361566

GSK-3 Inhibitor IV, SB-216763

• Sinónimos: GSK-3 Inhibitor IV, SB-216763, SB-216763
• Fórmula empírica (notación de Hill): C₁₉H₁₂Cl₂N₂O₂
• Número de CAS: 280744-09-4
• Peso molecular: 371.22
• Número MDL: MFCD09753369
• Código UNSPSC: 12352200
• NACRES: NA.77

Propiedades

• Análisis: ≥98% (HPLC)
• Nivel de calidad: 100
• formulario: solid
• fabricante / nombre comercial: Calbiochem^®
• condiciones de almacenamiento: OK to freeze
• color: orange
• solubilidad: DMSO: 50 mg/mL
• Condiciones de envío: ambient
• temp. de almacenamiento: 2-8°C
• InChI: 1S/C19H12Cl2N2O2/c1-23-9-13(11-4-2-3-5-15(11)23)17-16(18(24)22-19(17)25)12-7-6-10(20)8-14(12)21/h2-9H,1H3,(H,22,24,25)
• Clave InChI: JCSGFHVFHSKIJH-UHFFFAOYSA-N

Descripción

Descripción general

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.

Advertencia

Toxicity: Irritant (B)

Reconstitución

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

Otras notas

Gross, E., et al. 2008. Am. J. Phy. Heart Circ Physiol.294, H1497.
Bain, J., et al. 2007. Biochem. J.408, 297.
Lu, D., et al. 2004. PNAS.101, 3118.
Carmichael, J., et al. 2002. J. Biol. Chem.277, 33791.
Culbert, A.A., et al. 2001. FEBS Lett.507, 288.
Lochhead, P.A., et al. 2001. Diabetes50, 937.
Cross, D.A., et al. 2001. J. Neurochem.77, 94.
Coghlan, M.P., et al. 2000. Chem. Biol.7, 793.

Información legal

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Información de seguridad

• Código de clase de almacenamiento: 11 - Combustible Solids
• Clase de riesgo para el agua (WGK): WGK 3
• Punto de inflamabilidad (°F): Not applicable
• Punto de inflamabilidad (°C): Not applicable