Chemical Name: (5S)-(tert-Butoxycarbonylamino)-6-phenyl-(4R)-hydroxy-(2R)-benzylhexanoyl)-L-leucy-L-phenylalaninamide
Biological ActivityPotent and selective γ-secretase inhibitor (IC50 = 17 nM) that displays > 50-fold selectivity over a range of aspartyl, serine and cysteine proteases. Exhibits equal potency for inhibition of Aβ40 and Aβ42 peptides (IC50 values are 48 and 67 nM respectively in human neuroblastoma cells). Also regulates CXCR4 and VEGFR2 expression through inhibition of Notch signaling in vitro.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Regulation of CXCR4 by the Notch ligand delta-like 4 in endothelial cells.
Williams CK, Segarra M, Sierra Mde L, Sainson RC, Tosato G, Harris AL
Cancer Res., 2008;68(6):1889-95.
L-685,458, an aspartyl protease transition state mimic, is a potent inhibitor of amyloid-β-protein precursor γ-secretase activity.
Shearman et al.
Up-regulation of the Notch ligand delta-like 4 inhibits VEGF-induced endothelial cell function.
Williams et al.
Citations for L-685,458
The citations listed below are publications that use Tocris products. Selected citations for L-685,458 include:
5 Citations: Showing 1 - 5
HIV-1 counteracts an innate restriction by amyloid precursor protein resulting in neurodegeneration.
Authors: Chai Et al.
Nat Commun 2017;8:1522
Differential Inhibition of Signal Peptide Peptidase Family Members by Established γ-Secretase Inhibitors.
Authors: Ran Et al.
PLoS One 2015;10:e0128619
RAGE inhibition in microglia prevents ischemia-dependent synaptic dysfunction in an amyloid-enriched environment.
Authors: Origlia Et al.
J Neurosci 2014;34:8749
γ-Secretase processing and effects of γ-secretase inhibitors and modulators on long Aβ peptides in cells.
Authors: Ran Et al.
J Biol Chem 2014;289:3276
Canonical Notch signalling is inactive in urothelial carcinoma.
Authors: Greife Et al.
BMC Cancer 2014;14:628
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