Catalog Number: 2627
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.
Background References
  1. Regulation of CXCR4 by the Notch ligand delta-like 4 in endothelial cells.
    Williams CK, Segarra M, Sierra Mde L et al.
    Cancer Res.
  2. L-685,458, an aspartyl protease transition state mimic, is a potent inhibitor of amyloid-β-protein precursor γ-secretase activity.
    Shearman et al.
    Biochemistry, 2000;39:8698
  3. Up-regulation of the Notch ligand delta-like 4 inhibits VEGF-induced endothelial cell function.
    Williams et al.
    Blood, 2006;107:931
Citations:

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

1 Citations: Showing 1 - 1

  1. Canonical Notch signalling is inactive in urothelial carcinoma.
    Authors: Greife Et al.
    BMC Cancer 2014;14:628

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