Toggle Nav

Bax channel blocker

In stock
Catalog No.
A4459
Inhibitor of Bax-mediated mitochondrial cytochrome c release
Grouped product items
SizePriceStock Qty
10mg
$251.00
In stock
50mg
$1,057.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

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.

Chemical Properties

Physical AppearanceWhite solid
StorageDesiccate at RT
M.Wt540.12
Cas No.335165-68-9
FormulaC19H21Br2N3O.2HCl
Solubility<46.72mg/ml in DMSO; <2.34mg/ml in H2O
Chemical Name1-(3,6-dibromocarbazol-9-yl)-3-piperazin-1-ylpropan-2-ol;dihydrochloride
SDFDownload SDF
Canonical SMILESC1CN(CCN1)CC(CN2C3=C(C=C(C=C3)Br)C4=C2C=CC(=C4)Br)O.Cl.Cl
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Quality Control

Quality Control & MSDS

View current batch:

Chemical structure

Bax channel blocker