Overview

  • Product name

    L-685,458, gamma-secretase inhibitor
  • Description

    Potent, selective and non-competitive γ-secretase inhibitor
  • Alternative names

    • (5S)-(t-Butoxycarbonylamino)-6-phenyl-(4R)hydroxy-(2R)benzylhexanoyl)-L-leu-L-phe-amide
  • Biological description

    Potent, selective and non-competitive γ-secretase inhibitor (IC50 = 17 nM). Shows 50-fold selectivity over a range of aspartyl, serine and cysteine proteases. Inhibits Aβ40 and Aβ42 peptides (IC50 values are 48 and 67 nM respectively). Active in vivo. Orally active.

  • Purity

    > 98%
  • CAS Number

    292632-98-5
  • Chemical structure

    Chemical Structure

Properties

References

This product has been referenced in:

  • Borgegard T  et al. First and second generation ?-secretase modulators (GSMs) modulate amyloid-ß (Aß) peptide production through different mechanisms. J Biol Chem 287:11810-9 (2012). Read more (PubMed: 22334705) »
  • Chakraborty R  et al. Characterization of a Drosophila Alzheimer's disease model: pharmacological rescue of cognitive defects. PLoS One 6:e20799 (2011). Read more (PubMed: 21673973) »
  • Shearman MS  et al. L-685,458, an aspartyl protease transition state mimic, is a potent inhibitor of amyloid beta-protein precursor gamma-secretase activity. Biochemistry 39:8698-704 (2000). Read more (PubMed: 10913280) »

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