5.04276

PKC Activator VII, CGK062

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

Propriedades

• Ensaio: ≥98% (HPLC)
• Nível de qualidade: 100
• forma: solid
• potência: 12.2 μM IC₅₀
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: off-white
• solubilidade: DMSO: 100 mg/mL
• temperatura de armazenamento: −20°C

Descrição

Descrição geral

A cell permeable coumarin-containing compound that is shown to activate PKCα activity and induce cellular PKCα membrane translocation (Effective conc. 12.5 to 50 µM) as well as PKCα-mediated signaling events. Effectively affects the viability of CRT-dependent cancer cells (IC₅₀ = 1.62 to 18.6 µM; 48 h) in vitro and suppresses PC3-derived tumor expansion in mice (50 & 100 mg/kg/day; i.p) in vivo, while exhibiting little cytotoxicity toward WI38 normal fibroblasts.

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).

Ações bioquímicas/fisiológicas

Reversible: yes

Embalagem

Packaged under inert gas

Advertência

Toxicity: Standard Handling (A)

Outras notas

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

Informações legais

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

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 3
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable