General description
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 ApcMin mouse models (10 µmol/kg, i.p).
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 ApcMin mouse models (10 µmol/kg, i.p).
Biochem/physiol Actions
Cell permeable: yes
Product does not compete with ATP.
Reversible: no
Target IC50: 1.7 nM inhibiting Notch processing in SupT1 cells
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Other Notes
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
- UPC:
- 12352200
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 565789-1MG
