L-685,458, , >96% (HPLC), solid

Stock Code: 3573439
Manufacturer Part No: L1790-1MG
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Application


L-685,458 has been used to attenuate Notch signalling in ovary culture. It has also been used to analyze the specificity of the ?-secretase activity in brain tissue samples.


Biochem/physiol Actions


L-685,458 is a potent, selective, structurally novel γ-secretase inhibitor; equipotent inhibitor of both Aβ1-42 and Aβ1-40 production.


L-685,458 mimics the transition state in aspartyl protease. It possesses an IC50 of 17nM with respect to inhibition of A? synthesis. It is known to block Notch (neurogenic locus notch homolog protein) signaling, which in turn reduces ERK (extracellular signal regulated kinase) phosphorylation by EGF (epidermal growth factor). L-685,458 targets the active site and substrate binding site of the enzyme.


Features and Benefits


This compound was developed by Merck & Co., Inc., Kenilworth, NJ, U.S.. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.


Legal Information


Manufactured and sold under license from Merck & Co., Inc., Kenilworth, NJ, U.S.


Packaging


1, 5 mg in glass bottle

Colourwhite
Quality Level100
InChI keyMURCDOXDAHPNRQ-ZJKZPDEISA-N
InChI1S/C39H52N4O6/c1-26(2)21-33(37(47)41-32(35(40)45)24-29-19-13-8-14-20-29)42-36(46)30(22-27-15-9-6-10-16-27)25-34(44)31(23-28-17-11-7-12-18-28)43-38(48)49-39(3,4
ManufacturerSIGMA-ALDRICH
Formsolid
Assay>96% (HPLC)

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