Apoptosis is induced by certain cytokines including TNF and Fas ligand in the TNF family through their death domain containing receptors. TNF-related apoptosis-inducing ligand (TRAIL or Apo2L), a member of this family, activates apoptosis in a variety of tumor cell lines by signaling through the death receptors, DR4 and DR5. Bioymifi directly activates DR5 (Kd = 1.2 ?M; IC50 = 2 ?M), inducing DR5 clustering, which leads to the initiation of FADD/caspase-8-dependent apoptosis in various cancer cells.1
1.Wang, G., Wang, X., Yu, H., et al.Small-molecule activation of the TRAIL receptor DR5 in human cancer cellsNat. Chem. Biol.984-90(2012)