PLK

Nε-(1-Carboxymethyl)-L-lysine is a unique post-translational modification (PTM) of proteins that is generated by the non-enzymatic glycation of lysine residues.

A Plk1 inhibitor

Poloppin is a potent, cell penetrant inhibitor of the mitotic Polo-like kinase (PLK) (IC50=26.9?μM) and prevents the protein-protein interaction via the Polo-box domain (PBD) (Kd= 29.5?μM). Poloppin selectively kills cells expressing mutant KRAS, enhancing death in mitosis.?Poloppin is used for the study of KRAS-mutant cancers as single agents, or in combination with c-MET inhibitors.

ON1231320 is a highly specific polo like kinase 2 (PLK2) inhibitor with an IC50 of 0.31 ?M. ON1231320 blocks tumor cell cycle progression in the G2/M phase in mitosis, causing apoptotic cell death. ON1231320, an arylsulfonyl pyrido-pyrimidinone, has antitumor activity.

(1E)-CFI-400437 dihydrochloride is a potent PLK4 (IC50= 0.6 nM) inhibitor and selective against other members of the PLK family (>10 μM). (1E)-CFI-400437 dihydrochloride inhibits Aurora A, Aurora B, KDR and FLT-3 with IC50s of 0.37, 0.21, 0.48, and 0.18 μM, respectively. Antiproliferative activity.

PLK4-IN-1 (Example A6) is a PLK4 inhibitor, with an IC50 of ≤ 0.1 μM.

Lipid 8 is an ionizable cationic lipid molecule that can be protonated in acidic buffers to efficiently compress mRNA, forming the core of lipid nanoparticles.

Plogosertib (CYC140) is a selective, potent, orally active ATP-competitive PLK1 inhibitor (IC50: 3 nM). Plogosertib is an anti-cancer agent with anti-proliferative activity and can be used for research on various tumors including esophageal cancer, gastric cancer, leukemia, non-small cell lung cancer, ovarian cancer and squamous cell carcinoma.

PLK4-IN-4 (compound 22) is a potent PLK4 inhibitor with an IC50 value of 7.9 nM.

SP27 is a PROTAC that can selective degrades PLK4, with a DC50 of 19.5 nM.

Aurora Kinases-IN-3 (Compound 15a) is an orally active AURKB inhibitor that elicits an AURKB-suppressive activity by disrupting the mitotic localization of AURKB.

PLK1/BRD4-IN-5 (Compound SC10) is an orally active PLK1 and BRD4 inhibitor with IC50 values of 0.3 nM and 60.8 nM, respectively.

PLK1/BRD4-IN-3 (Compound 21) is a selective dual inhibitor for bromodomain 4 (BRD4) and polo-like kinase 1 (PLK1).

Didrobaicalein is a PLK1 Inhibitor with an IC50 of 6.3 μM.

PMV6-PEG4-BI2536 is an RIPTAC-like bifunctional molecule that promotes the formation of the p53 Y 220C -PLK1 ternary complex ( EC 50 = 1.4 μM).

CZS-241 hydrochloride is an orally active and selective inhibitor of Polo-like Kinase 4 ( PLK4 ) ( IC 50 =2.6 nM).

8012-3246 is a selective PLK2 inhibitor with an IC 50 of 774.5 nM.

PROTAC PLK1 Degrader-2 is a peptide-based N-end rule PLK1 mini-PROTAC.

PI3K/PLK1 inhibitor

Non-ATP-competitive inhibitor of PLK1

NMS-1286937 is an orally active small-molecule compound. NMS-1286937 potently and selectively inhibits Polo-like kinase 1 (PLK1) activity with a half-maximal inhibitory concentration (IC 50 ) of 2nM.

polo-like kinase 1 （PLK) analogue