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Description
General description
A potent, cell-permeable, reversible γ-secretase inhibitor that preferentially appears to inhibit the secretion of Aβ1-40 (>90%) over Aβ1-42 (~15%). Aβtotal IC50 ~ 15 µM; Aβ1-40 IC50 ~ 22 µM; Aβ1-42 IC50 > 50 µM in CHO cells stable transfected with the cDNA encoding βAPP695. Reported to be about 10-fold more potent than Z-Val-Phe-CHO (MDL 28170; Cat. No. 208722).
A potent, cell-permeable, reversible inhibitor of γ-secretase that is reported to preferentially inhibit the secretion of Aβ1-40 (>90%) vs. Aβ1-42. IC50 = ~15 µM for Aβtotal; ~22 µM for Aβ1-40; and >50 µM for Aβ1-42 in CHO cells stably transfected with the cDNA encoding βAPP695. Reported to be about 10-fold more potent than Z-Val-Phe-CHO [MDL 28170 (Cat. No. 208722)].
Packaging
1 mg in Plastic ampoule
Biochem/physiol Actions
Cell permeable: yes
Primary Target
secretion of Aβ₁₋₄₀
Product does not compete with ATP.
Reversible: yes
Target IC50: ~ 15 µM for Aβtotal; ~ 22 µM for Aβ1-40; < 50 µM for Aβ1-42 in CHO cells stable transfected with the cDNA encoding βAPP695
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Sequence
trans-3,5-DMC-Ile-Leu-CHO (DMC = Dimethoxycinnamoyl)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.
Other Notes
Higaki, J.N., et al. 1999. J. Med. Chem. 42, 3889.
- Quality Level 100 assay