apcin

Apcin is a small molecule inhibitor of the Cell Division Cycle protein 20 (CDC20), which serves as a key activator and substrate recruiter for the Anaphase-Promoting Complex/Cyclosome (APC/C) E3 ubiquitin ligase. By binding to the D-box binding pocket of CDC20, apcin competitively blocks the interaction between CDC20 and its substrates, such as securin and cyclin B1, thereby inhibiting their ubiquitination and subsequent degradation. In the context of pulmonary arterial hypertension (PAH), apcin has been shown to suppress the hyper-proliferation and induce apoptosis of pulmonary artery smooth muscle cells (PASMCs) and adventitial fibroblasts (PAAFs) by restoring levels of the pro-apoptotic protein BIM. While primarily utilized as a high-affinity research tool to study cell cycle regulation and mitotic exit, its ability to reverse vascular remodeling in preclinical models highlights its potential as a therapeutic lead for proliferative diseases.