GAMMA-SECRETASE INHIBITOR XII - CALBIOCHEM (C15-1305-822)

General description

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).

Biochem/physiol Actions

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

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Sequence

Z-Ile-Leu-CHO

Other Notes

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

Legal Information

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

Molecular Weight: 362.46. Empirical Formula: C₂₀H₃₀N₂O₄. Quality Level: 100. Assay: ≥. 95% (HPLC). form: solid. manufacturer/tradename: Calbiochem^®. . storage condition: OK to freeze, protect from light. color: white. solubility: DMSO: 5 . mg/mL. shipped in: ambient. storage temp.: −. 20°C. Storage Class Code: 11 - Combustible Solids. WGK: WGK 1. Flash Point(F): Not applicable. Flash Point(C): Not applicable.