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Cat. No.: HY-161521

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PLK1-IN-10

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Based on 1 publication(s) in Google Scholar

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.

CAS No.: 2991469-21-5
Formula: C₂₃H₂₂FN₃O₄S
Molecular Weight:455.50

Storage:

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

Data Sheet (272 KB)

PLK1-IN-10 Chemical Structure

CAS No.: 2991469-21-5

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

PLK1 PBD

All Polo-like Kinase (PLK) Isoforms :

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]

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.

Chemical Information

CAS No. 2991469-21-5
Molecular Weight 455.50
Formula C₂₃H₂₂FN₃O₄S
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.

Publications (1)

All In Vivo Efficacy Study

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Journal Impact Factor

J Exp Clin Cancer Res

CCNY-mediated phosphorylation and TET2-BACH1-driven DNA demethylation activate PRC1 to augment NSCLC progression. [Abstract]

2025 Jul 15;44(1):206. PMID: 40665337

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

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. Volume of xenograft tumors by week.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
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]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Purity & Documentation
References

1/16
1/16

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

Customer Validation
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. Volume of xenograft tumors by week.

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PLK1-IN-10

Publications Citing Use of MedChemExpress (MCE) PLK1-IN-10

All Polo-like Kinase (PLK) Isoforms