Bax channel blocker is a potent inhibitor of Bax-mediated mitochondrial cytochrome c release.
Potent inhibitor of Bax-mediated mitochondrial cytochrome c release (IC 50 = 0.52 μ M). Suggested to inhibit Bax channel formation/activity.
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].
[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.
