Description: BI2536 is an effective Plk1 inhibitor (IC50: 0.83 nM). It has 4- and 11-fold greater selectivity than Plk2 and Plk3. Target: Epigenetic Reader Domain, Apoptosis, PLK. Smiles: C(C)[C@H]1N(C=2C(N(C)C1=O)=CN=C(NC3=C(OC)C=C(C(NC4CCN(C)CC4)=O)C=C3)N2)C5CCCC5. References: Steegmaier M, et al. BI 2536, a...

Polo-like kinases (Plks) are serine/threonine kinases with key roles in cell cycling. BI-2536 is a 2-aminopyrimidine-containing inhibitor of Plk1 (IC50 = 0.83 nM). It displays 4- and 11-fold selectivity for Plk1 over Plk2 and Plk3, respectively. BI-2536 induces mitotic arrest and apoptosis in diverse human cancer...

Soluble in DMSO, Ethanol. Polo-like kinase 1 (Plk1) is a regulator of the cell cycle that has been implicated in the pathology of many cancers. BI-2536 is a potent and selective small-molecule inhibitor of mammalian Plk1. It has inhibitory activity at subnanomolar concentrations and inhibits tumor growth in...

PLK1 inhibitor.

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 IC50 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...