γ-Secretase Inhibitor XII

A cell-permeable, reversible dipeptide aldehyde that reduces Aβ production by blocking γ-secretase activity in vitro (Aβ₄₀ IC₅₀ = 7.9 µM; Aβ₄₂ IC₅₀ = 7.6 µM) and in cultured CHO 2b-7 cells that stably overexpress APP695 (Aβ₄₀ IC₅₀ = 11.5 µM; Aβ₄₂ IC₅₀ = 8.3 µM). Also blocks the generation of CTFγ (γ-secretase-generated carboxyl-terminal fragment). Does not affect the formation of amyloid-β-precursor protein (APP).

A cell-permeable, reversible dipeptide aldehyde that reduces amyloid-β protein (Aβ) production by blocking γ-secretase activity in vitro (Aβ₄₀ IC₅₀ = 7.9 µM; Aβ₄₂ IC₅₀ = 7.6 µM) and in cultured cells that stably over-express APP695 (Aβ₄₀ IC₅₀ = 11.5 µM; Aβ₄₂ IC₅₀ = 8.3 µM). Also shown to block the generation of γCTF (γ-secretase-generated carboxy-terminal fragment).

Cell permeable: yes

Primary Target
Aβ40 in vitro

Product does not compete with ATP.

Reversible: yes

Target IC₅₀: 7.9 µM for Aβ40; 7.6 µM for Aβ42 in vitro

Packaged under inert gas

Toxicity: Standard Handling (A)

Z-Ile-Leu-CHO

Weijzen, S., et al. 2002. Nat. Med.8, 979.
McLendon, C., et al. 2000. FASEB J.14, 2383.

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