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 number:
UNSPSC Code:
12352200
NACRES:
NA.77
产品名称
Bax Channel Blocker, A cell-permeable dibromocarbazolo-piperazinyl derivative that displays anti-apoptotic properties.
SMILES string
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
assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, desiccated (hygroscopic), protect from light
color
off-white
solubility
DMSO: 10 mg/mL
shipped in
ambient
Quality Level
General description
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).
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Bax-channel forming activity
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
Packaging
Packaged under inert gas
Physical form
Supplied as a trifluoroacetate salt.
Preparation Note
Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Peixoto, P., et al. 2009. Biochem J.423, 381.
Bombrun, A., et al. 2003. J. Med. Chem.46, 4365.
Bombrun, A., et al. 2003. J. Med. Chem.46, 4365.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Carcinogenic / Teratogenic (D)
存储类别
11 - Combustible Solids
wgk
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable
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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