Apoptosis Activator 2 is a small molecule apoptosis activator with IC50 value of about 4μM [1].
Apoptosis Activator 2 is a cell permeable compound that promotes apoptosis by activating caspases in a cytochrome c- and Apaf-1-dependent manner. 20μM Apoptosis Activator 2 increases the fraction of Apaf-1 in the apoptosome when there is 0.15μM cytochrome c. It is found to induce the oligomerization of Apaf-1. Through the induction of apoptosis, Apoptosis Activator 2 notably induces caspase-3 activation, PARP cleavage and DNA fragmentation. Moreover, this induction of apoptosis only occurs in tumor cell lines (such as breast, lung, colon, and epidermal cancer cell lines). Normal cell lines are resistant to Apoptosis Activator 2 [1, 2].
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.