PKC Activator VII, CGK062-Calbiochem

半岛bd体育手机客户端 说明

一般描述

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 ?M) as well as PKCα-mediated signaling events. Effectively affects the viability of CRT-dependent cancer cells (IC₅₀= 1.62 to 18.6 ?M; 48 h)in vitroand 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 ?M) and induce cellular PKCα membrane translocation (Effective conc. 12.5 to 50 ?M 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 ?M, respectively, in SW480, HCT15, PC3, SNU475, and DLD-1 cultures; 48 h)in vitroand 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 ?M; 48 h).

生化/生理作用

Reversible: yes

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

其他说明

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

法律信息

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

基本信息

经验(实验)分子式	C23H20O7
分子量	408.40

半岛bd体育手机客户端 性质

质量水平	100
测定	≥98% (HPLC)
形式	solid
效能	12.2 μM IC50
manufacturer/tradename	Calbiochem?
储存条件	OK to freeze protect from light
颜色	off-white
溶解性	DMSO: 100 mg/mL
储存温度	?20℃

安全信息

储存分类代码	11 - Combustible Solids
WGK	WGK 3
闪点(F)	Not applicable
闪点(C)	Not applicable