| 产品描述： | DNA-PK 抑制剂;DNA-PK Inhibitors;;InformationYU238259 YU238259 is a novel inhibitor of homology-dependent DNA repair(HDR) , but does not inhibit non-homologous end-joining (NHEJ), in cell-based GFP reporter assays.TargetsHDRIn vitroYU238259 exhibits potent synthetic lethality in the setting of DNA damage response and DNA repair defects. Treatment with YU238259 is not only synergistic with ionizing radiation (IR), etoposide, and PARP inhibition, but this synergism is heightened by BRCA2-deficiency. Synthetic lethality of YU238259 in HDR-deficient cells results from accumulation of unresolved DSBs following additional inhibition of residual HDR pathway activity. Inhibition of HDR activity by YU238259 has little to no effect on the NHEJ pathway. YU238259 sensitizes tumor cells to radiation therapy and DSB-inducing chemotherapy .In vivoGrowth of BRCA2-deficient human tumor xenografts in nude mice is significantly delayed by YU238259 treatment even in the absence of concomitant DNA-damaging therapy.Cell Research(from reference)Cell lines：U2OS cells Concentrations：25 μM Incubation Time：1 h |
| 靶点： |
HDR |
| 体内研究： |
YU238259 (3 mg/kg，腹腔注射) 抑制裸鼠体内 BRCA2 缺陷肿瘤异种移植物的生长。 |
| 参考文献： |
1. Stachelek GC, et al. YU238259 Is a Novel Inhibitor of Homology-Dependent DNA Repair That Exhibits Synthetic Lethality and Radiosensitization in Repair-Deficient Tumors. Mol Cancer Res. 2015 Oct;13(10):1389-97. |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.174 ml |
10.871 ml |
21.741 ml |
| 5 mM |
0.435 ml |
2.174 ml |
4.348 ml |
| 10 mM |
0.217 ml |
1.087 ml |
2.174 ml |
| 50 mM |
0.043 ml |
0.217 ml |
0.435 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京