A cell-permeable dipeptide that inhibits y-secretase activity and suppresses Ab production (Ab total IC50=115nM; Ab42 IC50=200nM). 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, bAPP695. Reported to reduce extracellular Ab plaques and intracellular Ab accumulation in 3xTgAD transgenic mice.
Solubility:
DMSO (20mg/ml)
Molecular Weight:
~432.5
Storage and Stability:
Lyophilized powder may be stored at -20 degrees C. Stable for 12 months at -20 degrees C. Reconstitute with sterile DMSO. Aliquot to avoid repeated freezing and thawing. Store at -20 degrees C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.
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