plk1 in 2

PLK1-IN-2 is a PLK1 kinase inhibitor with an IC [50] value of 0.384 μM.

PROTACPLK1 Degrader-2 (Compound NC1) is a PLK1 PROTAC degrader with a dissociation constant (Kd) of 6.06 μM. It significantly inhibits the proliferation of HeLa cells, inducing cell cycle arrest and apoptosis. In mouse models with HeLa cell xenografts, PROTACPLK1 Degrader-2 displays strong antitumor activity, making it a valuable tool for studying cervical cancer.

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].

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.

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

Arg12-AHX is a synthetic ligand-linker conjugate for E3 ligase, utilized in synthesizing PROTACs like PROTACPLK1 Degrader-2. This compound, PROTACPLK1 Degrader-2, functions as a PLK1 PROTAC degrader with anti-tumor activity.

POI ligand-3 (Compound 4j) is a peptide-based PLK1PBD inhibitor and can be utilized as a target protein ligand in the synthesis of PROTACs, such as PROTACPLK1 Degrader-2.

Anticanceragent 306, a spirotetraacid derivative, serves as an inhibitor of MMP1, MMP7, and PLK1. It exhibits antiproliferative effects on H1299, RKO, and MCF-7 cells, with IC50 values of 19.25 μM, 3.29 μM, and 102.36 μM, respectively. The compound induces cell cycle arrest by upregulating p21 protein and downregulating CCND1 and CCNB1 proteins, and it modulates Bcl-2 and Bax expression to trigger apoptosis (apoptosis). Furthermore, by downregulating MMP1 and MMP7 proteins, it inhibits tumor invasion and metastasis. Anticanceragent 306 is applicable in studies related to lung cancer, colorectal cancer, and breast cancer.

JH295 is a highly potent and selective inhibitor of NIMA-related kinase 2 (Nek2), exhibiting irreversible inhibition activity with an IC 50 value of 770 nM. This compound effectively inhibits cellular Nek2 using the alkylation of Cys22. Importantly, JH295 does not exhibit any inhibitory effects toward Cdk1, Aurora B, or Plk1, which are kinases involved in mitotic processes. Furthermore, JH295 has no impact on bipolar spindle assembly or the spindle assembly checkpoint mechanism.