SB 216763

Name SB 216763
Supplier Tocris Bioscience
Catalog 1242
Prices $85.00, $175.00, $709.00
Sizes 1 mg, 10 mg, 50 mg
Function Type Inhibitor
Cas Number 280744-09-4
Chemical Name 3-(2,4-Dichlorophenyl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
Formula C19H12Cl2N2O2
Molecular Weight 371.22
Purity >98 %
Description Potent and selective, ATP-competitive glycogen synthase kinase-3 (GSK-3) inhibitor (IC 50 = 34.3 nM for GSK-3 α ). Equally effective at inhibiting human GSK-3 α and GSK-3 β . Exhibits minimal activity against 24 other protein kinases (IC 50 >10 μ M). 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.
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Product References

Selective small molecule inhibitors of glycogen synthase kinase-3 modulate - Selective small molecule inhibitors of glycogen synthase kinase-3 modulate

Coghlan MP, Culbert AA, Cross DA, Corcoran SL, Yates JW, Pearce NJ, Rausch OL, Murphy GJ, Carter PS, Roxbee Cox L, Mills D, Brown MJ, Haigh D, Ward RW, Smith DG, Murray KJ, Reith AD, Holder JC. Chem Biol. 2000 Oct;7(10):793-803.

Selective small-molecule inhibitors of glycogen synthase kinase-3 activity - Selective small-molecule inhibitors of glycogen synthase kinase-3 activity

Cross DA, Culbert AA, Chalmers KA, Facci L, Skaper SD, Reith AD. J Neurochem. 2001 Apr;77(1):94-102.

Regulation and function of glycogen synthase kinase-3 isoforms in neuronal - Regulation and function of glycogen synthase kinase-3 isoforms in neuronal

Liang MH, Chuang DM. J Biol Chem. 2007 Feb 9;282(6):3904-17. Epub 2006 Dec 5.

3-(2,4-dichlorophenyl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione - 3-(2,4-dichlorophenyl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione

Gurrieri C, Piazza F, Gnoato M, Montini B, Biasutto L, Gattazzo C, Brunetta E, Cabrelle A, Cinetto F, Niero R, Facco M, Garbisa S, Calabrese F, Semenzato G, Agostini C. J Pharmacol Exp Ther. 2010 Mar;332(3):785-94.

Glycogen synthase kinase 3 (GSK3) inhibitor, SB-216763, promotes pluripotency in - Glycogen synthase kinase 3 (GSK3) inhibitor, SB-216763, promotes pluripotency in

Kirby LA, Schott JT, Noble BL, Mendez DC, Caseley PS, Peterson SC, Routledge TJ, Patel NV. PLoS One. 2012;7(6):e39329.