PLK Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
S7837 Centrinone (LCR-263) Centrinone (LCR-263) is a selective and reversible polo-like kinase 4 (PLK4) inhibitor with Ki of 0.16 nM.
Leukemia, 2025, 10.1038/s41375-025-02729-w
Arch Biochem Biophys, 2025, 768:110383
S5893 Poloxin Poloxin is a non-ATP competitive Polo-like Kinase 1 polo-box domain (Plk1 PBD) inhibitor with an apparent IC50 of 4.8 μM. This compound's IC50 values against the PBDs of Plk2 and Plk3 as Plk1 are approximately 4-fold and 11-fold higher, respectively in fluorescence polarization assays.
Nat Commun, 2023, 14(1):355
S8342 ON1231320 ON1231320 (7ao), an arylsulfonyl pyrido-pyrimidinone, is a highly specific inhibitor of polo like kinase 2 (PLK2). It also blocks tumor cell cycle progression in the G2/M phase in mitosis and causes apoptosis.
Cell Rep, 2024, 43(8):114510
S1239 TAK-960 TAK-960 is a novel, investigational, orally bioavailable, potent, and selective PLK1 inhibitor that has shown activity in several tumor cell lines, including those that express multidrug-resistant protein 1 (MDR1).
S2880 GW843682X GW843682X is a selective, ATP-competitive inhibitor of PLK1 and PLK3, with IC50s of 2.2 nM and 9.1 nM, respectively, and is also >100-fold selective against ~30 other kinases.
S5807 HMN-176 HMN-176 is an active metabolite of HMN-214, which has a potent antitumor activity in mouse xenograft models. This compound effectively inhibits PLK-1 by interference with its normal subcellular spatial distribution at centrosomes and along the cytoskeletal structure.
E8058 TC-S 7005 TC-S 7005 is an inhibitor of Polo-like kinase (Plk) with IC50 of 4 nM for Plk2, 24 nM for Plk3, and 214 nM for Plk1.
S2758 Wortmannin (SL-2052) Wortmannin is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. Wortmannin blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays. Wortmannin also inhibits PLK1 activity.
Nat Commun, 2025, 16(1):1313
EMBO J, 2025, 10.1038/s44318-025-00507-z
EMBO Mol Med, 2025, 10.1038/s44321-025-00222-6
Verified customer review of Wortmannin (SL-2052)