PLK1-IN-10

Cat. No.: HY-161521: FAQs
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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.

For research use only. We do not sell to patients.

PLK1-IN-10 Chemical Structure

CAS No. : 2991469-21-5

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PLK1 PLK2 PLK3 PLK4

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

PLK1 PBD

In Vitro

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.

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.

In Vivo

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.

Molecular Weight

455.50

Formula

C₂₃H₂₂FN₃O₄S

CAS No.

2991469-21-5

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Li P, Li Y, et al. Identification of naphthalimide-derivatives as novel PBD-targeted polo-like kinase 1 inhibitors with efficacy in drug-resistant lung cancer cells. Eur J Med Chem. 2024 May 5;271:116416. [Content Brief]

PLK1-IN-10 Related Classifications

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

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

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