Centrinone is a selective and reversible inhibitor of polo-like kinase 4 (Plk4), a serine-threonine protein kinase that initiates centriole/centrosome assembly.

HMN-214 is a potent PLK1 inhibitor an average IC50 of 0.12 μM, and a prodrug of HMN-176, which alters the cellular spatial orientation of Plk1.

Poloxin is a non-ATP competitive Polo-like Kinase 1 (PLK1) inhibitor that targets the polo-box domain.

CFI400945 is a potent and selective,orally bioavailable PLK4 inhibitor with an IC50 value of 2.8 ±1.4 nM have potential antineoplastic activity.

RO3280 is a potent, highly selective inhibitor of Polo-like kinase 1 (PLK1) with IC50 of 3 nM.

CFI-400437 is a selective ATP-competitive PLK4 inhibitor with IC50 value of 1.55nM.

MLN0905 is a small-molecule and potent inhibitor of PLK1 with IC50 of 2 nM.

Rigosertib Sodium (Random Configuration) is a non-ATP-competitive inhibitor of PLK1 with IC50 of 9 nM in a cell-free assay. It shows 30-fold greater selectivity against Plk2 and no activity to Plk3.

SBE13 HCl is a potent and selective PLK1 inhibitor with IC50 of 0.2 nM while 875 nM and 66 μM for PLK3 and PLK2. SBE 13 could also induce cell cycle arrest, reduce cell proliferation with EC50 of 5-60 µM, and induce apoptosis in a broad range of human cancer cell lines.

NMS-1286937 is an orally bioavailable, small-molecule Polo-like kinase 1 (PLK1) inhibitor (IC50=2 nM) with potential antineoplastic activity and no inhibition on PLK2 and PLK3.

Poloxime is an analogue of thymoquinone, which bind to the phosphoserine/phosphothreonine recognition site of the polo-box domain of polo-like kinase 1.

GW843682X is a selective PLK1 and PLK3 inhibitor with IC50s of 2.2 nM (PLK1) and 9.1 nM (PLK3) and displays > 100-fold selectivity over ~30 other kinases tested including cdk1 and cdk2.

Rigosertib is a non-ATP-competitive inhibitor of PLK1 with IC50 of 9 nM and shows 30-fold greater selectivity against PLK2 and no activity to PLK3.

GSK461364 is a potent small molecule Polo-like kinase 1 (PLK1) inhibitor with a Ki of 2.2 nM.

TAK-960 is an investigational, orally bioavailable, potent, and selective PLK1 inhibitor (IC50=1.5 nM) that has shown activity in several tumor cell lines, including those that express multidrug-resistant protein 1 (MDR1).

BI6727 is an ATP-competitive kinase inhibitor from the dihydropteridinone class of compounds.

LFM-A13 is a potent and selective inhibitor of Btk with IC50 of 17.2 μM and also inhibits PLK3 with IC50 of 7.2 μM.