Description

• A cell-permeable (aryl,indole) maleimide compound that acts as a potent, selective, ATP-competitive inhibitor of GSK-3 activity (K i = 9.1nM for GSK-3α)
• At 10μM concentration, does not significantly inhibit a panel of 24 other protein kinases tested
• Reported to stimulate glycogen synthesis in Chang human liver cells (EC 50 = 3.6μM) and induce transcription of β-catenin-LEF/TCF (lymphoid enhancer factor/T cell factor) regulated reporter gene in HEK293 human embryonic kidney cell lines
• Offers protection against polyglutamine-induced death in SK-N-SH and COS-7 cells and attenuates hypoxia-induced apoptosis in VSMC and COS-7 cells
• Shown to reduce phosphoenolpyruvate carboxykinase (PEPCK) and glucose-6-phosphatase (G6Pase) expression in hepatoma cells
• Promotes the survival of CLL lymphocytes via Wnt/β-catenin-mediated transcription activation
• Exhibits delayed cardioprotection in vivo in a rat model via a KATP (ATP-sensitive potassium channels) and MPTP (mitochondrial permeability transition pore)-dependent mechanism at reperfusion.