您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > Bax channel blocker
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Bax channel blocker
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Bax channel blocker图片
CAS NO:335165-68-9
规格:98%
分子量:540.12
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
Inhibitor of Bax-mediated mitochondrial cytochrome c release
CAS:335165-68-9
分子式:C19H21Br2N3O.2HCl
分子量:540.12
纯度:98%
存储:Store at -20°C

Background:

IC50: 0.52 μM in Bax assay


Bax channel blocker is an inhibitor of Bax-mediated mitochondrial cytochrome c release.


In the cytosol, cytochrome c is found to form a complex with dATP, Apaf-1, and procaspase-9, which results in caspase 9 activation followed by downstream activation of other caspases, such as caspase 8, ultimately leading to the cell death. After caspase 8 cleavage, the 15.5 kDa C-terminal fragment of Bid interacts with Bak and Bax.


In vitro: Bax channel blocker, a 3,6-dibromocarbazole derivative, was observed to inhibit cytochrome c releasing from mitochondria by Bax channel modulation. The monohydroxy analogue Bax channel blocker remained the unprecedented inhibition of Bax-induced cytochrome c release at 10 μM. The IC50 value of Bax channel blocker was determined to be 0.52 μM, indicating that Bax channel blocker was a Bax channel inhibitor as hypothesized. Moreover, in the liposome assay, Bax channel blocker showing significant inhibition (>65%) of cytochrome c release at 10 μM also demonstrated sub-micromolar IC50 value [1].


In vivo: So far, there is no animal in vivo study conducted for Bax channel blocker.


Clinical trial: N/A


Reference:
[1] Bombrun A,Gerber P,Casi G,Terradillos O,Antonsson B,Halazy S.  3,6-dibromocarbazole piperazine derivatives of 2-propanol as first inhibitors of cytochrome c release via Bax channel modulation. J Med Chem.2003 Oct 9;46(21):4365-8.