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Merck
CN

196805

Bax Channel Blocker

≥95% (HPLC), Bid-induced cytochrome C release blocker, solid

别名:

Bax Channel Blocker, (±)-1-(3,6-Dibromocarbazol-9-yl)-3-piperazin-1-yl-propan-2-ol, iMAC1

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关于此项目

经验公式(希尔记法):
C19H21Br2N3O
化学文摘社编号:
分子量:
467.20
MDL编号:
UNSPSC代码:
12352200
NACRES:
NA.77
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产品名称

Bax Channel Blocker, A cell-permeable dibromocarbazolo-piperazinyl derivative that displays anti-apoptotic properties.

质量水平

方案

≥95% (HPLC)

表单

solid

制造商/商品名称

Calbiochem®

储存条件

OK to freeze
desiccated (hygroscopic)
protect from light

颜色

off-white

溶解性

DMSO: 10 mg/mL

运输

ambient

储存温度

2-8°C

SMILES字符串

FC(F)(F)C(=O)O.FC(F)(F)C(=O)O.Brc1cc2c([n](c4c2cc(cc4)Br)CC(O)CN3CCNCC3)cc1

InChI

1S/C19H21Br2N3O.2C2HF3O2/c20-13-1-3-18-16(9-13)17-10-14(21)2-4-19(17)24(18)12-15(25)11-23-7-5-22-6-8-23;2*3-2(4,5)1(6)7/h1-4,9-10,15,22,25H,5-8,11-12H2;2*(H,6,7)

InChI key

LPXZQYWZSBDVIG-UHFFFAOYSA-N

一般描述

A cell-permeable dibromocarbazole-piperazinyl derivative that displays anti-apoptotic properties. Reported to effectively block Bid-induced cytochrome c release from HeLa cell mitochondria (~80% inhibition at 5 µM) by inhibiting Bax channel activity.
A cell-permeable dibromocarbazolo-piperazinyl derivative that displays anti-apoptotic properties. Effectively blocks Bid-induced cyctochrome c release from HeLa cell mitochondria (~80% inhibition at 5 µM) by inhibiting Bax channel-forming activity (IC50 = 520 nM in a liposome channel assay).

生化/生理作用

Cell permeable: yes
Primary Target
Bax-channel forming activity
Product does not compete with ATP.
Reversible: no
Target IC50: 520 nM blocks Bid-induced cyctochrome c release from HeLa cell mitochondria by inhibiting Bax channel-forming activity in a liposome channel assay

包装

Packaged under inert gas

外形

Supplied as a trifluoroacetate salt.

制备说明

Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

其他说明

Peixoto, P., et al. 2009. Biochem J.423, 381.
Bombrun, A., et al. 2003. J. Med. Chem.46, 4365.

法律信息

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

免责声明

Toxicity: Carcinogenic / Teratogenic (D)

储存分类代码

11 - Combustible Solids

WGK

WGK 1

闪点(°F)

Not applicable

闪点(°C)

Not applicable


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Dulguun Amgalan et al.
Nature cancer, 1(3), 315-328 (2020-08-11)
Doxorubicin remains an essential component of many cancer regimens, but its use is limited by lethal cardiomyopathy, which has been difficult to target, owing to pleiotropic mechanisms leading to apoptotic and necrotic cardiac cell death. Here we show that BAX

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