BAX activator 27c is a selective small molecule BAX activator with binding IC50 of 0.3 uM in competitive FP binding assays, shows >40-fold selectivity over other antiapoptotic BCL-2 family proteins.
BAX activator 27c exhibits broad-spectrum cytotoxicity in various AML cells (IC50 < 10 uM).
BAX activator 27c exhibits direct and selective interaction with BAX rather than BAK in living cells. binds to cytosolic BAX in a dose-dependent manner but had no obvious effect on mitochondrial BAX.
BAX activator 27c (1.25-10 uM) induced time-dependent BAX oligomerization.
BAX activator 27c primarily induced late-stage apoptosis, promoted the cleavage of caspase-9, caspase-3, and PARP in a dose-dependent manner in THP-1 cells.
BAX activator 27c exhibited reasonable potency in hematologic cancer cells with IC50 values ranging from 2 to 5 μmol/L, but relatively lower potency in solid tumor cells.