| 产品描述: | 强效泛RSK抑制剂;Potent pan-RSK inhibitor;产品介绍:LJI308 是一种有效的泛 RSK 抑制剂,对 RSK1、RSK2 和 RSK3 的 IC50 分别为 6 nM、4 nM 和 13 nM。LJI308 抑制辐照、EGF 处理和 表达 KRAS 突变的细胞中 RSK (T359/S363) 和 YB-1 (S102) 的磷酸化。;Product Application:LJI308 is a potent pan-ribosomal S6 kinase (RSK) inhibitor, with IC50s of 6 nM, 4 nM, and 13 nM for RSK1, RSK2, and RSK3, respectively. LJI308 inhibits the phosphorylation of RSK (T359/S363) and YB-1 (S102) after irradiation, treatment with EGF, and in cells expressing a KRAS mutation |
| 参考文献: |
1. Aronchik I, et al. Novel potent and selective inhibitors of p90 ribosomal S6 kinase reveal the heterogeneity of RSK function in MAPK-driven cancers. Mol Cancer Res. 2014 May;12(5):803-12. 2. Lettau K, et al. Simultaneous Targeting of RSK and AKT Efficiently Inhibits YB-1-Mediated Repair of Ionizing Radiation-Induced DNA Double-Strand Breaks in Breast Cancer Cells. Int J Radiat Oncol Biol Phys. 2021;109(2):567-580. 3. Davies AH, et al. Inhibition of RSK with the novel small-molecule inhibitor LJI308 overcomes chemoresistance by eliminating cancer stem cells. Oncotarget. 2015;6(24):20570-20577. 4. Jain R, et al. Discovery of Potent and Selective RSK Inhibitors as Biological Probes. J Med Chem. 2015 Sep 10;58(17):6766-83. |
| 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 |
2.715 ml |
13.573 ml |
27.146 ml |
| 5 mM |
0.543 ml |
2.715 ml |
5.429 ml |
| 10 mM |
0.271 ml |
1.357 ml |
2.715 ml |
| 50 mM |
0.054 ml |
0.271 ml |
0.543 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。 |