Biochem/physiol Actions

Reversible: no

Target IC₅₀: 115 nM suppressing Aβtotal production; 200 nM suppressing Aβ42 production

Product does not compete with ATP.

Cell permeable: yes

General description

A cell-permeable dipeptide that inhibits γ-secretase activity and suppresses Aβ production (Aβ total IC₅₀ = 115 nM; Aβ₄₂ IC₅₀ = 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.

A cell-permeable dipeptide that suppresses Aβ production by blocking γ-secretase (Aβ_total IC₅₀ = 115 nM, Aβ₄₂ IC₅₀ = 200 nM). Prevents Aβ₃₄ generation 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 µl) solution of γ-Secretase Inhibitor IX (Cat. No. 565784) in DMSO is also available.

Legal Information

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

Other Notes

Morohashi, Y., et al. 2006. J. Bio. Chem.Vol. 281, 14670.Nishitomo, K. et al. 2006 J. 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.

Packaging

5 mg in Glass bottle

Packaged under inert gas

10 mg in Plastic ampoule

Warning

Toxicity: Standard Handling (A)