bi2536

BI2536 is an effective Plk1 inhibitor (IC50: 0.83 nM). It has 4- and 11-fold greater selectivity than Plk2 and Plk3.

BI-2563 is a small molecule compound with potential antitumor properties. It binds to Polo-like kinase 1 (Plk1) and inhibits its activity, resulting in mitotic arrest, interruption of cell division, and apoptosis in susceptible tumor cell populations. Plk1 is a serine/threonine-protein kinase that serves as a key regulator of several critical processes essential for mitosis and cytokinesis.

BI2536-PEG2-Halo is a bifunctional molecule that integrates a Halo tag ligand with the Polo-like kinase 1 (PLK1) inhibitor BI-2536. This compound selectively exerts cytotoxic effects on mutant p53 cancer cells and inhibits the proliferation of 293T cells expressing the Halo-p53R273H(FL)-mCherry tag, with an IC50 value of 23 nM.

(S)-BI 2536 serves as a dual inhibitor, targeting both PLK1 kinase and the BRD4 bromodomain, with Ki values of 0.42 nM and 54 nM, respectively. It is recognized as the less active enantiomer of BI 2536.