艾泼米辛
| CAS号 | 134381-21-8 | 货号 | BCP13740 |
| 中文名 | 艾泼米辛 | ||
| 英文名 | Epoxomicin | ||
| 中文别名 | 埃泼米辛; | ||
| 英文别名 | BU-4061T; | ||
| 分子式 | C28H50N4O7 | 分子量 | 554.72 |
| 生物活性 | Epoxomicin is a potent anti-tumor agent isolated from Actinomycetes that is used as a selective and irreversible inhibitor of the 20S proteasome. It inhibits proteasome activity in cell growth assays with an IC50 value of 4 nM and demonstrates potent cytotoxicity against B16-F10, HCT116, and Moser solid tumor cells, as well as P388 and K562 leukemia cells with IC50 values ranging from 2-44 nM. By inhibiting osteoblast proteasome activity, epoxomicin stimulates bone formation at concentrations as low as 10 nM. Intraperitoneal injection of 1.5 mg/kg epoxomicin given daily for two weeks induces Parkinson's-like symptoms in rats and addition of 100 nM epoxomicin to rat ventral midbrain cultures results in apoptosis specific to dopaminergic neurons. Epoxomicin-induced parkinsonism can be a useful model to examine mechanisms and therapies for the disease. | ||
| 信号通路 | Protease/Metabolic Enzyme | ||
| 靶 点 | Proteasome | ||
结构式
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