ZM223 hydrochloride is an orally active, potent non-covalent NEDD8 activating enzyme (NAE) inhibitor with excellent anticancer activity.
IC50&Target
NEDD8 activating enzyme (NAE)
体外研究
ZM223 hydrochloride (0.1-1 μM; 4 hours) inhibits both HCT-116 and U-2OS cancer cells with IC50s of 100 and 122 nM, respectively.
ZM223 hydrochloride (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.
运输条件
Room temperature in continental US; may vary elsewhere.