PLK1 Inhibitor

MLN0905 (PLK1 Inhibitor) is an effective PLK1 inhibitor(IC50=2 nM).

CCB02 is a selective CPAP-tubulin interaction inhibitor (IC50: 689 nM) with anti-tumor activity, showing no inhibition on cell cycle- and centrosome-related kinases, nor affecting the phosphorylation status of Aurora-A, CDK2, Plk1, Plk2, and CHK1.

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.

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

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

Plogosertib (CYC140) is an orally active, selective, potent, and ATP-competitive PLK1 inhibitor with an IC50 value of 3 nM.Plogosertib exhibits antiproliferative and anticancer activity and can be used for the study of solid and hematologic tumors. and hematologic tumors.

AAPK-25 is a potent and selective Aurora PLK dual inhibitor with anti-tumor activity, causing mitotic delay and arresting cells in prometaphase, followed by increased apoptosis. It targets Aurora-A -B -C with Kd values ranging from 23-289 nM.

GW843682X (GW843682) is a selective and ATP-competitive inhibitor of PLK1 and PLK3 (IC50s = 2.2 nM and 9.1 nM).

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).

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

Onvansertib (NMS-1286937) is a PLK1 inhibitor (IC50=2 nM) with high selectivity and oral activity. Onvansertib has antitumor activity and inhibits tumor growth.

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

Wortmannin (SL-2052) is a PI3K inhibitor (IC50=3 nM) that is covalent and irreversible. Wortmannin is also an inhibitor of PlK1 and PlK3 (IC50=5.8 48 nM) that blocks autophagy.

Poloxin is a non-ATP competitive Polo-like Kinase 1 inhibitor targeting the polo-box domain (IC50: appr 4.8 μM).

TC-S 7005 is an effective inhibitor of Polo-like kinases (IC50s: 214 nM, 4 nM and 24 nM for Plk1, Plk2, and Plk3).

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

HMN-176 is a stilbene derivative which inhibits mitosis, interfering with polo-like kinase-1 (plk1).

Rigosertib sodium (ON-01910), a non-ATP-competitive inhibitor of PLK1(IC50=9 nM), exhibits 30-fold higher specificity activity over Plk2 and no effect on Plk3.

Poloxime is a hydrolysis product of poloxin and is a non-ATP-competitive Plk1 inhibitor. It also has moderate Plk1 inhibitory activity.

Rigosertib (ON-01910) is a selective, non-ATP-competitive PLK1 inhibitor (IC50: 9 nM) and multi-kinase inhibitor. As a selective anti-cancer agent, Rigosertib induces apoptosis by inhibiting the PI3 kinase Akt pathway, promotes histone H2AX phosphorylation, and induces G2 M arrest in the cell cycle.

Mps1-IN-2 is a potent, selective, and ATP-competitive inhibitor of both Mps1 and Plk1.

TTK PLK1-IN-1 (Formula I) is an inhibitor of threonine tyrosine kinase (TTK) and polo-like kinase 1 (PLK1), with IC50 values of 7 nM and 72 nM, respectively. It regulates the spindle assembly checkpoint (SAC) and exhibits antitumor activity against triple-negative breast cancer (TNBC).

PLK1-IN-11 (Cluster 4, 16953209) is a PLK1 inhibitor with an IC50 of 1 μM. It is applicable in research on various cancers such as pancreatic, ovarian, breast, and non-small cell lung cancer.

Cyclapolin 9 is a selective, potent, and ATP-competitive inhibitor of polo-like kinase 1 (PLK1) with an IC50 of 500 nM, and has not shown activity against other kinases.