2. Cell Cycle/DNA Damage PI3K/Akt/mTOR
  3. DNA-PK
  4. DNA-PK-IN-13

DNA-PK-IN-13 (Compound SK10) is a DNA-PK inhibitor that exhibits potent inhibitory activity (IC50= 0.11 nM). DNA-PK-IN-13 regulates tumor cell proliferation by decreasing the expression level of γH2A.X and enhancing the sensitivity of tumor cells to chemotherapeutic agents. DNA-PK-IN-13 is suitable for oncology studies.

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DNA-PK-IN-13 Chemical Structure

DNA-PK-IN-13 Chemical Structure

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DNA-PK-IN-13 Related Antibodies

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Description

DNA-PK-IN-13 (Compound SK10) is a DNA-PK inhibitor that exhibits potent inhibitory activity (IC50= 0.11 nM). DNA-PK-IN-13 regulates tumor cell proliferation by decreasing the expression level of γH2A.X and enhancing the sensitivity of tumor cells to chemotherapeutic agents. DNA-PK-IN-13 is suitable for oncology studies[1].

In Vitro

DNA-PK-IN-13 displays the best antiproliferative activities with IC50 values of 0.6 μM against Jurkat T-cell[1].
DNA-PK-IN-13 (0.1-40 μM; 10 min) concentration-dependently decreases the expression level of γH2A.X in Jurkat cells and HepG2 cells[1].
DNA-PK-IN-13 (1 μM; 24 hours) in combination with doxorubicin (HY-15142A) (0.1 μM) results in a significant decrease in the proportion of S-phase and an increase in the proportion of G2/M-phase in the Jurkat cell[1].

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

DNA-PK-IN-13 Related Antibodies

Western Blot Analysis[1]

Cell Line: HepG2 cells, Jurkat cells
Concentration: 0.1; 0.5; 5; 10; 20; 40μM
Incubation Time: 10min
Result: Concentration-dependently decreased the expression level of γH2A.X in Jurkat cells and HepG2 cells. DNA-PK-IN-13 can affect the production of γH2A.X and thus inhibit DNA damage repair.

Cell Cycle Analysis[1]

Cell Line: Jurkat cells
Concentration: 1μM; Dox 0.1μM
Incubation Time: 24h
Result: DNA-PK-IN-13 alone did not demonstrate statistically significant differences in the cell cycle. However, when combined with doxorubicin, DNA-PK-IN-13 influenced the cell cycle, contributing to cell death.
In Vivo

DNA-PK-IN-13 has good oral bioavailability (F = 31.8%)[1].


Pharmacokinetic Analysis in DNA-PK-IN-13[1]

Route Dose (mg/kg) AUC0-t (ug/L·h) AUC0−∞ (ug/L·h) t1/2 (h) Tmax (h) Cl (L/h/kg) Vz (L/kg) C0 (ug/L) Cmax (ug/L) F (%)
i.v. 2 604.4 ± 61.6 605.4 ± 61.9 1.0 ± 0.4 0.083 3.3 ± 0.3 4.7 ± 1.9 1003.9 ± 201.8 NA /
p.o. 10 949.5 ± 405.2 962.3 ± 412.1 2.0 ± 0.6 1.4 ± 1.1 12.6 ± 7.4 38.8 ± 30.2 NA 324.1 ± 149.0 31.8


DNA-PK-IN-13 (i.p.; 10 mg/kg; single dose) has tumor suppressor activity in CT26 colon cancer mice.Co-administration with doxorubicin (2.5 mg/kg) is effective and safe[1].
DNA-PK-IN-13 (i.p.; 10 mg/kg; 13 consecutive days) in combination with PD-1/PD-L1 inhibitors inhibits tumor growth more significantly[1].

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

Animal Model: CT26 colon cancer mouse [1]
Dosage: 10 mg/kg single dose
Administration: i.p
Result: Single-agent treatment reduced tumor weight by 30.8% and tumor volume by 32.1%.
Co-administration with doxorubicin (2.5 mg/kg) produced more significant tumor inhibitory activity, with a TGI of 50.2%. No significant weight loss or deaths were observed.
Molecular Weight

414.46

Formula

C22H22N8O
Unlabeled CAS

SMILES

CC(C(NC1=NC=C2C(N(CC3=NN=CN23)C4CCOCC4)=N1)=C5)=CC6=C5N=CC=C6
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-13 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-13DNA-PKDNA-dependent protein kinaseAntitumor activityImmunomodulatory effectsCancerCT26 colon cancer miceInhibitorinhibitorinhibit

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