DNA-PK-IN-16
DNA-PK-IN-16 is an orally active DNA-dependent protein kinase (DNA-PK) inhibitor with an IC50 of 10.2 nM. DNA-PK-IN-16 induces the upregulation of γH2A.X, a biomarker of DNA double-strand breaks. DNA-PK-IN-16 exhibits antiproliferative activity in various cancer cell lines. DNA-PK-IN-16 enhances the infiltration of CD8+ T cells in tumor tissues through synergistic action with anti-PD-L1 monoclonal antibody. DNA-PK-IN-16 is applicable for cancer research.
For research use only. We do not sell to patients.
- Formula: C25H28N8O
- Molecular Weight:456.54
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
DNA-PK-IN-16 (compound D11) (48 h) potently inhibits the proliferation of LoVo, B16-F10, Jurkat, HL-60, MDA-MB-436 and MDA-MB-231 cancer cells, with IC50 values ranging from 1.6 to 6.9 μM[1].
DNA-PK-IN-16 (1-10 μM; 24 h) upregulates the expression of γH2A.X in a concentration-dependent manner in Bleomycin (HY-108345)-treated LoVo cells, indicating impaired DNA damage repair function[1].
DNA-PK-IN-16 (1-10 μM; 24 h) dose-dependently induces apoptosis in LoVo cells, reduces mitochondrial membrane potential, disrupts cell cycle progression, and inhibits cell migration[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LoVo, B16-F10, Jurkat, HL-60, MDA-MB-436, MDA-MB-231 cancer cell lines
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Concentration:/
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Incubation Time:48 h
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Result:Exhibited robust antiproliferative activity across all six cell lines, with IC50 values of 1.6 μM (LoVo), 5.3 μM (B16-F10), 1.9 μM (Jurkat), 2.1 μM (HL-60), 3.6 μM (MDA-MB-436), and 6.9 μM (MDA-MB-231).
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Cell Line:LoVo cells
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Concentration:1, 5, 10 μM
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Incubation Time:24 h
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Result:Dose-dependently decreased the proportion of cells in the G2/M phase and increased the proportion of cells in the S phase.
DNA-PK-IN-16 (50 mg/kg; p.o.; once daily) inhibits the growth of B16-F10 melanoma (49.2% TGI), and also synergizes with anti-PD-L1 monoclonal antibody to enhance antitumor efficacy by increasing CD8+ T cell infiltration (69.6% TGI), while maintaining favorable safety profiles[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (male, 6-8 weeks old, subcutaneously inoculated with LoVo cells)[1]
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Dosage:25 mg/kg; 50 mg/kg
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Administration:i.g.; once daily; 15 days
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Result:Achieved a tumor growth inhibition (TGI) rate of 30.1% at 25 mg/kg.
Achieved a TGI rate of 72.9% at 50 mg/kg.
Downregulated Ki-67 and PCNA (cell proliferation markers) in a dose-dependent manner.
Upregulated TUNEL-positive apoptotic cells in a dose-dependent manner.
Enhanced γH2A.X signals (a marker of DNA double-strand breaks) in tumor tissues in a dose-dependent manner.
Caused no significant body weight loss or reduced food intake in mice during treatment.
Chemical Information
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Molecular Weight 456.54
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Formula C25H28N8O
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SMILES
C1(C2=CN=C(N=C2)N3CCNCC3)=CC=C(C4=C1)N=CC5=C4N(C6CCOCC6)C7=NCCN57
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
DNA-PK-IN-16 Related Classifications
HY-181848 Related Classifications
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