2. Cell Cycle/DNA Damage PI3K/Akt/mTOR Apoptosis
  3. DNA-PK Apoptosis
  4. 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.

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DNA-PK-IN-16

DNA-PK-IN-16 Chemical Structure

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DNA-PK-IN-16 Related Antibodies

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Description

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[1].

In Vitro

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.

DNA-PK-IN-16 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: LoVo, B16-F10, Jurkat, HL-60, MDA-MB-436, MDA-MB-231 cancer cell lines
Concentration: /
Incubation Time: 48 h
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).

Cell Cycle Analysis[1]

Cell Line: LoVo cells
Concentration: 1, 5, 10 μM
Incubation Time: 24 h
Result: Dose-dependently decreased the proportion of cells in the G2/M phase and increased the proportion of cells in the S phase.
Parmacokinetics
Species Dose Route AUC0-t AUC0-∞ T1/2 CL C0 Cmax Bioavailability
Rat[1] 2 mg/kg i.v. 1198.4 μg/L·h 2084.8 μg/L·h 36.1 h 1.2 L/h/kg 625.3 μg/L / /
Rat[1] 20 mg/kg p.o. 8398.4 μg/L·h 8898.4 μg/L·h 50.0 h 8.8 L/h/kg / 1404.3 μg/L 42.6 %
In Vivo

DNA-PK-IN-16 (25-50 mg/kg; p.o.; once daily; 15 days) dose-dependently inhibits the growth of LoVo colorectal cancer xenografts[1].
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.

Animal Model: BALB/c nude (male, 6-8 weeks old, subcutaneously inoculated with LoVo cells)[1]
Dosage: 25 mg/kg; 50 mg/kg
Administration: i.g.; once daily; 15 days
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.
Molecular Weight

456.54

Formula

C25H28N8O
SMILES

C1(C2=CN=C(N=C2)N3CCNCC3)=CC=C(C4=C1)N=CC5=C4N(C6CCOCC6)C7=NCCN57
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
References
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DNA-PK-IN-16 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:

DNA-PK-IN-16DNA-PKApoptosisDNA-dependent protein kinasecancer cell linesSprague-Dawley ratstumor tissueanti-PD-L1 monoclonal antibodyDNA double-strand breaksCD8+ T-cellγH2A.XLoVo cellsInhibitorinhibitorinhibit

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