ZM223 hydrochloride is an orally active, potent non-covalent NEDD8 activating enzyme (NAE) inhibitor with excellent anticancer activity[1].
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[1].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[1]. Cell Viability Assay[1] Cell Line: HCT116 colon cancer cells and U-2OS osteosarcoma cells
[1]. Ma H, et al. Discovery of benzothiazole derivatives as novel non-sulfamide NEDD8 activating enzyme inhibitors by target-based virtual screening. Eur J Med Chem. 2017 Jun 16;133:174-183.