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InSolution γ-Secretase Inhibitor X-Calbiochem

产品编号:4145191
规格:InSolution γ-Secretase Inhibitor X is a 1 mM solution in DMSO. A highly potent inhibitor of g-secretase (IC50 = 17, 48, 67 nM for Aβtotal, Aβ40 & Aβ42 in SHSY5Y cells overexpressing spβA4CTF).
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
产品价格
产品编号包装单位单价(元)国内现货国外库存询价单
4145191250 μG5810
4145191500 μG7680
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
total
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)
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