2. Cell Cycle/DNA Damage
  3. Polo-like Kinase (PLK)
  4. PLK1-IN-10

PLK1-IN-10 (Compound 4Bb) is an orally active PLK1 PBD (polo-box domain) inhibitor. PLK1-IN-10 blocks the interaction of PLK1 with the cell division regulator protein 1 (PRC1) and decreases the protein expression of the CDK1-Cyclin B1 complex. PLK1-IN-10 reacts with glutathione (GSH) to increase cellular oxidative stress, ultimately leading to cell death.

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CAS 番号 : 2991469-21-5

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PLK1-IN-10 関連抗体

Top Publications Citing Use of Products

    PLK1-IN-10 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2025 Jul 15;44(1):206.  [Abstract]

    Western blot analysis was used to detect the protein and phosphorylation levels of PRC1 in cells after treatment. H1299 cells were subcutaneously injected into nude mice to construct xenografts, followed by intratumoral injections (10 mg/kg: Bobcat339, HPPE, or PLK1-IN-10) starting from day 7.

    Polo-like Kinase (PLK) アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    PLK1 PLK2 PLK3 PLK4

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    • 純度とドキュメンテーション

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    製品説明

    PLK1-IN-10 (Compound 4Bb) is an orally active PLK1 PBD (polo-box domain) inhibitor. PLK1-IN-10 blocks the interaction of PLK1 with the cell division regulator protein 1 (PRC1) and decreases the protein expression of the CDK1-Cyclin B1 complex. PLK1-IN-10 reacts with glutathione (GSH) to increase cellular oxidative stress, ultimately leading to cell death[1].

    IC50 & Target

    PLK1 PBD

     

    Cellular Effect
    Cell Line Type Value Description References
    A549 IC50
    10.56 μM
    Compound: 4Bb
    Anticancer activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by crystal violet staining based analysis
    Anticancer activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by crystal violet staining based analysis
    		[PMID: 38657480]
    A549/CDDP IC50
    2.65 μM
    Compound: 4Bb
    Anticancer activity against human A549/DDP cells assessed as inhibition of cell growth incubated for 48 hrs by crystal violet staining based analysis
    Anticancer activity against human A549/DDP cells assessed as inhibition of cell growth incubated for 48 hrs by crystal violet staining based analysis
    		[PMID: 38657480]
    MCF7 IC50
    6.54 μM
    Compound: 4Bb
    Anticancer activity against human MCF7 cells assessed as inhibition of cell growth incubated for 48 hrs by crystal violet staining based analysis
    Anticancer activity against human MCF7 cells assessed as inhibition of cell growth incubated for 48 hrs by crystal violet staining based analysis
    		[PMID: 38657480]
    MGC-803 IC50
    3.2 μM
    Compound: 4Bb
    Anticancer activity against human MGC-803 cells assessed as inhibition of cell growth incubated for 48 hrs by crystal violet staining based analysis
    Anticancer activity against human MGC-803 cells assessed as inhibition of cell growth incubated for 48 hrs by crystal violet staining based analysis
    		[PMID: 38657480]
    NCI-H460 IC50
    2.31 μM
    Compound: 4Bb
    Anticancer activity against human NCI-H460 cells assessed as inhibition of cell growth incubated for 48 hrs by crystal violet staining based analysis
    Anticancer activity against human NCI-H460 cells assessed as inhibition of cell growth incubated for 48 hrs by crystal violet staining based analysis
    		[PMID: 38657480]
    SK-OV-3 IC50
    2.84 μM
    Compound: 4Bb
    Anticancer activity against human SK-OV-3 cells assessed as inhibition of cell growth incubated for 48 hrs by crystal violet staining based analysis
    Anticancer activity against human SK-OV-3 cells assessed as inhibition of cell growth incubated for 48 hrs by crystal violet staining based analysis
    		[PMID: 38657480]
    T-24 IC50
    2.9 μM
    Compound: 4Bb
    Anticancer activity against human T24 cells assessed as inhibition of cell growth incubated for 48 hrs by crystal violet staining based analysis
    Anticancer activity against human T24 cells assessed as inhibition of cell growth incubated for 48 hrs by crystal violet staining based analysis
    		[PMID: 38657480]
    体外実験

    PLK1-IN-10 (0-6 μM; 48 h) induces cell cycle arrest in the G2/M phase in A549 and A549/DDP cells, inhibiting cell proliferation[1].
    PLK1-IN-10 (20 μM) stabilizes PLK1 protein in A549/DDP cells across a range of temperatures[1].
    PLK1-IN-10 (5 μM; 24 h) reacts with GSH, producing a dose- and time-dependent fluorescent response, with higher fluorescence intensity in A549/DDP cells[1].
    PLK1-IN-10 (0-9 μM; 48 h) increases intracellular ROS levels in A549/DDP cells[1].
    PLK1-IN-10 (10 μM; 48 h) inhibits the interaction between PLK1 and PRC1, leading to the appearance of multinucleated cells[1].
    PLK1-IN-10 shows an anticancer activity of IC50=7.83 μM against NCI-H1975 cells[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    PLK1-IN-10 関連抗体

    Western Blot Analysis[1]

    Cell Line: A549, A549/DDP
    Concentration: 0, 1.5, 3, 6 μM
    Incubation Time: 48 h
    Result: Downregulated the expression of PLK1, CDK1, Cyclin B1, as well as significantly downregulated the expression of the CDK1-Cyclin B1 complex and Cdc25 protein.

    Cell Cycle Analysis[1]

    Cell Line: A549, A549/DDP
    Concentration: 0, 1.5, 3, 6 μM
    Incubation Time: 48 h
    Result: Significantly increased the number of A549 and A549/DDP cells in the G2/M phase, inducing mitotic catastrophe.
    体内実験

    PLK1-IN-10 (30, 50 mg/kg; i.p.; every two days for 32 days) significantly inhibits tumor growth in A549/DDP drug-resistant xenograft mice, with the 50 mg/kg group even causing tumor regression[1].
    PLK1-IN-10 (30 mg/kg; p.o.; every two days for 20 days) effectively inhibits tumor growth in NCI-H1975 drug-resistant xenograft mice[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: A549/DDP drug-resistant xenograft mice[1]
    Dosage: 30, 50 mg/kg
    Administration: i.p.; once every two days for 32 days
    Result: TGI reached 42% for the 30 mg/kg group and 62% for the 50 mg/kg group.
    Extended the median survival time from 38 days in the control group to 53 days in the 30 mg/kg group and 62 days in the 50 mg/kg group.
    Had no significant impact on the body weight and major organs of the mice, except for a slight difference in heart index observed in the 30 mg/kg group.
    Significantly reduced the number of Ki-67 positive cells in the tumor tissue.
    Showed no significant differences in H&E staining of major organs, further confirming its good biosafety.
    Animal Model: NCI-H1975 drug-resistant xenograft mice[1]
    Dosage: 30 mg/kg
    Administration: p.o.; once every two days for 20 days
    Result: TGI reached 44%. Caused no harm to the body weight and major organs of the mice.
    分子量

    455.50

    分子式

    C23H22FN3O4S
    CAS 番号
    SMILES

    CN(C)CCN(C1=O)C(C2=CC=C(S(NCC3=CC=C(F)C=C3)(=O)=O)C4=CC=CC1=C42)=O
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件

    Please store the product under the recommended conditions in the Certificate of Analysis.
    純度とドキュメンテーション
    参考文献
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    PLK1-IN-10 Related Classifications

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    Keywords:

    PLK1-IN-102991469-21-5Polo-like Kinase (PLK)Drug resistanceMitotic catastropheCell redox homeostasiscancerCell Cycle ArrestGSH DepletionOxidative Stress InducerMitotic CatastropheInhibitorinhibitorinhibit

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