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DAPT [Amyloid-β (Aβ); Aβ42 Inhibitor]

[CAT#: MOD2005ZP78]

γ-secretase inhibitor. Classical notch inhibitor. Induces neuronal differentiation

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Description
DAPT is a γ-secretase inhibitor that blocks Notch signaling. It is a classic notch inhibitor. According to reports, although low-dose inhibition of amyloid β (Aβ), in cell culture and animal models, Aβ production has increased.

DAPT is used for various stem cell applications.
It has been shown that when used in combination with other small molecules that inhibit SMAD (SB 431542, LDN193189), activation of WNT (CHIR99021) and inhibition of FGF signaling (SU5402), DAPT produces 75% of post-mitotic neurons in the 11 days after differentiation. These are defined as peripheral sensory neurons.

The combination of DAPT with LDN193189, SB431542, XAV939, PD0325901 and SU5402 has been shown to accelerate the induction of cortical neurons with mature electrophysiological properties on the 16th day of differentiation.

DAPT It also enhances neuronal differentiation in ESC-derived embryoid bodies regardless of Hh signaling.

In addition, the compound promotes cardiac differentiation of murine pluripotent stem cells and enhances the reprogramming of mouse fibroblasts to iCLM (induced cardiac-like myocytes).
Synonyms
GSI-IX
Chemical Name
N-[N-(3,5-Difluorophenacetyl-L-alanyl)]-S-phenylglycine tbutyl ester
Modulator Type
Inhibitor
Relevant Disease
Neurological Disorders
Assay Description
DAPT inhibits Aβ production by more than 90%, and only affects a moderate decrease of APPβ in the medium. Although treatment with DAPT can reduce APPβ by about 30%, this effect is not concentration-dependent, and can be reversed by removing DAPT [1]. CNE-2 cells were treated with increasing concentrations of DAPT (0, 25, 50, and 75 μM), and the Notch 1 fragment Val1744-NICD produced by γ-secretase was reduced in a dose-dependent manner after 48 hours (P<0.01). At a concentration of 50 μM, DAPT almost completely inhibited the activation of γ-secretase [3].
Reference
[1]. Dovey HF, et al. Functional gamma-secretase inhibitors reduce beta-amyloid peptide levels in brain. J Neurochem. 2001 Jan;76(1):173-81.

[2]. Li S, et al. DAPT protects brain against cerebral ischemia by down-regulating the expression of Notch 1 and nuclear factor κB in rats. Neurol Sci. 2012 Dec;33(6):1257-64.

[3]. Zhou JX, et al. γ-secretase inhibition combined with cisplatin enhances apoptosis of nasopharyngeal carcinoma cells.Exp Ther Med. 2012 Feb;3(2):357-361.
Assay Description
DAPT was given to PDAPP mice (100 mg/kg s.c.), and the levels of DAPT and Aβ in the cerebral cortex were checked. At 3 hours after treatment, the DAPT peak in the brain reached 490 ng/g, and continued to maintain levels above 100 ng/g (~200 nM) during the first 18 hours. These concentrations of DAPT in the brain exceed their IC50 levels, thereby reducing Aβ (115 nM) in neuronal cultures, and have strong and maintain efficacy [1]. DAPT protects the brain from cerebral ischemia by down-regulating the expression of Notch 1 and nuclear factor kappa B in rats. Western blot analysis also showed that the expression of Notch 1 and NF-κB in the DAPT group (0.03 mg/kg) decreased significantly (P <0.05 vs. MCAO group) [2].
References
[1]. Dovey HF, et al. Functional gamma-secretase inhibitors reduce beta-amyloid peptide levels in brain. J Neurochem. 2001 Jan;76(1):173-81.

[2]. Li S, et al. DAPT protects brain against cerebral ischemia by down-regulating the expression of Notch 1 and nuclear factor κB in rats. Neurol Sci. 2012 Dec;33(6):1257-64.
Molecular Weight
432.5
Form
Powder
Chemical Formula
C23H26F2N2O4
Source
Synthetic
SMILES
C[C@@H](C(=O)N[C@@H](C1=CC=CC=C1)C(=O)OC(C)(C)C)NC(=O)CC2=CC(=CC(=C2)F)F
Solubility
Soluble in DMSO (100mM)
IC50
15 nM (Aβ), 200 nM (Aβ42)
CAS NO.
208255-80-5
PubChem Substance ID
5311272
Purity
>98%
Shipping
Room Temperature
Handling Advice
For obtaining a higher solubility, please warm the tube at 37 °C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -32°C for several months.
Research Use Only
For research use only

For Research Use Only. Not For Clinical Use.
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