L-685,458

Cat. No. 2627

L-685,458 C39H52N4O6 [292632-98-5]

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Chemical Name: (5S)-(tert-Butoxycarbonylamino)-6-phenyl-(4R)-hydroxy-(2R)-benzylhexanoyl)-L-leucy-L-phenylalaninamide

Biological Activity

Potent 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.

Technical Data

M.Wt:
672.85
Formula:
C39H52N4O6
Solubility:
Soluble to 15 mM in DMSO
Purity:
>97 %
Storage:
Store at -20°C
CAS No:
292632-98-5

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Datasheet

Certificate of Analysis / Product Datasheet
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References are publications that support the products' biological activity.

Williams et al (2008) Regulation of CXCR4 by the Notch ligand delta-like 4 in endothelial cells. Cancer Res. 68 1889. PMID: 18339870.

Williams et al (2006) Up-regulation of the Notch ligand delta-like 4 inhibits VEGF-induced endothelial cell function. Blood 107 931. PMID: 16219802.

Shearman et al (2000) L-685,458, an aspartyl protease transition state mimic, is a potent inhibitor of amyloid-β-protein precursor γ-secretase activity. Biochemistry 39 8698. PMID: 10913280.

If you know of a relevant reference for L-685,458 please let us know.

Citations are publications that use Tocris products. Selected citations for L-685,458 include:

Greife et al (2014) Canonical Notch signalling is inactive in urothelial carcinoma. BMC Cancer 14 628. PMID: 25167871.

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Keywords: L-685,458, supplier, Potent, selective, γ-secretase, gamma-secretase, inhibitors, inhibits, Aβ4, beta40, β42, beta42, Proteinases, Proteases, b-amyloid, β-Amyloid, beta-Amyloid, Precursor, Protein, APP, beta, Peptides, L685458, amyloidbeta, amyloidb, amyloidβ, Tocris Bioscience, γ-Secretase Inhibitor products

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