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SB-216763 is a Potent and selective inhibitor of glycogen synthase kinase-3 (GSK-3) with IC50 of 34.3 nM. It competes with ATP and potently inhibits the activity against both GSK-3α and GSK-3β.

GSK-3, one of several known substrates of PKB, is a serine/threonine protein kinase that mediates the addition of phosphate molecules onto serine and threonine amino acid residues.

SB-216763 treatment can protect neurones of both central and peripheral nervous system from cell death which is mediated by PI3K pathway ex vivo [1]. This component was also shown to maintain the pluripotency of mouse embryonic stem cells (mESCs) without exogenous leukemia inhibitory factor (LIF) when cultured on mouse embryonic fibroblasts (MEFs) [2].

The component has also been used extensively in various animal models to study the role of GSK-3. In a bleomycin-induced mice lung fibrosis model, SB-216763 administration protected mice from lung inflammation and the subsequent fibrosis, which was associated with decreased production of inflammatory cytokine by macrophages [3]. Besides, treatment of SB-216763 reduced infarct size and prevented cardiac ischemia in a model of regional myocardial ischemia-reperfusion in rats [4].

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