2. Cell Cycle/DNA Damage PI3K/Akt/mTOR Apoptosis
  3. DNA-PK Apoptosis
  4. DNA-PK-IN-16

DNA-PK-IN-16 是一种具有口服活性的 DNA 依赖性蛋白激酶 (DNA-PK) 抑制剂。 IC50 为 10.2 nM。DNA-PK-IN-16 可诱导 DNA 双链断裂生物标志物 γH2A.X 的上调。DNA-PK-IN-16 在多种癌细胞系中均表现出抗增殖活性。DNA-PK-IN-16 可通过与抗 PD-L1 单克隆抗体协同作用，增强肿瘤组织中 CD8+ T 细胞的浸润。DNA-PK-IN-16 可用于癌症研究。

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DNA-PK-IN-16

DNA-PK-IN-16 Chemical Structure

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DNA-PK-IN-16 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-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].

体外研究
(In Vitro)

DNA-PK-IN-16 (compound D11) (48 h) 可强效抑制 LoVo、B16-F10、Jurkat、HL-60、MDA-MB-436 及 MDA-MB-231 癌细胞的增殖，IC50 值为 1.6 至 6.9 μM[1]。
DNA-PK-IN-16 (1-10 μM; 24 h) 可在 Bleomycin (HY-108345) 处理的 LoVo 细胞中，浓度依赖性地上调 γH2A.X 的表达，表明 DNA 损伤修复功能受损[1]。
DNA-PK-IN-16 (1-10 μM; 24 h) 可呈剂量依赖性诱导 LoVo 细胞凋亡，降低细胞线粒体膜电位，破坏细胞周期进程和抑制细胞迁移[1]。

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

DNA-PK-IN-16 相关抗体:

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.
药代动力学
(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 %
体内研究
(In Vivo)

DNA-PK-IN-16 (25-50 mg/kg；灌胃；每日 1 次; 15 天) 可剂量依赖性地抑制 LoVo 结直肠癌异种移植物的生长[1]。
DNA-PK-IN-16 (50 mg/kg；灌胃；每日 1 次) 单药使用可抑制 B16-F10 黑色素瘤的生长 (49.2% TGI)，还可与抗 PD-L1 单克隆抗体协同作用，通过增加 CD8+ T 细胞浸润来增强抗肿瘤效力 (69.6% TGI )，同时维持良好的安全性特征[1]。

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.
分子量

456.54

Formula

C25H28N8O
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-16 相关分类

  • 摩尔计算器

  • 稀释计算器

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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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目录号：
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