794466-17-4

DAP-81 is a diaminopyrimidine derivative that targets PLKs, destabilizing kinetochore microtubules. Other spindle tubules are stabilized, resulting in monopolar mitotic spindles. In vitro, DAP-81 inhibits Plk1 at an IC50 of 0.9 nM. DAP-81 is currently in ongoing preclinical evaluations.