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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; | ||
SMILES | O=C([C@@H](NC([C@H]([C@@H](C)O)NC([C@@H](NC([C@H]([C@@H](C)CC)N(C)C(C)=O)=O)[C@@H](C)CC)=O)=O)CC(C)C)[C@@]1(C)CO1 | ||
化学名称 | |||
分子式 | C28H50N4O7 | 分子量 | 554.72 |
纯度 | 98% | 配送 | 惯例下常温包邮 |
产品描述 | 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. |
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