R&D Systems Inc. Tocris Bioscience Boston Biochem

SB 216763

Cat. No. 1616

SB 216763 C19H12Cl2N2O2 [280744-09-4]

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Chemical Name: 3-(2,4-Dichlorophenyl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione

Biological Activity

Potent 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 Information

Sold for research purposes under agreement from GlaxoSmithKline

Technical Data

M.Wt:
371.22
Formula:
C19H12Cl2N2O2
Solubility:
Soluble to 75 mM in DMSO
Purity:
>98 %
Storage:
Store at RT
CAS No:
280744-09-4

The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.

Resources

Other Information

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch
Select another batch:
Safety Data Sheet: View Safety Data Sheet

References

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.

If you know of a relevant citation for this product please let us know.

Keywords: SB 216763, supplier, Potent, selective, GSK-3, inhibitors, Glycogen, Synthase, Kinases, 3, Carbohydrate, Metabolism, SB216763, GlaxoSmithKline, GSK

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