BI-2536 is a potent inhibitor of PLK1 (Polo-like kinase 1, IC₅₀ ~0.83 nM) and BRD4 (IC₅₀ ~37 nM).  It also inhibits PLK2 and PLK3 with IC₅₀ of 3.5 nM and 9.0 nM, respectively. BI-2536 treatment ranging from 10 nM to 100 nM leads to the blocking of the recruitment of γ-tubulin and phosphorylation of Apc6 at mitotic centrosomes, inhibition of cohesin release from chromosome arms, induction of monopolar spindles, and other Plk1 dependent processes. BI-2536 inhibits the growth of a panel of 32 human cancer cell lines with EC₅₀ of 2-25 nM. It also displaces BRD4 from chromatin and suppresses c-Myc expression. The combination of inhibitory activities on independent kinase and bromodomain oncogenic pathways exemplifies a new strategy for rational single-agent polypharmacological targeting. 

How to Use:

In vitro:  BI-2536 was used at 0.1-1 µM in vitro.

In vivo:  BI-2536 was dosed to mice by IV injection at 50 mg/kg once or twice a week in xenograft models. (Formulated in hydrochloric acid (0.1 N), and diluted with 0.9% NaCl)

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