bi 2536

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.

(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.

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.

PLK1 BRD4-IN-2 (compound 15), an analog of BI-2536, simultaneously inhibits both Polo-like kinase 1 (PLK1 IC 50 = 40 nM) and BRD4 bromodomain (BRD4-BD1 IC 50 = 28 nM) as a dual inhibitor [1].

BI-4834 is a potent and selective Polo-like kinase 1 (PLK1) inhibitor. BI-4834 is also analogue (or Me-Too) of BI-2536. In vitro test shows that BI 4834 inhibits PLK1 with IC50=7.6 nm, but with higher selectivity over the related enzyme PLK3 (IC50 198.4 nm) as BI-2536.