Biochem/physiol Actions
Potent and selective cytosolic BAX dimer modulator that effectively induces apoptosis in cancer cells by selectively modulating inactive BAX.
BDM19, a potent BAX dimer modulator with a Kd of 560 nM, selectively binds to the N-terminal trigger site of inactive BAX, thereby inhibiting its dimerization with an IC50 of 5 μM. By stabilizing the inactive conformation of BAX, BDM-19 allosterically activates it, targeting cells containing cytosolic inactive BAX monomers and dimers. This leads to a dose-dependent translocation of BAX to mitochondria, subsequent cytochrome c release, and induction of apoptosis.