BI 2536 was originally reported as a potent (IC50s Plk1 = 0.83nM, Plk2 = 3.5nM and Plk3 = 9.0nM) and selective2 Polo-like kinase inhibitor (IC50s Plk1 = 0.83nM, Plk2 = 3.5nM and Plk3 = 9.0nM) that caused mitotic arrest and apoptosis induction in various human cancer cell lines.1 It was later found to be a potent inhibitor (IC50 = 100nM) of BET family member BRD4 and able to potently suppress c-Myc expression in MM.1S multiple myeloma cells.3 BI 2536 destabilizes N-Myc by inhibiting the deactivation of the ubiquitin E3 ligase Fbw7 by Plk1.4
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