Cat. No. 2627
Chemical Name: (5S)-(tert-Butoxycarbonylamino)-6-p
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.
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 / Safety Data Sheet
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 this product 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.
Do you know of a great paper that uses L-685,458 from Tocris? If so please let us know.
View Related Products by Product Action
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
Find multiple products by catalog number
New Products in this Area
High affinity angiotensin-converting enzyme (ACE) ligandTMI 1
Adam 17 (TACE) and MMP inhibitor; orally bioavailableRitonavir
HIV-1 and HIV-2 protease inhibitorAcetyl Pepstatin
High affinity aspartic protease inhibitor; inhibits HIV-1/2 proteinasesONO 6818
High affinity and selective human neutraphil elastase 1 (HNE1) inhibitor; orally active
Follow Tocris on LinkedIn
Visit our LinkedIn page for the latest Tocris news, events and updates.