| 产品描述： | ML364是去泛素化酶USP2的小分子抑制剂，IC50为1.1 μM（以含内部淬灭荧光双泛素为底物） |
| 靶点： |
USP8(Cell-free assay):0.95 μM; USP2(Cell-free assay):1.1 μM;DUB |
| 体外研究： |
ML364 induces an increase in cellular cyclin D1 degradation and causes cell cycle arrest in Mino and HCT116 cancer cell lines. ML364 is antiproliferative in cancer cell lines. ML364 also causes a decrease in homologous recombination-mediated DNA repair. It is inactive against caspase 6, caspase 7, MMP1, MMP9, and USP15, but does inhibit USP8 with an IC50 of 0.95 μM. In a panel of 102 kinases that included regulators of the cell cycle there is no binding observed to any of the enzymes tested using 10 μM ML364. |
| 细胞实验： |
Cell lines: LnCAP cells and MCF7 cells Concentrations: 0-20 μM Incubation Time: 24 h Method: ML364 promotes degradation of cyclin D1 in LnCAP cells and MCF7 cells. Cells are treated with ML364 for 24 h, and cyclin D1 protein levels are assessed by Western blotting using a tubulin control. |
| 参考文献： |
1. Davis MI, et al. Small Molecule Inhibition of the Ubiquitin-specific Protease USP2 Accelerates cyclin D1 Degradation and Leads to Cell Cycle Arrest in Colorectal Cancer and Mantle Cell Lymphoma Models. J Biol Chem. 2016, 291(47):24628-24640.. |
| 溶解性： |
Soluble in DMSO、Ethanol |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
1.932 ml |
9.661 ml |
19.322 ml |
| 5 mM |
0.386 ml |
1.932 ml |
3.864 ml |
| 10 mM |
0.193 ml |
0.966 ml |
1.932 ml |
| 50 mM |
0.039 ml |
0.193 ml |
0.386 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