Notch 信号通路广泛存在于脊椎动物和非脊椎动物,在进化上高度保守,通过相邻细胞之间的相互作用调节细胞、组织、器官的分化和发育。Notch信号通路由 Notch受体、Notch配体(DSL蛋白)、CSL (CBF-1,Suppressor of hairless,Lag的合称)DNA结合蛋白、其他的效应物和Notch的调节分子等组成。
DAPT: a γ-secretase inhibitor that blocks Notch signaling. As an inhibitor of Notch, DAPT has been used to study autoimmune and lymphoproliferative diseases, such as ALPS and lupus erythematosus (SLE). As an inhibitor of γ-secretase with IC50 of 0.115 and 0.2 μM for total Aβ and Aβ42 levels, respectively, DAPT may be useful in the study of β-amyloid (Aβ) formation. It is shown to cause a reduction in Aβ40 and Aβ42 levels in human primary neuronal cultures and in brain extract, cerebrospinal fluid and plasma in vivo.
Purity: Greater than 99% as determined by LC/MS analysis. LC/MS and/or NMR data available upon request.
Biological Activity: In a cell-based assay measuring the activation of the Notch pathway reporter gene, this compound gave IC50 of 500 nM.