产品说明
一般描述
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 beyond theG1 phase of the cell cycle. Reported to induce apoptosis in human monoblast U937 cells. Also inhibits NF-κB activation (IC50 = 10 µM)
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).
包装
200, 400 μg in Plastic ampoule
1 mg in Glass bottle
生化/生理作用
Target IC50: 500 nM against 20S proteasome; 10 µM against NF-κB activation
Primary Target
20S proteasome (MCP; multicatalytic proteinase complex)
Product does not compete with ATP.
Reversible: no
Cell permeable: no
警告
Toxicity: Standard Handling (A)
重悬
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.
其他说明
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. Science268, 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. USA91, 3358.
Omura, S., et al. 1991. J. Antibiot.44, 117.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
基本信息
经验(实验)分子式 | C15H24N2O7S |
分子量 | 376.43 |
产品性质
质量水平 | 100 |
测定 | ≥99% (HPLC) |
形式 | solid |
manufacturer/tradename | Calbiochem® |
储存条件 | OK to freeze |
颜色 | white |
溶解性 | DMSO: 50 mg/mL water: soluble |
运输 | ambient |
储存温度 | −20℃ |
安全信息
储存分类代码 | 11 - Combustible Solids |
WGK | WGK 1 |
闪点(F) | Not applicable |
闪点(C) | Not applicable |