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InSolution γ-Secretase Inhibitor X-Calbiochem
产品编号: | 4145191 |
规格: | InSolution |
包装规格: | 250 μG,500 μG |
产品类别: | 进口试剂 |
品牌: | Sigma-Aldrich |
优惠价: | 立即咨询 |
产品别名
InSolution γ-Secretase Inhibitor X-Calbiochem
L-685,458, {1S-Benzyl-4R-[1-(1S-carbamoyl-2-phenethylcarbamoyl)-1S-3-methylbutylcarbamoyl]-2R-hydroxy-5-phenylpentyl}carbamic Acid tert-butyl Ester
基本信息
Empirical Formula【经验(实验)分子式】 | C39H52N4O6 |
Molecular weight | 672.85 |
General description【一般描述】 | A cell-permeable hydroxyethylene dipeptide isostere that acts as a potent and highly specific inhibitor of γ-secretase (Aβ total IC50 = 17 nM; Aβ40 IC50 = 48 nM; and Aβ42 IC50 = 67 nM in SH-SY5Y cells overexpressing spβA4CTF). Binds to presenilin and blocks Notch intracellular domain production. Also reported to block the formation of εCTF, resulting in the accumulation of α- and βCTF. Functions as a transition state analog mimic at the catalytic site of an aspartyl protease, however, it exhibits over 100-fold greater selectivity for γ-secretase than for cathepsin D. A cell-permeable hydroxyethylene dipeptide isostere that acts as a highly specific and a potent inhibitor of γ-secretase (Aβtotal IC50 = 17 nM, Aβ40 IC50 = 48 nM, and Aβ42 IC50 = 67 nM in SHSY5Y cells overexpressing spβA4CTF). Binds to presenilin and blocks Notch intracellular domain production. Functions as a transition state analog mimic at the catalytic site of an aspartyl protease, however, it exhibits over 100-fold greater selectivity for γ-secretase than for cathepsin D. |
Biochem/physiol Actions【生化/生理作用】 | Product does not compete with ATP. Cell permeable: yes Target IC50: Aβtotal 17 nM, Aβ40 48 nM, and Aβ42 67 nM in SHSY5Y cells overexpressing spβA4CTF Reversible: no Primary Target Aβtotal |
Warning【警告】 | Toxicity: Standard Handling (A) |
Physical form【外形】 | A 1 mM (250 µg in 372 µl or 500 µg in 744 µl) solution in DMSO. |
Reconstitution【重悬】 | Following initial thaw, aliquot and freeze (-20°C). |
Other Notes【其他说明】 | Weidemann, A., et al. 2002. Biochemistry41, 2825. Doerfler, P., et al. 2001. Proc. Natl. Acad. Sci. USA98, 9312. Li, Y.M., et al. 2000. Proc. Natl. Acad. Sci. USA97, 6138. Shearman, M.S., et al. 2000. Biochemistry39, 8698. |
Legal Information【法律信息】 | CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany |
产品性质
Quality Level【质量水平】 | 100 |
Assay【测定】 | ≥90% (HPLC) |
form【形式】 | liquid |
manufacturer/tradename | Calbiochem® |
storage condition【储存条件】 | OK to freeze desiccated protect from light |
shipped in【运输】 | ambient |
storage temp.【储存温度】 | −20℃ |
packaging【包装】 | 250, 500 μg in Plastic ampoule Packaged under inert gas |
安全信息
Storage Class Code【储存分类代码】 | 10 - Combustible liquids |
WGK | WGK 1 |
Flash Point(F)【闪点(F)】 | 188.6 °F - (Dimethylsulfoxide) |
Flash Point(C)【闪点(C)】 | 87 ℃ - (Dimethylsulfoxide) |