centrinone

Centrinone is a potent and highly selective small-molecule inhibitor of Polo-like kinase 4 (PLK4), which serves as the master regulator of centriole duplication. By binding to the ATP-binding site of PLK4, centrinone effectively blocks the formation of new centrioles, leading to the progressive loss of centrosomes during successive cell divisions. In normal cells, this centrosome depletion typically triggers a p53-dependent cell cycle arrest in the G1 phase. However, many cancer cell lines exhibit a centrosome-independent proliferation capability, allowing them to continue dividing despite the loss of centrosomes, albeit often with increased genomic instability or altered spindle assembly. Centrinone is primarily utilized as a chemical biology tool to study centrosome biology and has been investigated in preclinical research for its potential to selectively target cancer cells or modulate hyperproliferative skin conditions, though results in some models like psoriasis and skin papilloma have been negative.

Other names

centrinone-B