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经验配方 CAS号 C₁₅H₂₄N₂O₇S 1258004-00-0 描述 概述 An irreversible proteasome inhibitor. A Streptomyces metabolite that acts as a highly specific inhibitor of the 20S proteasome (MCP; multicatalytic proteinase complex) (IC50 = 500 nM for 20S proteasome). Blocks proteasome activity by targeting the catalytic β-subunit. Acts as a covalent inhibitor of the chymotrypsin- and trypsin-like activities of the proteasome. Induces neurite outgrowth in Neuro 2A mouse neuroblastoma cells and inhibits progression of synchronized Neuro 2A cells and MG-63 human osteosarcoma cells beyond the G1 phase of the cell cycle. Reported to induce apoptosis in human monoblast U937 cells. Also inhibits NF-κB activation (IC50 = 10 µM). 产品目录编号 426100 品牌系列 Calbiochem®
同义词 Proteasome Inhibitor VI 参考 参考 Keyomarsi, K., et al. 2011. Cell. Biol. Toxicol. 27, 123.
Adams, J., and Stein, R. 1996. Ann. Rep. Med. Chem. 31, 279.
Dick, L.R., et al. 1996. J. Biol. Chem. 271, 7273.
Oda, K., et al. 1996. Biochem. Biophys. Res. Commun. 219, 800.
Fenteany, G., et al. 1995. Science 268, 726.
Imajoh-Ohmi, S., et al. 1995. Biochem. Biophys. Res. Commun. 217, 1070.
Jensen, T.J., et al. 1995. Cell 83, 129.
Katagiri, M.M., et al. 1995. J. Antibiot. 48, 344.
Mori, S., et al. 1995. J. Biol. Chem. 270, 29447.
Tanaka, H., et al. 1995. Biochem. Biophys. Res. Commun. 216, 291.
Fenteany, G., et al. 1994. Proc. Natl. Acad. Sci. USA 91, 3358.
Omura, S., et al. 1991. J. Antibiot. 44, 117.产品信息 CAS号 1258004-00-0 具有ATP竞争性 N 形式 White solid Hill配方 C₁₅H₂₄N₂O₇S 化学配方 C₁₅H₂₄N₂O₇S Molar Mass 376.4 可逆 N 结构配方图像 生物信息 主靶 20S proteasome (MCP; multicatalytic proteinase complex) 主靶IC50 500 nM against 20S proteasome; 10 µM against NF-κB activation 纯度 ≥99% by HPLC 理化信息 细胞可渗透 N 溶解度 DMSO or H₂O 储存和货运信息 货运代码 Ambient Temperature Only
毒性 Standard Handling
储存 -20°C
无需冷冻 No
特殊指南 Following reconstitution in DMSO, aliquot and freeze (-20°C). DMSO stock solutions are stable for up to 1 month at -20°C. Unstable in aqueous solutions; reconstitute in H₂O just prior to use.
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