產(chǎn)品目錄

規(guī)格	10mg 50mg
CAS	335165-68-9
別名
化學(xué)名	1-(3,6-dibromocarbazol-9-yl)-3-piperazin-1-ylpropan-2-ol;dihydrochloride
分子式	C19H21Br2N3O.2HCl
分子量	540.12
溶解度	<46.72mg/ml in DMSO
儲(chǔ)存條件	Desiccate at RT
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

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.

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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