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- 详细信息
- 文献和实验
- 技术资料
- 库存:
大量
- 英文名:
Epoxomicin
- 保质期:
1年
- 供应商:
上海联迈生物工程有限公司
- 保存条件:
-20℃保存
- 规格:
5mg
| 产品编号 | 产品名称 | 产品包装 | 产品价格 |
| LM7198-5mg | Epoxomicin (20S Proteasome抑制剂) | 5mg | 2933.00元 |
| 化学名 | (2S,3S)-2-[[(2S,3S)-2-[acetyl(methyl)amino]-3-methylpentanoyl]amino]-N-[(2S,3R)-3-hydroxy-1-[[(2S)-4-methyl-1-[(2R)-2-methyloxiran-2-yl]-1-oxopentan-2-yl]amino]-1-oxobutan-2-yl]-3-methylpentanamide | ![]() |
| 简称 | Epoxomicin | |
| 别名 | BU-4061T, BU 4061T | |
| 中文名 | N/A | |
| 化学式 | C28H50N4O7 | |
| 分子量 | 554.72 | |
| CAS号 | 134381-21-8 | |
| 纯度 | 98% | |
| 溶剂/溶解度 | Water<1mg/ml; DMSO10mg/ml; Ethanol<1mg/ml | |
| 溶液配制 | 5mg加入0.9ml DMSO,或者每5.55mg加入1ml DMSO,配制成10mM溶液。LM7198-10mM用DMSO配制。 |
| 产品描述 | 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 | - | - | - | - |
| IC50 | - | - | - | - | - |
| 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 | N/A | ||||
| 特征 | N/A | ||||
| 酶活性检测实验 | |
| 方法 | N/A |
| 细胞实验 | |
| 细胞系 | N/A |
| 浓度 | N/A |
| 处理时间 | N/A |
| 方法 | N/A |
| 动物实验 | |
| 动物模型 | N/A |
| 配制 | N/A |
| 剂量 | N/A |
| 给药方式 | N/A |
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:
| 产品编号 | 产品名称 | 包装 |
| LM7198-10mM | Epoxomicin (20S proteasome抑制剂) | 10mM×0.2ml |
| LM7198-5mg | Epoxomicin (20S proteasome抑制剂) | 5mg |
| LM7198-25mg | Epoxomicin (20S proteasome抑制剂) | 25mg |
| — | 说明书 | 1份 |
-20℃保存,至少一年有效。5mg和25mg包装也可室温保存,至少6个月有效。如果溶于非DMSO溶剂,建议分装后-80℃保存,预计6个月内有效。
注意事项:
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文献和实验The 20S proteasome is a multicatalytic protein complex, present in all eukaryotic cells, that plays a major role in intracellular protein degradation. In mammalian cells, this symmetrical cylindrical complex is composed of two copies
Assays for Proteasome Inhibition
activity of the proteasome is contained within this central 20S core (MW=730 kDa), a multicatalytic protease that has three well characterized peptidase activities. The three peptidases: chymotryptic, tryptic, and postglutamyl peptide hydrolytic activities
Assays for Proteasome Assembly and Maturation
The 20S proteasome is a complex multisubunit protease that is present in all phylae of life. Eukaryotic 26S proteasomes, which are composed of 20S proteasomes and 19S activator complexes, mediate the degradation of ubiquitylated proteins
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