E8431 (Z2371498431) is a specific small molecule antagonist of fusogenic protein DCSTAMP, disrupts DCSTAMP-RAP1B interaction and inhibits RAP1-RAC1 signaling-mediated cytoskeletal reorganization required for osteoclast maturation and fusion, demonstrats significant osteoclastogenesis inhibition (IC50=0.7758 μM) without cytotoxic effects on mBMMs.
E8431 effectively reduces the formation of bone-resorbing cells without harming other cells.
E8431 binds to human and mouse DCSTAMP proteins with binding energies of −10.4 kcal/mol and −10.1 kcal/mol, respectively.
E8431 promotes angiogenesis in the coculture system of mEPCs with mBMMs in vitro.
potentiates osteogenic and angiogenic processes through inhibitory modulation of PDGFBB secretion from pre-osteoclastic fusion events in vitro.
E8431 directly disrupts the binding of DCSTAMP and RAP1B, effectively suppresses osteoclastogenesis by disrupting DCSTAMP-RAP1B interactions, thereby inhibiting RAP1–RAC1 signaling-mediated cytoskeletal reorganization required for osteoclast maturation and fusion.