The γ₄₀-Secretase Inhibitor I controls the biological activity of γ₄₀-Secretase. This small molecule/inhibitor is primarily used for Neuroscience applications.
Synonym(s):
γ4₀-Secretase Inhibitor I, t-3,5-DMC-IL-CHO, N- trans-3,5-Dimethoxycinnamoyl)-Ile-leucinal, t-3,5-DMC-IL-CHO, N-trans-3,5-Dimethoxycinnamoyl)-Ile-leucinal
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 M; Aβ1-40 IC50 ~ 22 M; Aβ1-42 IC50 >50 M in CHO cells stable transfected with the cDNA encoding βAPP695.
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)].
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
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class
11 - Combustible Solids
wgk_germany
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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