GSK-3 Inhibitor IV, SB-216763 – CAS 280744-09-4 – Calbiochem

Descrição detalhada : A cell-permeable (aryl,indole) maleimide compound that acts as a potent, selective, ATP-competitive inhibitor of GSK-3 activity (Ki = 9.1 nM for GSK-3alpha). 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 beta-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/beta-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.
Sinónimos : GSK-3 Inhibitor IV, SB-216763 - CAS 280744-09-4 - Calbiochem; SB-216763
Fórmula molecula r: C19H12Cl2N2O2
Armazenamento : 2-8C; 2-8C
Embalagem : 1X10MG