MilliporeSigma™ Calbiochem™ GSK-3 Inhibitor IV, SB-216763

Description

A cell-permeable (aryl,indole) maleimide compound that acts as a potent, selective, ATP-competitive inhibitor of GSK-3 activity (K_i

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 (EC₅₀ = 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.

Specifications

• Color: Orange
• Description: 98% by HPLC
• CAS: 280744-09-4
• Molecular Formula: C₁₉H₁₂Cl₂N₂O₂
• Formula Weight: 371.2g/mol
• Solubility: DMSO
• Form: Solid
• Quantity: 10 mg