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565765

Sigma-Aldrich

γ4₀-Secretase Inhibitor I

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

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About This Item

Empirical Formula (Hill Notation):
C23H34N2O5
Molecular Weight:
418.53
UNSPSC Code:
12352200

Quality Level

100

Assay

≥95% (HPLC)

form

lyophilized 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

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 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

Packaging

Packaged under inert gas

Preparation Note

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.
trans-3,5-DMC-Ile-Leu-CHO (DMC = Dimethoxycinnamoyl)

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

Storage Class Code

11 - Combustible Solids

WGK

WGK 1

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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