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.
|Storage||Store at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 672.85. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.49 mL||7.43 mL||14.86 mL|
|5 mM||0.3 mL||1.49 mL||2.97 mL|
|10 mM||0.15 mL||0.74 mL||1.49 mL|
|50 mM||0.03 mL||0.15 mL||0.3 mL|
The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.
References are publications that support the products' biological activity.
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
Williams et al (2006) Up-regulation of the Notch ligand delta-like 4 inhibits VEGF-induced endothelial cell function. Blood 107 931 PMID: 16219802
Williams et al (2008) Regulation of CXCR4 by the Notch ligand delta-like 4 in endothelial cells. Cancer Res. 68 1889 PMID: 18339870
If you know of a relevant reference for L-685,458, please let us know.
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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, Gamma-Secretase, Tocris Bioscience
1 Citation for L-685,458
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.
Literature in this Area
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