Biological Activity
DAPT is a functional γ-secretase inhibitor and significantly reduces the production of total Aβ and Aβ42 in human primary neuronal cultures (IC50= 115 nM for total Aβ, IC50= 200 nM for Aβ42) [1], as well as in brain extract, CSF, and the plasma in vivo dose- and time-dependently [2]. DAPT efficiently blocks Notch signaling in hybrid human-mouse fetal thymus organ culture (FTOC) [3]. DAPT decreases lymphoproliferation in CBA-lpr mice and autoimmunity in MRL-lpr mice. By using a novel intermittent low-dose schedule, DAPT is well tolerated for months and the reported side effects of γ-secretase inhibitor are avoided [4]. DAPT-mediated suppression of Notch response enhances neuronal differentiation in ESCs-derived embryoid bodies (EBs) independently of SHH signaling [5].
Chemical Properties
| Cas No.: 208255-80-5 | M. Wt.: 432.46 |
| Formula: C23H26F2N2O4 | Purity: >98.5% |
| Synonym: GSI-IX, LY-374973 | |
| Chemical Name: N-[N-(3,5-difluorophenacetyl)-l-alanyl]-S-phenylglycine t-butyl ester | |
| Appearance: White solid | |
| Solubility: Soluble in DMSO (85 mg/mL) and in ethanol (50 mg/mL). Slightly soluble in water (<1 mg/ml). | |
| Storage: Store solid at -20 ºC for the stability of two years | |
