[CAS NO. 331244-89-4]  BAM7

BAM7 directly binds the previously uncharacterized BH3-binding groove at the N-terminal face of BAX. BAM7 is selective for the BH3-binding groove at the N-terminal face of BAX. BAM7 directly interacts with BAX at the very surface used by the BIM BH3 helix to trigger BAX activation. BAM7 results in functional BAX activation. BAM7 triggers the conversion of BAX from monomer to oligomer in a dose- and time-responsive manner, the kinetics of which approach saturation at a 1:8 dose ratio of BAX:BAM7. BAM7 triggers in vitro BAX oligomerization, BAX-mediated pore formation and BAX-dependent cell death. BAM7 selectively induces BAX-mediated apoptosis by triggering the hallmark features of intracellular BAX activation. BAM7 only kills the cell line that contains BAX, eliciting the biochemical and morphologic features of BAX-mediated apoptosis.