Epoxomicin (BU-4061T) is a potent anti-tumor agent isolated from Actinomycetes that is used as a selective and irreversible inhibitor of the 20S proteasome.
信号通路
Metabolism; Proteases
靶点
20S proteasome
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IC50
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体外研究
Epoxomicin inhibits proteasome activity in cell growth assays with an IC50 value of 4nM 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 2-44nM. By inhibiting osteoblast proteasome activity, epoxomicin stimulates bone formation at concentrations as low as 10nM.
体内研究
Intraperitoneal injection of 1.5mg/kg epoxomicin given daily for two weeks induces Parkinson's-like symptoms in rats and addition of 100nM epoxomicin to rat ventral midbrain cultures results in apoptosis specific to dopaminergic neurons.
临床实验
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特征
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相关实验数据(此数据来自于公开文献,联迈生物并不保证其有效性):
酶活性检测实验
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细胞实验
细胞系
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浓度
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处理时间
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动物实验
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配制
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剂量
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给药方式
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参考文献: 1. Kim KB, et al. Bioorg Med Chem Lett. 1999 Dec 6, 9(23), 3335-40. 2. Hanada M, et al. J Antibiot (Tokyo). 1992 Nov, 45(11), 1746-52. 3. Garrett IR, et al. J Clin Invest. 2003 Jun, 111(11), 1771-82. 4. McNaught KS, et al. Ann Neurol. 2004 Jul, 56(1), 149-62. 5. Rideout HJ, et al. J Neurochem. 2005 Jun, 93(5), 1304-13. 包装清单: