BI-2536

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 IC50s of 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 IC50 of 3.5 nM and 9.0 nM, respectively. BI-2536 suppresses IFNB (encoding IFN-beta) 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.