Go6976

Go6976CAS号: 136194-77-9分子式: C24H18N4O分子量: 378.43描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)

产品描述
描述

Go6976是一种强效的PKC抑制剂,其对PKC (老鼠大脑), PKCα, and PKCβ1的IC50分别为7.9nM,2.3 nM, 和 6.2 nM 。此外,也是JAK2 和 Flt3的强抑制剂。

纯度
>98%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
别名
PD406976
外观
Off-white solid
可溶性/溶解性
DMSO :18 mg/mL warmed (47.69 mM)
生物活性
靶点
JAK2;FLT3;PKCα;PKCβ1;PKC
In vitro(体外研究)
Go6976 have no effect on the kinase activity of the Ca(2+)-independent PKC subtypes delta, epsilon, and zeta. Beside WT JAK2, Go6976 also inhibits the mutant forms (JAK2 V617F and TEL-JAK2) found in haematological malignancies, and has activity against mutant forms of FLT3. In AML cells, Go6976 reduces the survival to 55% of control in FLT3-ITD cases and to 69% in FLT3-WT samples. Go 6976 potently inhibits HIV-1 induction by Bryostatin 1, tumor necrosis factor alpha, and interleukin 6.
In vivo(体内研究)
Go6976 (2.5 mg/kg i.p.), as a PKD inhibitor, effectively prevents LPS/D: -GalN-induced acute liver injury by inhibition of MAPKs activation to reduce TNF-α production, and significantly improves the survival of LPS/D-GalN-challenged mice.

分子结构图

Go6976