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PLK

Polo-like kinase (PLK) is a highly conserved serine/threonine protein kinase with a highly homologous serine/threonine kinase domain at its N-terminus, which regulates PLK activity and subcellular dynamics at the C-terminus and targeted polo-box domain (PBD). There are many PLK family members, and there are four subtypes in the human body, namely PLK1, PLK2, PLK3, and PLK4, which play important roles in the regulation of various phases of the cell cycle.

  • Onvansertib
    T62471034616-18-6
    Onvansertib (NMS-1286937) is a PLK1 inhibitor (IC50=2 nM) with high selectivity and oral activity. Onvansertib has antitumor activity and inhibits tumor growth.
    • $30
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  • Ocifisertib(CFI-400945 free base)
    T73841338806-73-7
    Ocifisertib (CFI-400945 free base) is a potent, selective and orally active inhibitor of polo-like kinase 4 (PLK4; Ki value 0.26 nM; IC50 value 2.8 nM).
    • $38
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  • Wortmannin
    T628319545-26-7
    Wortmannin (SL-2052) is a PI3K inhibitor (IC50=3 nM) that is covalent and irreversible. Wortmannin is also an inhibitor of PlK1 and PlK3 (IC50=5.8 48 nM) that blocks autophagy.
    • $32
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    TargetMol | Citations Cited
  • Volasertib
    T6019755038-65-4
    Volasertib (BI 6727) (BI-6727) is a potent inhibitor of PLK1 (IC50: 0.87 nM), inducing mitotic arrest and apoptosis. It also inhibits PLK2 PLK3 (IC50s: 5 56 nM).
    • $39
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  • GSK461364
    T6282929095-18-1
    GSK461364 (GSK461364A)(Ki=2.2 nM) inhibits purified Plk1 .The specificity of GSK461364 for Plk1 is more than 1000-fold over Plk2 3.
    • $31
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  • BI 2536
    T6173755038-02-9
    BI2536 is an effective Plk1 inhibitor (IC50: 0.83 nM). It has 4- and 11-fold greater selectivity than Plk2 and Plk3.
    • $38
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  • Poloxin-2
    T25969321695-37-8In house
    Poloxin-2 is a potent and selective Plk1 PBD inhibitor with anti-tumour activity that reduces the protein level of Plk1 in HeLa cells.
    • $350
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  • Dihydrobaicalein
    TN384835683-17-1
    Dihydrobaicalein is a natural product from Scutellaria baicalensis, a PLK1 inhibitor (IC50:6.3 μM).Dihydrobaicalein inhibits VRK2 and PLK2.
    • $195
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  • Rigosertib
    T16750592542-59-1
    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.
    • $34
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  • Plogosertib
    T713991137212-79-3In house
    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.
    • $228 TargetMol
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  • Mps1-IN-2
    T18391228817-38-6
    Mps1-IN-2 is a potent, selective, and ATP-competitive inhibitor of both Mps1 and Plk1.
    • $34
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  • Ro3280
    T26341062243-51-9
    Ro3280 (Ro5203280) is an effective, specific inhibitor of PLK1(IC50=3, Kd=0.09 nM).
    • $55
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  • Pyridoxine
    T097365-23-6
    Pyridoxine (Vitamin B6) is the 4-methanol form of vitamin B6 and is converted to pyridoxal 5-phosphate in the body. Although pyridoxine and vitamin B6 are still frequently used as synonyms, especially by medical researchers, this practice is erroneous and sometimes misleading.
    • $39
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  • Centrinone
    T149271798871-30-3
    Centrinone (LCR-263) (LCR-263) is a reversible inhibitor of polo-like kinase 4 (PLK4; Ki:0.16 nM).
    • $56
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  • MLN0905
    T27041228960-69-7
    MLN0905 (PLK1 Inhibitor) is an effective PLK1 inhibitor(IC50=2 nM).
    • $33
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  • TAK-960
    T72001137868-52-0
    TAK-960 is an orally bioavailable, selective inhibitor of Plks with IC50 values of 0.8, 16.9, and 50.2 nM for Plk1, Plk2, and Plk3, respectively.
    • $58
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  • HMN-214
    T2438173529-46-9
    HMN-214 (IVX-214) is a potent PLK1 inhibitor with an average IC50 of 0.12 μM.
    • $34
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  • Cyclapolin 9
    T2270040533-25-3
    Cyclapolin 9 is a selective, potent, and ATP-competitive inhibitor of polo-like kinase 1 (PLK1) with an IC50 of 500 nM, and has not shown activity against other kinases.
    • $93
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  • (E/Z)-Rigosertib sodium
    T60701225497-78-8
    ON-01910 is a non-ATP-competitive PLK1 inhibitor(IC50 of 9 nM, in a cell-free assay). It shows 30-fold greater selectivity against Plk2 and no activity to Plk3. Rigosertib inhibits PI3K Akt pathway and activates oxidative stress signals. Rigosertib induces apoptosis in various cancer cells.It is a synthetic benzyl styryl sulfone analogue with potential antineoplastic activity.
    • $34
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  • AAPK-25
    T102152247919-28-2
    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.
    • $52
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  • PHA-680632
    T6338398493-79-3
    PHA-680632 is potent inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 27 nM, 135 nM and 120 nM, respectively. It has 10- to 200-fold higher IC50 for FGFR1, FLT3, LCK, PLK1, STLK2, and VEGFR2 3.
    • $39
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  • GW843682X
    T15454660868-91-7
    GW843682X (GW843682) is a selective and ATP-competitive inhibitor of PLK1 and PLK3 (IC50s = 2.2 nM and 9.1 nM).
    • $32
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  • Centrinone-B
    T149261798871-31-4In house
    Centrinone-B (LCR-323) is a potent and highly selective PLK4 inhibitor with a Ki of 0.59 nM.
    • $199
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  • HMN-176
    T3643173529-10-7
    HMN-176 is a stilbene derivative which inhibits mitosis, interfering with polo-like kinase-1 (plk1).
    • $29
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  • (1E)-CFI-400437 dihydrochloride
    T222881247000-76-5
    (1E)-CFI-400437 dihydrochloride (CFI-400437 dihydrochloride) is a selective and potent polo-like kinase 4 (PLK4) inhibitor.
    • $80
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  • Poloxin
    T16560321688-88-4
    Poloxin is a non-ATP competitive Polo-like Kinase 1 inhibitor targeting the polo-box domain (IC50: appr 4.8 μM).
    • $29
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  • TC-S 7005
    T170081082739-92-1
    TC-S 7005 is an effective inhibitor of Polo-like kinases (IC50s: 214 nM, 4 nM and 24 nM for Plk1, Plk2, and Plk3).
    • $52
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  • 5-ETHYL-4,5,6,7-TETRAHYDRO-THIAZOLO[5,4-C]PYRIDIN-2-YLAMINE
    T891217899-49-9
    5-ETHYL-4,5,6,7-TETRAHYDRO-THIAZOLO[5,4-C]PYRIDIN-2-YLAMINE targets PLK1.
    • $51
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  • 3MB-PP1
    T21678956025-83-5In house
    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.
    • $48
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  • ON1231320
    T196641312471-39-8
    ON1231320 (GBO-006) is a Polo-like kinase 2 (PLK2) inhibitor.
    • $34
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  • T521
    T28904891020-54-5In house
    T521 is a selective inhibitor of the PBD of Plk1 and shows no inhibitory effect on Plk2 and Plk3.
    • $410
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  • LFM-A13
    T6217244240-24-2
    LFM-A13(IC50=2.5 μM), a specific Bruton's tyrosine kinase (BTK), is more than 100-fold specificity than other protein kinases, such as JAK1, JAK2, HCK, EGFR, and IRK.
    • $30
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  • Rigosertib sodium
    T5818592542-60-4
    Rigosertib sodium (ON-01910), a non-ATP-competitive inhibitor of PLK1(IC50=9 nM), exhibits 30-fold higher specificity activity over Plk2 and no effect on Plk3.
    • $33
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  • SBE13 Hydrochloride
    T22711052532-15-6
    SBE13 Hydrochloride (SBE 13 HCl) is an effective and specific PLK1 inhibitor (IC50: 0.2 nM); no inhibition om Aurora A kinase, Plk2/3.
    • $29
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  • 7-O-Prenylscopoletin
    TN324713544-37-1
    7-O-Prenylscopoletin and cedrelopsin show high antiproliferative activities against cancer cell lines.
    • $440
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  • Poloxime
    T1655917302-61-3
    Poloxime is a hydrolysis product of poloxin and is a non-ATP-competitive Plk1 inhibitor. It also has moderate Plk1 inhibitory activity.
    • $39
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