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γ-Secretase inhibitor

 
ALX-260-127-M001 1 mg 344.00 USD
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Reversible peptidomimetic inhibitor of γ-secretase (IC50=10-25µM for total β-amyloid), presenilinase (IC50=0.1-1µM), and calpain II (IC50=100µM).

Product Specification

Alternative Name:MW167
 
Formula:C33H57N5O9F2
 
MW:705.8
 
Formulation:Lyophilized.
 
Purity:≥90%
 
Solubility:Soluble in DMSO containing 10% water.
 
Shipping:Ambient
 
Long Term Storage:-20°C
 
Use/Stability:Stock solutions in DMSO are stable for 6 months when stored at -20°C.
 
Handling:Protect from moisture.
 
ALX-260-127 structure
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ALX-260-127 structure

Product Literature References

Notch1 signaling is mediated by importins alpha 3, 4, and 7: K. Huenniger, et al.; Cell. Mol. Life Sci. 67, 3187 (2010), Abstract;
DLL1-mediated Notch activation regulates endothelial identity in mouse fetal arteries: I. Sorensen, et al.; Blood 113, 5680 (2009), Abstract;
Glutamate receptor subunit 3 is modified by site-specific limited proteolysis including cleavage by gamma-secretase: E.L. Meyer, et al.; J. Biol. Chem. 278, 23786 (2003), Abstract; Full Text
Presenilin endoproteolysis mediated by an aspartyl protease activity pharmacologically distinct from gamma-secretase: W.A. Campbell, et al.; J. Neurochem. 85, 1563 (2003), Abstract;
Peptidomimetic probes and molecular modeling suggest that Alzheimer's gamma-secretase is an intramembrane-cleaving aspartyl protease: M.S. Wolfe, et al.; Biochemistry 38, 4720 (1999), Abstract;
A substrate-based difluoro ketone selectively inhibits Alzheimer's gamma-secretase activity: M.S. Wolfe, et al.; J. Med. Chem. 41, 6 (1998), Abstract;
Evidence that the 42- and 40-amino acid forms of amyloid beta protein are generated from the beta-amyloid precursor protein by different protease activities: M. Citron, et al.; PNAS 93, 13170 (1996), Abstract; Full Text

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