5.04276

PKC Activator VII, CGK062

• Synonyme(s) : PKC Activator VII, CGK062, Protein Kinase C Activator VII
• Formule empirique (notation de Hill): C₂₃H₂₀O₇
• Numéro CAS: 1001129-59-4
• Poids moléculaire : 408.40
• Code UNSPSC : 12352200

Propriétés

• Pureté: ≥98% (HPLC)
• Niveau de qualité: 100
• Forme: solid
• Puissance: 12.2 μM IC₅₀
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: off-white
• Solubilité: DMSO: 100 mg/mL
• Température de stockage: −20°C

Description

Description générale

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).

Actions biochimiques/physiologiques

Reversible: yes

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Autres remarques

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

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable