L-685,458

Name: L-685,458
Brand: Tocris Bioscience
SKU: 2627

Tocris Bioscience, part of Bio-Techne | Catalog # 2627

Citations (39)

COA / SDS

Potent and selective γ-secretase inhibitor

Key Product Details

Chemical Name:	(5S)-(tert-Butoxycarbonylamino)-6-phenyl-(4R)-hydroxy-(2R)-benzylhexanoyl)-L-leucy-L-phenylalaninamide
Purity:	≥97%

View Full Technical Details for L-685,458

Technical Data
Citations

Biological Activity for L-685,458

L-685,458 is a potent and selective γ-secretase inhibitor (IC₅₀ = 17 nM) that displays > 50-fold selectivity over a range of aspartyl, serine and cysteine proteases. L-685,458 binds with high affinity to the related aspartyl protease, signal peptide peptidase (SPP; K_D = 5.1 nM), and inhibits SPP expressed in HEK293 cells (IC₅₀ = 10 μM). L-685,458 exhibits equal potency for inhibition of Aβ40 and Aβ42 peptides (IC₅₀ values are 48 and 67 nM respectively in human neuroblastoma cells). It also regulates CXCR4 and VEGFR2 expression through inhibition of Notch signaling in vitro.

Technical Data for L-685,458

Formula	C₃₉H₅₂N₄O₆
Storage	Store at -20°C
Purity	≥97%
CAS Number	292632-98-5

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for L-685,458

Solubility

Soluble Soluble to 15 mM in DMSO

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References for L-685,458

References are publications that support the biological activity of the product.

Maury Y, Come J, Piskorowski R, Salah-Mohellibi N, Chevaleyre V, Peschanski M, Martinat C, Nedelec S Combinatorial analysis of developmental cues efficiently converts human pluripotent stem cells into multiple neuronal subtypes. Nat Biotechnol, 2015;33(1):89-96. 2015 PMID: 25383599
Williams CK, Segarra M, Sierra Mde L, Sainson RC, Tosato G, Harris AL Regulation of CXCR4 by the Notch ligand delta-like 4 in endothelial cells. Cancer Res., 2008-03-15;68(6):1889-95. 2008-03-15 PMID: 18339870
Nakajima C, Kulik A, Frotscher M, Herz J, Schafer M, Bock H, May P Low density lipoprotein receptor-related protein 1 (LRP1) modulates N-methyl-D-aspartate (NMDA) receptor-dependent intracellular signaling and NMDA-induced regulation of postsynaptic protein complexes. J Biol Chem, 2013;288(30):21909-23. 2013 PMID: 23760271
Csaszar, Elizabet, Wang, Weijia, Usenko, Tatiana, Qiao, Wenlian, Delaney, Colleen, Bernstein, Irwin D, Zandstra, Peter W Blood stem cell fate regulation by Delta-1-mediated rewiring of IL-6 paracrine signaling. Blood, 2014;123(5):650-8. 2014 PMID: 24243972
P Saxena, BC Heng, P Bai, M Folcher, H Zulewski, M Fussenegge A programmable synthetic lineage-control network that differentiates human IPSCs into glucose-sensitive insulin-secreting beta-like cells Nat Commun, 2016;7(0):11247. 2016 PMID: 27063289
Shearman et al. L-685,458, an aspartyl protease transition state mimic, is a potent inhibitor of amyloid-β-protein precursor γ-secretase activity. Biochemistry, 2000;39:8698 PMID: 10913280
Williams et al. Up-regulation of the Notch ligand delta-like 4 inhibits VEGF-induced endothelial cell function. Blood, 2006;107:931 PMID: 16219802

L-685,458

Tocris Bioscience, part of Bio-Techne | Catalog # 2627

Key Product Details

Biological Activity for L-685,458

Technical Data for L-685,458

Solubility for L-685,458

Dilution Calculator

Reconstitution Calculator

References for L-685,458

Product Documents for L-685,458

COA

Certificate of Analysis

SDS

CONTACT INFORMATION

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