SB216763

SB216763 is a potent and selective small molecule inhibitor of glycogen synthase kinase 3 (GSK-3), acting on both GSK-3α and GSK-3β isoforms with an IC₅₀ of approximately 34 nM. It is cell-permeable and functions as an ATP-competitive inhibitor at the kinase's ATP-binding domain. By inhibiting GSK-3 activity, SB216763 modulates key cellular processes including cell death, cell cycle regulation, carcinogenesis, autophagy, and signal transduction pathways such as Wnt/β-catenin signaling. Preclinical studies have shown that SB216763 can protect neurons from apoptosis in models of central and peripheral nervous system injury; it enhances remyelination after nerve damage by promoting myelin gene expression. The compound has also demonstrated anti-inflammatory effects in animal models of lung fibrosis by reducing cytokine production from macrophages. Additionally, it maintains pluripotency in mouse embryonic stem cells without exogenous leukemia inhibitory factor.

Other names

3-(2,4-dichlorophenyl)-4-(1-methylindol-3-yl)pyrrole-2,5-dioneGSK-3 Inhibitor IVGSK3 Inhibitor IVGSK 3 Inhibitor IV