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Merck

196805

Bax Channel Blocker

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

Synonym(s):

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

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About This Item

Empirical Formula (Hill Notation):
C19H21Br2N3O
CAS Number:
335165-69-0
Molecular Weight:
467.20
MDL number:
MFCD09037523
UNSPSC Code:
12352200
NACRES:
NA.77

Key Documents

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Product Name

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

storage temp.

2-8°C

Quality Level

100

Related Categories

Disclaimer

Toxicity: Carcinogenic / Teratogenic (D)

Biochem/physiol Actions

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

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).

Other Notes

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

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.

Legal Information

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

Storage Class

11 - Combustible Solids

wgk

WGK 1

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

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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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