GSK461364 (GSK461364A)(Ki=2.2 nM) inhibits purified Plk1 .The specificity of GSK461364 for Plk1 is more than 1000-fold over Plk2/3.

Volasertib (BI 6727) (BI-6727) is a potent inhibitor of PLK1 (IC50: 0.87 nM), inducing mitotic arrest and apoptosis. It also inhibits PLK2/PLK3 (IC50s: 5/56 nM).

3MB-PP1 is a bulky purine analog and a Polo-like kinase 1 (Plk1) inhibitor. In cells expressing analog-sensitive Plk1 alleles, 3MB-PP1 blocks mitotic progression and cell division arise by targeting Plk1. 3MB-PP1 specifically inhibits analog-sensitive Ssn3 (Cdk8). 3MB-PP1 inhibits Leu93 Mutant Zipper-interacting protein kinase with IC50 of 2 μM. 3MB-PP1 can be used for the research of cell division and hypha formation of Candida albicans.

SBE13 Hydrochloride (SBE 13 HCl) is an effective and specific PLK1 inhibitor (IC50: 0.2 nM); no inhibition om Aurora A kinase, Plk2/3.

Pyridoxine (Vitamin B6) is the 4-methanol form of vitamin B6 and is converted to pyridoxal 5-phosphate in the body. Although pyridoxine and vitamin B6 are still frequently used as synonyms, especially by medical researchers, this practice is erroneous and sometimes misleading.

ON-01910 is a non-ATP-competitive PLK1 inhibitor(IC50 of 9 nM, in a cell-free assay). It shows 30-fold greater selectivity against Plk2 and no activity to Plk3. Rigosertib inhibits PI3K/Akt pathway and activates oxidative stress signals. Rigosertib induces apoptosis in various cancer cells.It is a synthetic benzyl styryl sulfone analogue with potential antineoplastic activity.

T521 is a selective inhibitor of the PBD of Plk1 and shows no inhibitory effect on Plk2 and Plk3.

Poloxin-2 is a potent and selective Plk1 PBD inhibitor with anti-tumour activity that reduces the protein level of Plk1 in HeLa cells.