335165-68-9 Usage
Uses
Bax channel blocker is a potent inhibitor of Bax-mediated mitochondrial cytochrome c release.
Biological Activity
Potent inhibitor of Bax-mediated mitochondrial cytochrome c release (IC 50 = 0.52 μ M). Suggested to inhibit Bax channel formation/activity.
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].
IC 50
0.52 μm in bax assay
references
[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.
Check Digit Verification of cas no
The CAS Registry Mumber 335165-68-9 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 3,3,5,1,6 and 5 respectively; the second part has 2 digits, 6 and 8 respectively.
Calculate Digit Verification of CAS Registry Number 335165-68:
(8*3)+(7*3)+(6*5)+(5*1)+(4*6)+(3*5)+(2*6)+(1*8)=139
139 % 10 = 9
So 335165-68-9 is a valid CAS Registry Number.
InChI:InChI=1/C19H21Br2N3O.2ClH/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;;/h1-4,9-10,15,22,25H,5-8,11-12H2;2*1H
335165-68-9Relevant academic research and scientific papers
3,6-Dibromocarbazole piperazine derivatives of 2-propanol as first inhibitors of cytochrome C release via bax channel modulation
Bombrun, Agnes,Gerber, Patrick,Casi, Giulio,Terradillos, Olivier,Antonsson, Bruno,Halazy, Serge
, p. 4365 - 4368 (2007/10/03)
There is compelling evidence that Bax channel activity stimulates cytochrome c release leading ultimate]y to cell death, which is a key event in ischemic injuries and neurodegenerative diseases. Here 3,6-dibromocarbazole piperazine derivatives of 2-propan
9-(Piperazinylalkyl)carbazoles as Bax-modulators
-
, (2008/06/13)
The present invention is related to piperazine derivatives of carbazole notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such piperazine derivatives of carbazole. Said piperazine derivatives of car
