A γ-secretase inhibitor that blocks Notch processing (IC50 = 1.7 nM); reduces Aβ40 levels by 71% in an APP transgenic mouse model within 4 hours after a single 100 μM/kg dose

DBZ – 1 mg

Brand:
Cayman
CAS:
209984-56-5
Storage:
-20
UN-No:
Non-Hazardous - /

γ-Secretase is a multi-subunit aspartyl protease that cleaves amyloid precursor protein (APP) and many other type 1 transmembrane proteins, including Notch, E-cadherin, and ErbB4.{18537} The proteolysis of APP by secretases produces beta amyloid (Aβ), a 39- to 42-amino acid peptide which forms the amyloid plaques that are characteristic of Alzheimer’s disease.{10614} DBZ is a dipeptidic inhibitor of γ-secretase that potently blocks the cleavage of Notch into its active signaling effector, Notch intracellular domain, in human T cell lymphoma (SupT1) cells (IC50 = 1.7 nM).{23310} Within 4 hours after a single 100 μM/kg dose, DBZ demonstrates anti-Alzheimer activity in an APP transgenic mouse model characterized by high levels of Aβ40 by reducing Aβ40 levels by 71%.{23310}  

 

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Description

A γ-secretase inhibitor that blocks Notch processing (IC50 = 1.7 nM); reduces Aβ40 levels by 71% in an APP transgenic mouse model within 4 hours after a single 100 μM/kg dose

Formal name: N-[(1S)-2-[[(7S)-6,7-dihydro-5-methyl-6-oxo-5H-dibenz[b,d]azepin-7-yl]amino]-1-methyl-2-oxoethyl]-3,5-difluoro-benzeneacetamide

Synonyms:  ​YO-01027|Dibenzazepine

Molecular weight: 463.5

CAS: 209984-56-5

Purity: ≥98%

Formulation: A crystalline solid

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

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