A γ-secretase inhibitor (IC50 = 17 nM); selective for γ-secretase over HIV-1

L-685,458 – 10 mg

Brand:
Cayman
CAS:
292632-98-5
Storage:
-20
UN-No:
Non-Hazardous - /

L-685,458 is an inhibitor of γ-secretase (IC50 = 17 nM).{10285} It is selective for γ-secretase over HIV-1, cathepsin D, trypsin, HepC3 NS3, papain, and calpain I proteases (IC50s = >1,000 nM). L-685,458 inhibits production of amyloid-β (1-40) (Aβ40; Item No. 21617) and Aβ42 (Item No. 20574) in Neuro2A cells transfected with human amyloid precursor protein (APP; IC50s = 402 and 775 nM, respectively). It is also an inhibitor of Notch signaling that blocks hypoxia-induced activity of the Notch-responsive reporters 12xCSL and CBF1 in isolated rat intervertebral disc cells.{35885}  

 

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Description

A γ-secretase inhibitor (IC50 = 17 nM); selective for γ-secretase over HIV-1, cathepsin D, trypsin, HepC3 NS3, papain, and calpain I proteases (IC50s = >1,000 nM); inhibits production of Aβ40 and Aβ42 in Neuro2A cells transfected with human APP (IC50s = 402 and 775 nM, respectively); blocks hypoxia-induced activity of the Notch-responsive reporters 12xCSL and CBF1 in isolated rat intervertebral disc cells

Formal name: N-[(2R,4R,5S)-5-[[(1,1-dimethylethoxy)carbonyl]amino]-4-hydroxy-1-oxo-6-phenyl-2-(phenylmethyl)hexyl]-L-leucyl-L-phenylalaninamide

Synonyms:  γ-Secretase Inhibitor X

Molecular weight: 672.9

CAS: 292632-98-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Peptidases & Proteases||Research Area|Cell Biology|Proteolysis|Lysosomal Proteases||Research Area|Neuroscience|Neurodegenerative Disorders|Alzheimer’s Disease

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