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Sigma-Aldrich

γ-Secretase Inhibitor XI - CAS 62252-26-0 - Calbiochem

Synonym(s):

7-Amino-4-chloro-3-methoxyisocoumarin, JLK6

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About This Item

Assay

≥97% (HPLC)

form

solid

color

yellow

solubility

DMSO: 5 mg/mL

General description

A non-peptidic, cell-permeable, active site-directed, irreversible serine protease inhibitor that belongs to the class of isocoumarin analogs. Acts as a potent and selective inhibitor of γ-secretase and blocks the production of both amyloid-β 40 (Aβ40) and 42 (Aβ42) in HEK293 cells (70-80% inhibition at 100 μM concentration) expressing wild-type and Swedish-mutant β-amyloid precursor protein (βAPP). Does not exhibit any significant effect on either the processing or mΔEnotch-1 or the endoproteolysis of presenilins.

Application

The γ-Secretase Inhibitor XI controls the biological activity of γ-Secretase. This small molecule/inhibitor is primarily used for Neuroscience applications.

Biochem/physiol Actions

γ-secretase and blocks the production of both Aβ40 and Aβ42 in HEK293 cells expressing wild-type and Swedish-mutant β-amyloid precursor protein (APP)
Target IC50:< 100 μM against γ-secretase and blocks the production of both amyloid-β40 (Aβ40) and Aβ42 in HEK293 cells expressing wild-type and Swedish-mutant β-amyloid precursor protein (APP)

Physical form

t1/2 = 200 min in 100 μM HEPES, 500 μM NaCl, and 10% DMSO, pH 7.5.

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 2 weeks at -20°C. This product is not stable in aqueous solution, hence, dilute in aqueous solution right prior to use (t½ at 25°C = 3.3 h in 100 mM HEPE

Storage Class Code

11 - Combustible Solids

WGK

WGK 1

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


Certificates of Analysis (COA)

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