BI-2536 is a polo-like kinase 1 (PLK1) inhibitor that disrupts mitosis and cell division. BI-2536 exhibits anticancer activity and may induce apoptosis in cancer cells.

A selective inhibitor of Plk1 (IC₅₀ = 0.83 nM); induces mitotic arrest and apoptosis in diverse human cancer cell lines and drives regression of human tumor xenografts in nude mice; also an inhibitor of BRD4 (IC₅₀ = 25 nM).