| S7837 |
Centrinone (LCR-263)
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Centrinone (LCR-263) is a selective and reversible polo-like kinase 4 (PLK4) inhibitor with Ki of 0.16 nM.
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Leukemia, 2025, 10.1038/s41375-025-02729-w
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Arch Biochem Biophys, 2025, 768:110383
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| S5893 |
Poloxin
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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.
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Nat Commun, 2023, 14(1):355
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| S8342 |
ON1231320
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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.
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Cell Rep, 2024, 43(8):114510
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| S1239 |
TAK-960
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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).
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| S2880 |
GW843682X
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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.
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| S5807 |
HMN-176
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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.
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| E8058 |
TC-S 7005
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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.
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| S2758 |
Wortmannin (SL-2052)
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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.
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Nat Commun, 2025, 16(1):1313
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EMBO J, 2025, 10.1038/s44318-025-00507-z
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EMBO Mol Med, 2025, 10.1038/s44321-025-00222-6
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