Notch 信號(hào)通路廣泛存在于脊椎動(dòng)物和非脊椎動(dòng)物,在進(jìn)化上高度保守,通過相鄰細(xì)胞之間的相互作用調(diào)節(jié)細(xì)胞、組織、器官的分化和發(fā)育。Notch信號(hào)通路由 Notch受體、Notch配體(DSL蛋白)、CSL (CBF-1,Suppressor of hairless,Lag的合稱)DNA結(jié)合蛋白、其他的效應(yīng)物和Notch的調(diào)節(jié)分子等組成。
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.