GSK-3 Inhibitor IV, SB-216763

A cell-permeable (aryl,indole) maleimide compound that acts as a potent, selective, ATP-competitive inhibitor of GSK-3 activity (K_i = 9.1 nM for GSK-3α). At 10 µM concentration, does not significantly inhibit a panel of 24 other protein kinases tested. Reported to stimulate glycogen synthesis in Chang human liver cells (EC₅₀ = 3.6 µM) 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.

A cell-permeable (aryl,indole) maleimide compound that acts as a potent, selective, ATP-competitive inhibitor of GSK-3 activity (K_i = 9.1 nM for GSK-3α). At 10 µM concentration, does not significantly inhibit a panel of 24 other protein kinases tested. Reported to stimulate glycogen synthesis in Chang human liver cells (EC₅₀ = 3.6 µM) 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.

Toxicity: Irritant (B)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

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