Description
Apcin is an inhibitor of the E3 ligase activity of the mitotic anaphase-promoting complex/cyclosome (APC/C), which is a large multimeric complex. It functions as a ubiquitin ligase, initiating the metaphase-anaphase transition and regulating ordered transitions through the cell cycle by controlling the ubiquitin-mediated proteolysis of cell cycle proteins. It competitively binds to the D-box binding site of Cdc20 and prevents substrate recognition and ubiquitylation required for continuation of mitosis. It synergistically increases apoptosis in multiple myeloma cells in combination with proTAME (prodrug of TAME). It also prolongs mitotic duration in RPE1 cells in combination with proTAME in vitro. It blocks mitotic exit and being synergistically amplified by co-addition of Ts-Arg-OMe