SB 216763 is a potent, selective, ATP competitive and cell permeable inhibitor GSK-3 with Ki of 9 nM (GSK-3α), equally potent for GSK-3β.
SB 216763 displays no significant activity against a panel of 24 other protein kinases.
SB 216763 stimulates glycogen synthesis in human liver cells and induces expression of a beta-catenin-LEF/TCF regulated reporter gene in HEK293 cells, protects both central and peripheral nervous system neurones in culture from death, activates beta-catenin-mediated transcription, and enhances the survival of CLL lymphocytes.
SB 216763 displays therapeutic properties in a mouse model of pulmonary inflammation and fibrosis.
