产品描述: | ZM223 is a potent non-covalent NEDD8 activating enzyme (NAE) inhibitor, orally active |
靶点: |
NEDD8 activating enzyme (NAE);SerineProtease |
体外研究: |
ZM223 (0.1-1 μM; 4 hours) inhibits both HCT-116 and U-2OS cancer cells with IC50s of 100 and 122 nM, respectively. ZM223 (0.1-1 μM; 4 hours) causes a dose-response decrease in the level of NEDD8 and accumulation of the UBC12 protein, indicating the decrease of the subsequent NEDD8-UBC12 complex. Cell Viability Assay Cell Line: HCT116 colon cancer cells and U-2OS osteosarcoma cells Concentration: 0.1 μM, 1 μM Incubation Time: 4 hours Result: Inhibited both HCT-116 and U-2OS cancer cells. Western Blot Analysis Cell Line: HCT116 colon cancer cells Concentration: 0.1 μM, 1 μM Incubation Time: 4 hours Result: Caused a decrease in the level of NEDD8 and an increase in the downstream UBC12 protein. |
参考文献: |
1. Ma H, Zhuang C, Xu X, et al. Discovery of benzothiazole derivatives as novel non-sulfamide NEDD8 activating enzyme inhibitors by target-based virtual screening. Eur J Med Chem. 2017;133:174-183. doi:10.1016/j.ejmech.2017.03.076 |
溶解性: |
Soluble in DMSO |
保存条件: |
-20°C |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
1.99 ml |
9.95 ml |
19.899 ml |
5 mM |
0.398 ml |
1.99 ml |
3.98 ml |
10 mM |
0.199 ml |
0.995 ml |
1.99 ml |
50 mM |
0.04 ml |
0.199 ml |
0.398 ml |
|
注意: |
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