SB-216763 is a potent and selective inhibitor of glycogen synthase kinase-1 (GSK-3) IC50=34.3 nM (1). It acts at the ATP-binding domain, showing protective effects in lung fibrosis mouse model (2). SB-216763 also displays neuroprotective effects on cultured neurons (3). Lastly, it had been able to maintain mouse embryonic stem cells in a pluripotent state (4).
1) Coghlan et al. (2000), Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription; Chem. Biol., 7 793
2) 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
3) Cross et al. (2001), Selective small-molecule inhibitors of glycogen synthase kinase-3 activity protect primary neurones from death; J. Neurochem., 77 94
4) Kirby et al. (2012), Glycogen synthase kinase 3 (GSK3) inhibitor, SB-216763, promotes pluripotency in mouse embryonic stem cells; PLoS One, 7 e39329
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