5.04276

PKC Activator VII, CGK062

• Sinónimos: PKC Activator VII, CGK062, Protein Kinase C Activator VII
• Fórmula empírica (notación de Hill): C₂₃H₂₀O₇
• Número de CAS: 1001129-59-4
• Peso molecular: 408.40
• Código UNSPSC: 12352200

Propiedades

• Ensayo: ≥98% (HPLC)
• Nivel de calidad: 100
• Formulario: solid
• potencia: 12.2 μM IC₅₀
• fabricante / nombre comercial: Calbiochem^®
• condiciones de almacenamiento: OK to freeze; protect from light
• color: off-white
• solubilidad: DMSO: 100 mg/mL
• temp. de almacenamiento: −20°C

Descripción

Descripción general

A cell permeable coumarin-containing compound that is shown to activate PKCα activity toward GST-β-catenin or PKC substrate peptide in cell-free kinase assays (12.5 & 25 µM) and induce cellular PKCα membrane translocation (Effective conc. 12.5 to 50 µM in HEK293, PC3, SNU475, and SW480 cultures) as well as PKCα-mediated β-catenin phosphorylation (Ser33/37/45) and subsequent β-catenin degradation in a F-box Ub ligase complex component β-TrCP- (β-transducin repeat-containing protein) dependent, but GSK-3β-independent, manner. Effectively affects the viability of CRT- (β-catenin response transcription) dependent cancer cells (IC₅₀ = 1.62, 5.71, 9.40, 11.41, and 18.60 µM, respectively, in SW480, HCT15, PC3, SNU475, and DLD-1 cultures; 48 h) in vitro and suppresses PC3-derived tumor expansion in mice (23% and 11% of control size, respectively, with 50 or 100 mg/kg daily i.p. dose for 4 wks) in vivo, while exhibiting little cytotoxicity toward WI38 normal fibroblasts (IC₅₀ = 74.83 µM; 48 h).

Acciones bioquímicas o fisiológicas

Reversible: yes

Envase

Packaged under inert gas

Advertencia

Toxicity: Standard Handling (A)

Otras notas

Gwak, J., et al. 2012. PLoS One.7, e46697.

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