| 产品描述: | USP/UBP 选择性抑制剂;USP/UBP Selective Inhibitors;;InformationML364 is a small molecule inhibitor of thedeubiquitinase USP2with an IC50 of 1.1 μM in a biochemical assay using an internally quenched fluorescent di-ubiquitin substrate.TargetsUSP8 (Cell-free assay); USP2 (Cell-free assay) 0.95 μM; 1.1 μMIn vitroML364 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.Cell Research(from reference)Cell lines:LnCAP cells and MCF7 cells Concentrations:0-20 μM Incubation Time:24 h |
| 靶点: |
IC50: 1.1 μM (USP2);Kd: 5.2 μM (USP2) |
| 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 Nov 18;291(47):24628-24640. 2. Hashimoto M, et al. Inhibition of ubiquitin-specific protease 2 causes accumulation of reactive oxygen species, mitochondria dysfunction, and intracellular ATP decrement in C2C12 myoblasts. Physiol Rep. 2019 Jul;7(14):e14193. |
| 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 |
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: |
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