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.

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

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.

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

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

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.

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

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.

IIP0943 is a selective PLK1 (polo-like kinase 1) inhibitor with an IC50 of 5.1 nM for PLK1. It also exhibits inhibitory activity on the proliferation of HCT116 cells, with an IC50 of 0.22 µM. IIP0943 shows potential for research in the field of oncology.

PLK1-IN-14 (Compound Hit-4) is a selective PLK1 inhibitor with an IC50 of 22.61 pM for PLK1, and an IC50 of 0.09 nM for inhibiting the proliferation of DU-145 prostate cancer cells. It is applicable in prostate cancer research.

PLK1-IN-12 is a highly selective, orally active PLK1 inhibitor with an IC50 of 20 nM. It demonstrates greater selectivity for PLK1 over PLK2 (IC50: >10000 nM) and PLK3 (IC50: 3953 nM). PLK1-IN-12 exhibits anticancer efficacy across a wide range of cell lines and is applicable to anti-leukemia research.

PLK1-IN-13 is a selective, orally active PLK1 inhibitor with an IC50 of 0.27 nM. It also inhibits PLK2 (IC50: 12.72 nM) and PLK3 (IC50: 4.12 nM). PLK1-IN-13 induces cell cycle arrest at the G2 phase, promotes apoptosis, and downregulates the transcription of the cancer-associated oncogene c-MYC. This compound inhibits tumor growth and is applicable for research in acute myeloid leukemia (AML).

PLK1/PRC1-IN-1 (compound B4) is an inhibitor that prevents the formation of the PLK1/PRC1 protein complex. It is useful for research involving non-small cell lung cancer (NSCLC).

PLK1-IN-15 is a PLK1 inhibitor with an IC50 of 38.5 nM. It exhibits antiproliferative effects on HepG2, Huh7, H1299, and A549 cells, with IC50 values of 2.03, 2.08, 4.79, and 17.11 μM, respectively. Additionally, PLK1-IN-15 can induce cell cycle arrest in the G2/M phase and trigger apoptosis (Apoptosis), demonstrating anticancer activity.