Bioymifi(DR5 Activator) is the first novel and potent small-molecule activatior of the TRAIL receptor DR5 in human cancer cells.IC50 value:Target: In comparison with A2C2, bioymifi was able to promote cell death without the need for the Smac mimetic in T98G cells. Notably, at a 10-μM concentration, bioymifi induced processing of caspase-3 into smaller fragments. Z-VAD inhibited these caspase-mediated cleavages. caspase-3 was rapidly activated as early as 2 h after bioymifi treatment of T98G cells. The caspase-3 activity was markedly increased after 8 h of treatment. Bioymifi induces caspase-8-dependent apoptosis.
[1]. Wang G, et al. Small-molecule activation of the TRAIL receptor DR5 in human cancer cells. Nat Chem Biol. 2013 Feb;9(2):84-9.