SB216763

SB-216763 (280744-09-4) is a potent and selective inhibitor of glycogen synthase kinase-1 (GSK-3) IC50=34.3 nM.1 Acts at the ATP-binding domain. Displays protective effects in lung fibrosis mouse model.2 Displays neuroprotective effects on cultured neurons.3 SB-216763 maintains mouse embryonic stem cells in a pluripotent state.4?Cell permeable.

SB 216763 is a potent and selective cell permeale ATP-competitive inhibitor of GSK3a. It stimulates glycogen synthesis in Chang human liver cells.

SB-216763 was used to inhibit GSK-3β in human brain microvascular endothelial cell line and colorectal cancer cells.

ChEBI: 3-(2,4-dichlorophenyl)-4-(1-methyl-3-indolyl)pyrrole-2,5-dione is a member of indoles and a member of maleimides.

Potent and selective glycogen synthase kinase-3 (GSK-3) inhibitor (K i = 9 nM for GSK-3 α ); competes with ATP. Has minimal activity against 24 other protein kinases (IC 50 > 10 μ M). Stimulates glycogen synthesis, gene transcription and is neuroprotective.

SB-216763 is a small molecule that competes with ATP and potently inhibits the activity α and β isozymes of GSK-3. It acts as neuroprotectant and prevents neuronal cell death induced by PI3-kinase pathway. It also delays preconditioning, reduces infarct size and prevents cardiac ischemia.

Room temperature

[1] M P COGHLAN. Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription.[J]. Chemistry & biology, 2000, 7 10: 793-803. DOI:10.1016/s1074-5521(00)00025-9
[2] CARMELA GURRIERI. 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]. Journal of Pharmacology and Experimental Therapeutics, 2010, 332 3: 785-794. DOI:10.1124/jpet.109.153049
[3] D. CROSS. Selective small-molecule inhibitors of glycogen synthase kinase-3 activity protect primary neurones from death.[J]. Journal of Neurochemistry, 2001, 77 1: 94-102. DOI:10.1046/j.1471-4159.2001.t01-1-00251.x
[4] LESLIE A KIRBY. Glycogen synthase kinase 3 (GSK3) inhibitor, SB-216763, promotes pluripotency in mouse embryonic stem cells.[J]. PLoS ONE, 2012: e39329. DOI:10.1371/journal.pone.0039329