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DAPT | gamma-secretase inhibitor

DAPT (208255-80-5)is an inhibitor of γ-secretase (IC50 in human primary neurons = 115 nM for total Aβ or 200 nM for Aβ42 specifically)1. Oral administration of DAPT has been shown to reduce levels of Aβ in brain extract, cerebrospinal fluid and plasma from mice and rats.2,3 DAPT blocks Notch signaling which promotes neuronal differentiation of precursor cells.4 Enhances iPS cells without oncogenes KLF4 and CMYC5. Cell permeable.

References/Citations
1) Dovey et al. (2001), Functional gamma-secretase inhibitors reduce beta-amyloid peptide levels in brain; J. Neurochem., 76 173
2) Portelius et al. (2009), Effects of γ-secretase inhibition on the amyloid β isoform pattern in a mouse model of Alzheimer's disease; Cell Signal., 5 615
3) El Moueddon et al. (2006), Reduction of Aβ levels in the Sprague Dawley rat after oral administration of the functional γ-secretase inhibitor, DAPT: a novel non-transgenic model for Aβ production inhibitors; Curr. Pharma. Des., 12 1671
4) De Smedt et al. (2005), Different thresholds of notch signaling bias human precursor cells towards B-, NK-, monocytic/dendritic, or T-cell lineage in thymus microenvironment
; Blood, 106 2236
5) Ichida et al. (2014), Notch inhibition allows oncogene-independent generation of iPS cells; Nature Chem. Biol., 10 632

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Catalog#  10-4514

$60.00
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Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee.
 
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CAS:
208255-80-5
Catalog Number:
10-4514
Activity:
γ-secretase inhibitor
Alternate Names:
LY-374973
Chemical Name:
N-[N-(3,5-Difluorophenacetyl)-L-alanyl]-S-phenylglycine t-butyl ester
Molecular Weight:
432.46
Molecular Formula:
C23H26F2N2O4
Solubility:
Soluble in DMSO (up to 18 mg/ml).
Physical Properties:
White solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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