BI-2536

BI-2536 is a potent, ATP-competitive, well tolerated and effects Polo-like kinases (Plks) as well as a pan-BET (bromodomain and extra-terminal motif) family inhibitor. BI-2536 has an IC50of 0.83 and 25 nM with PLK1 and BRD4 inhibitor, respectively. BI-2536 also blocks the activities of Plk2 and Plk3 to a slightly lesser extent with IC50of 3.5 nM and 9.0 nM, respectively. BI-2536 suppresses IFNB (encoding IFN-ß) gene transcription. It also shows good blood-brain barrier permeability and causes mitotic arrest in glioblastoma-derived neural stem cells but not normal neural stem cells.