γ-Secretase Inhibitor XX-CAS 209984-56-5-Calbiochem

C₂₆H₂₃F₂N₃O₃

463.48

A cell-permeable, potent γ-secretase inhibitor that significantly lowers both brain and plasma Aβ₄₀ levels by ~72% in Tg2576 mutant APP transgenic mouse model (100 µmol/kg, b.i.d). Induces a heterogeneous reorganization of the crypt structural-proliferative units in the intestinal tract and of the stem cell niche in the colon. Also potently inhibits Notch processing (IC₅₀ = 1.7 nM in SupT1 cells) and induces conversion of proliferative crypt cells to post-mitotic goblet cells in both the C57BL/6 and Apc^Min mouse models (10 µmol/kg, i.p).
A cell-permeable dibenzazepine (dbz) compound that acts as a potent γ-secretase inhibitor and significantly lowers both brain and plasma Aβ₄₀ levels by ~72% in Tg2576 mutant APP transgenic mouse model (100 µmol/kg, b.i.d). Induces a heterogeneous reorganization of the crypt structural-proliferative units in the intestinal tract and of the stem cell niche in the colon. Also potently inhibits Notch processing (IC₅₀ = 1.7 nM in SupT1 cells) and induces conversion of proliferative crypt cells to post-mitotic goblet cells in both the C57BL/6 and Apc^Min mouse models (10 µmol/kg, i.p).

Cell permeable: yes
Target IC₅₀: 1.7 nM inhibiting Notch processing in SupT1 cells
Product does not compete with ATP.
Reversible: no

Toxicity: Standard Handling (A)

Droy-Dupré, L., et al. 2012. Dis. Model Mech.5, 107.
van Es, J.H., et al. 2005. Nature435, 959.
Milano, J., et al. 2004. Toxicol. Sci.82, 341.

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

100

≥95% (HPLC)

solid

Calbiochem^®

OK to freeze
protect from light

white

DMSO: 10 mg/mL

ambient

−20℃

500 μg in Plastic ampoule
1 mg in Glass bottle
Packaged under inert gas

11 - Combustible Solids

WGK 3