γ-Secretase Inhibitor IX-CAS 208255-80-5-Calbiochem

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一般描述

A cell-permeable dipeptide that suppresses Aβ production by blocking γ-secretase (Aβ_totalIC₅₀= 115 nM, Aβ₄₂IC₅₀= 200 nM). Prevents Aβ₃₄generation in murine N2a cells and hAPP/hBACE-1 transfected human HEK 293 cells. Reported to be functionally active in both HEK 293 cells and neuronal cultures without affecting the secretion of amyloid-β precursor protein (APP). Also shown to lower Aβ levels acutely in APP-transgenic mice. Reported to reduce extracellular Aβ plaques and intracellular Aβ accumulation in 3xTgAD transgenic mice. A 25 mM (5 mg/462 ?l) solution of γ-Secretase Inhibitor IX (Cat. No. 565784) in DMSO is also available.
A cell-permeable dipeptide that inhibits γ-secretase activity and suppresses Aβ production (Aβ total IC₅₀= 115 nM; Aβ₄₂IC₅₀= 200 nM). Reported to be functionally active in both HEK293 cells overexpressing human APP751 and neuronal cultures, however, it does not affect the secretion of amyloid-b precursor protein (APP). Effective in acutely lowering Ab in APPV717F-transgenic mice. Also effective in inhibiting the production of an ~6 kDa C-terminal cleavage product (CTFg) in HEK293 cells stably transfected with the Swedish mutant, βAPP₆₉₅. Reported to reduce extracellular Aβ plaques and intracellular Aβ accumulation in 3xTgAD transgenic mice.

包装

10 mg in Plastic ampoule
5 mg in Glass bottle
Packaged under inert gas

生化/生理作用

Cell permeable: yes
Product does not compete with ATP.
Reversible: no
Target IC₅₀: 115 nM suppressing Aβtotal production; 200 nM suppressing Aβ42 production

警告

Toxicity: Standard Handling (A)

其他说明

Morohashi, Y., et al. 2006.J. Bio. Chem.Vol. 281,14670.
Nishitomo, K. et al. 2006J. Neurochem.99,1555.
Oddo, S., et al. 2004.Neuron43,321.
Dovey, H.F., et al. 2001.J. Neurochem.76,173.
Sastre, M., et al. 2001.EMBO Rep.2,835.
Vandermeeren, M., et al. 2001.Neurosci. Lett.315,145.

法律信息

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

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