ZM223 hydrochloride 是一种有效的非共价 NEDD8 活化酶 (NAE) 抑制剂,具有口服活性。
产品描述
ZM223 hydrochloride is an orally active, potent non-covalent NEDD8 activating enzyme ( NAE ) inhibitor with excellent anticancer activity [1].
体外活性
ZM223 hydrochloride (0.1-1 μM; 4 hours) inhibits both HCT-116 and U-2OS cancer cells with IC 50 s 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 Concentration: 0.1 μM, 1 μM Incubation Time: 4 hours Result: Inhibited both HCT-116 and U-2OS cancer cells. Western Blot Analysis [1] 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.
分子式
C23H18ClF3N4O2S2
分子量
538.99
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years