γ-Secretase Inhibitor XXI, Compound E-CAS 209986-17-4-Calbiochem

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一般描述

A cell-permeable, potent, selective, peptidomimetic, non-transition-state analog inhibitor of γ-secretase and Notch processing (IC₅₀= 300 pM for Aβ₄₀in CHO cells overexpressing wild type βAPP; 240 pM for Aβ₄₀, 370 pM for Aβ₄₂, and 320 pM for NICD, respectively, in HEK293 cells stably transfected with βAPP₆₉₅and mNotchΔE(M1727V); 100 pM for both Aβ₄₀and Aβ₄₂in SH-SY5Y cells stably transfected with SPA4CT). Lowers Aβ levels in several APP transgenic mouse models. Reported to bind to presenilins and suppress the proteolytic cleavage of transmembrane protein substrates, including APLP1 and APLP2, CD44, ErbB4, E-cadherin, low density lipoprotein receptor-related proteins, Notch ligands, and p75^NTR. Only weakly affects presenilinase activity at much higher concentrations (200-400 ?M).

包装

500 μg in Plastic ampoule
1 mg in Glass bottle
Packaged under inert gas

生化/生理作用

Cell permeable: yes
Target IC₅₀: 300 pM for Aβ40 in CHO cells overexpressing wild typeβAPP; 240 pM for Aβ40, 370 pM for Aβ42, and 320 pM for NICD, respectively, in HEK293 cells stably transfected with βAPP695 and mNotchΔE(M1727V); 100 pM for both Aβ40
Primary Target
γ-secretase and Notch processing Ab40 in CHO cells overexpressing wild type bAPP
Product does not compete with ATP.
Reversible: no

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

其他说明

Milano, J., et al. 2004.Toxicol. Sci.82,341.
Jung, K.M., et al. 2003.J. Biol. Chem.278,42161.
Murakami, D., et al. 2003.Oncogene22,1511.
Campbell, W.A., et al. 2003.J. Neurochem.85,1563.
Berechid, B.E., et al., 2002.J. Biol. Chem.277,8154.
Lee, H.J., et al. 2002.J. Biol. Chem.277,6318.
May, P., et al. 2002.J. Biol. Chem.277,18736.
Scheinfeld, M.H., et al. 2002.J. Biol. Chem.277,44195.
Ni, C. Y., et al. 2001.Science294,2179.
Beher, D., et al. 2001.J. Biol. Chem.276,45394.
Doerfler, P., et al. 2001.Proc. Natl. Acad. Sci. USA98,9312.
Seiffert, D., et al. 2000.J. Biol. Chem.275,34086.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

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安全信息