An inhibitor of γ-secretase

DAPT – 50 mg

Brand:
Cayman
CAS:
208255-80-5
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. 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. DAPT is an inhibitor of γ-secretase, blocking the production of total Aβ in human primary neuronal cultures with an IC50 value of 115 nM and Aβ42 with an IC50 value of 200 nM.{18537} DAPT is also effective in vivo, reducing brain levels of Aβ when given orally to mice that are transgenic for human APPV717F or to rats.{18537,18534,18535} Through its effects on γ-secretase, DAPT indirectly inhibits Notch, affecting cell signaling and cell differentiation.{18536,18538}  

 

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Description

An inhibitor of γ-secretase, blocking the production of total Aβ in human primary neuronal cultures with an IC50 value of 115 nM and Aβ42 with an IC50 value of 200 nM; reduces brain levels of Aβ in vivo when given orally; indirectly inhibits Notch, affecting cell signaling and cell differentiation

Formal name: N-[2S-(3,5-difluorophenyl)acetyl]-L-alanyl-2-phenyl-glycine, 1,1-dimethylethyl ester

Synonyms:  GSI-IX

Molecular weight: 432.5

CAS: 208255-80-5

Purity: ≥95%

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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