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

DNA-PK-IN-13 (Compound SK10) 是 DNA-PK 抑制剂，表现出极强的抑制活性 (IC50= 0.11 nM)。DNA-PK-IN-13 通过降低 γH2A.X 的表达水平和增强肿瘤细胞对化疗药物的敏感性，调节肿瘤细胞的增殖。DNA-PK-IN-13 具适用于肿瘤学研究。

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DNA-PK-IN-13 Chemical Structure

DNA-PK-IN-13 Chemical Structure

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DNA-PK-IN-13 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(In Vitro)

DNA-PK-IN-13 在 Jurkat (T lymphoma) 细胞中，表现出最佳的抗增殖活性 IC50 = 0.6 μM[1]。
DNA-PK-IN-13 (0.1-40 μM; 10 分钟) 浓度依赖性地降低 Jurkat 细胞和 HepG2 细胞 γH2A.X 的表达水平[1]。
DNA-PK-IN-13 (1 μM; 24 小时) 与 doxorubicin (HY-15142A) (0.1 μM) 组合后 Jurkat 细胞周期的 S 期比例显着降低，G2/M 期比例增加[1]。

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

DNA-PK-IN-13 相关抗体:

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.
体内研究
(In Vivo)

DNA-PK-IN-13 拥有良好的口服生物利用度 (F = 31.8%)[1]。


药代动力学分析[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.; 10mg/kg; 单剂量) 在 CT26 结肠癌小鼠中显示出肿瘤抑制活性。和 doxorubicin (2.5 mg/kg) 联合给药是有效和安全的[1]。
DNA-PK-IN-13 (i.p.; 10mg/kg; 连续13天) 和 PD-1/PD-L1 抑制剂联合用药抑制肿瘤生长更显著[1]。

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.
分子量

414.46

Formula

C22H22N8O
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

DNA-PK-IN-13 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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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