycogen synthase kinase-3 activity protect primary neurones from death. J.Neurochem. 77 94. PMID: 11279265.
Liang and Chuang (2006) Regulation and function of glycogen synthase kinase-3 isoforms in neuronal survival. J.Biol.Chem. 282 3904. PMID: 17148450.
Gurrieri et al (2010) 3-(2,4-dichlorophenyl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione (SB216763), a glycogen synthase kinase-3 inhibitor, displays therapeutic properties in a mouse model of pulmonary inflammation and fibrosis. J.Pharmacol.Exp.Ther. 332 785. PMID: 19959748.
Kirby et al (2012) Glycogen synthase kinase 3 (GSK3) inhibitor, SB-216763, promotes pluripotency in mouse embryonic stem cells. PLoS One 7 e39329. PMID: 22745733.
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Keywords: SB 216763, supplier, Potent, selective, GSK-3, inhibitors, Glycogen, Synthase, Kinases, 3, Carbohydrate, Metabolism, SB216763, GlaxoSmithKline, GSK
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December 16 - 18, 2014
Booth Number: 12