Uses
Activates apoptosis in cells; shows selectivity for cancer cells against normal cell lines
Uses
Apoptosis Activator 2 activates caspases in a cytochrome c-dependent manner and induces apoptosis in tumor cells.
Definition
ChEBI: 1-[(3,4-dichlorophenyl)methyl]indole-2,3-dione is a member of indoles.
Biological Activity
Apoptosis activator; promotes the cytochrome c-dependent oligomerization of Apaf-1 into the mature apoptosome. Increases procaspase-9 processing and subsequent caspase-3 activation. Induces apoptosis in tumor cells (IC 50 = 4-9 μ M for leukaemia cells) with weak or no effect on normal cell lines or those defective/deficient in Apaf-1, caspase-9 or caspase-3 activity (IC 50 > 40 μ M).
References
[1] nguyen jt, wells ja. direct activation of the apoptosis machinery as a mechanism to target cancer cells. proc natl acad sci u s a. 2003 jun 24;100(13):7533-8.
[2] nguyen tv, jayaraman a, quaglino a, pike cj. androgens selectively protect against apoptosis in hippocampal neurones. j neuroendocrinol. 2010 sep;22(9):1013-22.
