Cat. No. 1616
Chemical Name: 3-(2,4-Dichlorophenyl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
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.
If you know of a relevant citation for this product please let us know.
View Related Products by Target
Keywords: SB 216763, supplier, Potent, selective, GSK-3, inhibitors, Glycogen, Synthase, Kinases, 3, Carbohydrate, Metabolism, SB216763, GlaxoSmithKline, GSK
Find multiple products by catalog number
New Products in this Area
Potent protein kinase D (PKD) inhibitorHarmine
Potent and selective Dyrk1A inhibitorAZ 628
Potent Raf kinase inhibitorCHIR 99021 trihydrochloride
Hydrochloride salt of CHIR 99021 (Cat. No. 4423); selective GSK-3 inhibitorYZ9
PFKFB3 inhibitor; inhibits cell growthKU 0060648
Dual DNA-PK and PI 3-K inhibitorKB SRC 4
Potent and selective c-Src inhibitorProINDY
Dyrk1A/B inhibitor; prodrug of INDY (Cat. No. 4997)INDY
Dyrk1A/B inhibitorAZD 6482
Potent and selective PI 3-Kβ inhibitorAS 1892802
Potent ROCK inhibitor; orally bioavailableSC 79
Akt activatorSNS 314 mesylate
Potent pan-Aurora kinase inhibitorPD 180970
p210bcr/abl kinase inhibitor; also inhibits c-Src and KITPD 334581
MEK1 inhibitorSB 747651A dihydrochloride
Potent MSK1 inhibitor; also inhibits other AGC group kinases
Win a Kindle
December 16, 2013