565772
γ-Secretase Inhibitor XI - CAS 62252-26-0 - Calbiochem
Synonym(s):
7-Amino-4-chloro-3-methoxyisocoumarin, JLK6
assay
≥97% (HPLC)
form
solid
color
yellow
solubility
DMSO: 5 mg/mL
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)
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.
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
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’.
Already Own This Product?
Find documentation for the products that you have recently purchased in the Document Library.
J E Kerrigan et al.
Journal of medicinal chemistry, 38(3), 544-552 (1995-02-03)
A series of 3-alkoxy-7-amino-4-chloroisocoumarins with various 3-alkoxy substituents have been prepared and evaluated as inhibitors of human leukocyte elastase (HLE). In addition, a new series of acyl, urea, and carbamate derivatives of 7-amino-4-chloro-3-methoxyisocoumarin (1), 7-amino-4-chloro-3-propoxyisocoumarin (3), and 7-amino-4-chloro-3-(2-bromoethoxy)isocoumarin (6) have
K Sasaki et al.
The Journal of biological chemistry, 268(30), 22782-22787 (1993-10-25)
This report describes the isolation of a cDNA encoding a novel human Gal beta (1-3/1-4)GlcNac alpha 2,3-sialyl-transferase involved in the biosynthesis of the sialyl Lewis x determinant (NeuAc alpha 2-3 Gal beta 1-4(Fuc alpha 1-3)GlcNAc). A cDNA library of the
Amyloid-lowering isocoumarins are not direct inhibitors of gamma-secretase.
William P Esler et al.
Nature cell biology, 4(5), E110-E111 (2002-05-04)
J W Harper et al.
Biochemistry, 24(25), 7200-7213 (1985-12-03)
The time-dependent inactivation of several serine proteases including human leukocyte elastase, cathepsin G, rat mast cell proteases I and II, and human skin chymase by a number of 3-alkoxy-4-chloroisocoumarins, 3-alkoxy-4-chloro-7-nitroisocoumarins, and 3-alkoxy-7-amino-4-chloroisocoumarins at pH 7.5 and the inactivation of several
A Petit et al.
Nature cell biology, 3(5), 507-511 (2001-05-02)
We have designed new non-peptidic potential inhibitors of gamma-secretase and examined their ability to prevent production of amyloid-beta 40 (Abeta40) and Abeta42 by human cells expressing wild-type and Swedish-mutant beta-amyloid precursor protein (betaAPP). Here we identify three such agents that
Our team of scientists has experience in all areas of research including Life Science, Material Science, Chemical Synthesis, Chromatography, Analytical and many others.
Contact Technical Service