Bioactivity | 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]. |
Invitro | 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. 0 --> DNA-PK-IN-13 相关抗体: Western Blot Analysis[1] Cell Line: |
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 |
Formula | C22H22N8O |
Molar Mass | 414.46 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Cheng B, Y et al. Discovery of Novel Heterotricyclic Compounds as DNA-Dependent Protein Kinase (DNA-PK) Inhibitors with Enhanced Chemosensitivity, Oral Bioavailability, and the Ability to Potentiate Cancer Immunotherapy. J Med Chem. 2024 Apr 25;67(8):6253-6267 |