L-685,458

• Supplier: Tocris Bioscience
• Catalog: 1949
• Prices: $259.00
• Sizes: 1 mg
• Function Type: Inhibitor
• Cas Number: 292632-98-5
• Chemical Name: (5S)-(tert-Butoxycarbonylamino)-6-phenyl-(4R)-hydroxy-(2R)-benzylhexanoyl)-L-leucy-L-phenylalaninamide
• Formula: C39H52N4O6
• Molecular Weight: 672.85
• Purity: >97 %
• Description: Potent and selective γ -secretase inhibitor (IC 50 = 17 nM) that displays > 50-fold selectivity over a range of aspartyl, serine and cysteine proteases. Exhibits equal potency for inhibition of A β 40 and A β 42 peptides (IC 50 values are 48 and 67 nM respectively in human neuroblastoma cells). Also regulates CXCR4 and VEGFR2 expression through inhibition of Notch signaling in vitro .

Product References

L-685,458, an aspartyl protease transition state mimic, is a potent inhibitor of - L-685,458, an aspartyl protease transition state mimic, is a potent inhibitor of

Shearman MS, Beher D, Clarke EE, Lewis HD, Harrison T, Hunt P, Nadin A, Smith AL, Stevenson G, Castro JL. Biochemistry. 2000 Aug 1;39(30):8698-704.

Up-regulation of the Notch ligand Delta-like 4 inhibits VEGF-induced endothelial - Up-regulation of the Notch ligand Delta-like 4 inhibits VEGF-induced endothelial

Williams CK, Li JL, Murga M, Harris AL, Tosato G. Blood. 2006 Feb 1;107(3):931-9. Epub 2005 Oct 11.

Regulation of CXCR4 by the Notch ligand delta-like 4 in endothelial cells. - 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 Mar 15;68(6):1889-95.