BX-795

BX-795CAS号: 702675-74-9分子式: C23H26IN7O2S分子量: 591.47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)

产品描述
描述

BX795 is a potent and selective dual inhibitor of TBK1/PDK1 with IC50s of 2 nM/6 nM respectively; > 50 fold selectivity over PKA, PKC, c-Kit, GSK3β etc.

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
BX 795; BX-795
外观
white to light brown powder
可溶性/溶解性
Ethanol :59.2 mg/mL (100 mM)
DMSO :59.2 mg/mL (100 mM)
生物活性
靶点
PDK-1
In vitro(体外研究)
BX795 effectively blocks PDK1 activity in PC-3 cells, as shown by their ability to block phosphorylation of S6K1, Akt, PKCδ, and GSK3β. BX795 potently inhibits tumor cell growth on plastic with IC50 of 1.6, 1.4, and 1.9 μM for MDA-468, HCT-116 and MiaPaca cells, respectively. In soft agar, BX795 displays higher growth inhibition with IC50 of 0.72, and 0.25 μM for MDA-468, and PC-3 cells, respectively. In addition, BX795, as an inhibitor of the TBK1/IKKε, blocks TBK1- and IKKε-mediated activation of IRF3 and production of IFN-β. In platelet physiological responses, BX795 produces inhibitory effect on 2-MeSADP-induced or collagen-induced aggregation, ATP secretion and thromboxane generation. 

分子结构图

BX-795