Catalog Number: 2634
Chemical Name: N-[(3,5-Difluorophenyl)acetyl]-L-alanyl-2-phenyl]glycine-1,1-dimethylethyl ester
Biological Activity
Inhibitor of γ-secretase; causes a reduction in Aβ40 and Aβ42 levels in human primary neuronal cultures (IC50 values are 115 and 200 nM for total Aβ and Aβ42 respectively) and in brain extract, cerebrospinal fluid and plasma in vivo. Does not affect APPα and APPβ levels. Blocks Notch signaling in hybrid human-mouse fetal thymus organ culture (FTOC). Activity causes ESCs to commit to neuronal differentiation.
Technical Data
  • M.Wt:
    432.46
  • Formula:
    C23H26F2N2O4
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
    >99%
  • Storage:
    Store at +4°C
  • CAS No:
    208255-80-5
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Functional gamma-secretase inhibitors reduce beta-amyloid peptide levels in brain.
    Dovey et al.
    J.Neurochem., 2001;76:173
  2. Different thresholds of notch signaling bias human precursor cells towards B-, NK-, monocytic/dendritic, or T-cell lineage in thymus microenvironment.
    De Smedt et al.
    Blood, 2005;106:3498
  3. The notch response inhibitor DAPT enhances neuronal differentiation in embryonic stem cell-derived embryoid bodies independently of sonic hedgehog signaling.
    Crawford and Roelink
    Dev.Dyn., 2007;236:886
Citations:

The citations listed below are publications that use Tocris products. Selected citations for DAPT include:

27 Citations: Showing 1 - 10
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  1. ErbB4 signaling stimulates pro-inflammatory macrophage apoptosis and limits colonic inflammation.
    Authors: Schumacher
    Cell Death Dis 2017;8:e2622
  2. A modular platform for differentiation of human PSCs into all major ectodermal lineages.
    Authors: Tchieu Et al.
    Cell Stem Cell 2017;21:399
  3. Canonical Notch signaling plays an instructive role in auditory supporting cell development.
    Authors: Campbell Et al.
    Zoological Lett 2016;6:19484
  4. Generation of serotonin neurons from human pluripotent stem cells.
    Authors: Lu Et al.
    Nat Biotechnol 2016;34:89
  5. Notch3 drives development and progression of cholangiocarcinoma
    Authors: Guest Et al.
    Proc Natl Acad Sci U S A. 2016;113:12250
  6. Analysing human neural stem cell ontogeny by consecutive isolation of Notch active neural progenitors.
    Authors: Edri Et al.
    Nat Commun 2015;6:6500
  7. Generation of clinical-grade human induced pluripotent stem cells in Xeno-free conditions.
    Authors: Wang Et al.
    Stem Cell Res Ther 2015;6:223
  8. On the origin of vertebrate somites.
    Authors: Onai Et al.
    Blood 2015;1:33
  9. A small molecule targeting ALK1 prevents Notch cooperativity and inhibits functional angiogenesis.
    Authors: Kerr Et al.
    Angiogenesis 2015;18:209
  10. Neurogenin 3 Expressing Cells in the Human Exocrine Pancreas Have the Capacity for Endocrine Cell Fate.
    Authors: Gomez Et al.
    Sci Rep 2015;10:e0133862
  11. Astrocyte-derived endothelin-1 inhibits remyelination through notch activation.
    Authors: Hammond Et al.
    Neuron 2014;81:588
  12. Canonical Notch signalling is inactive in urothelial carcinoma.
    Authors: Greife Et al.
    BMC Cancer 2014;14:628
  13. Mir-23a and mir-125b regulate neural stem/progenitor cell proliferation by targeting Musashi1.
    Authors: Gioia Et al.
    Anticancer Res 2014;11:1105
  14. Generating regionalized neuronal cells from pluripotency, a step-by-step protocol.
    Authors: Kirkeby Et al.
    Front Cell Neurosci 2013;6:64
  15. The role of Notch and γ-secretase inhibition in an ovarian cancer model.
    Authors: Shah Et al.
    J Neurosci 2013;33:801
  16. Presenilin1 regulates histamine neuron development and behavior in zebrafish, danio rerio.
    Authors: Sundvik Et al.
    J Neurosci 2013;33:1589
  17. Notch increases the shedding of HB-EGF by ADAM12 to potentiate invadopodia formation in hypoxia.
    Authors: Díaz Et al.
    J Cell Biol 2013;201:279
  18. Inflammation-mediated notch signaling skews fanconi anemia hematopoietic stem cell differentiation.
    Authors: Du Et al.
    J Immunol 2013;191:2806
  19. Opposing effects of bacitracin on human papillomavirus type 16 infection: enhancement of binding and entry and inhibition of endosomal penetration.
    Authors: Campos Et al.
    J Virol 2012;86:4169
  20. Notch signaling inhibits axon regeneration.
    Authors: Bejjani and Hammarlund
    PLoS One 2012;73:268
  21. Fibulin-3 promotes glioma growth and resistance through a novel paracrine regulation of Notch signaling.
    Authors: Hu Et al.
    Cancer Res 2012;72:3873
  22. Macrophage-derived Wnt opposes Notch signaling to specify hepatic progenitor cell fate in chronic liver disease.
    Authors: Boulter Et al.
    Nat Med 2012;18:572
  23. Notch and TGFβ form a reciprocal positive regulatory loop that suppresses murine prostate basal stem/progenitor cell activity.
    Authors: Valdez Et al.
    RNA Biol 2012;11:676
  24. Notch promotes vascular maturation by inducing integrin-mediated smooth muscle cell adhesion to the endothelial basement membrane.
    Authors: Scheppke Et al.
    Cell Stem Cell 2012;119:2149
  25. Characterization of full-length and proteolytic cleavage fragments of desmoglein-2 in native human colon and colonic epithelial cell lines.
    Authors: Kolegraff Et al.
    Cell Adh Migr 2011;5:306
  26. Mindbomb 1, an E3 ubiquitin ligase, forms a complex with RYK to activate Wnt/β-catenin signaling.
    Authors: Berndt Et al.
    J Cell Biol 2011;194:737
  27. Group II metabotropic glutamate receptor stimulation triggers production and release of Alzheimer's amyloid(β)42 from isolated intact nerve terminals.
    Authors: Kim Et al.
    Neuron 2010;30:3870
Expand to show all 27 Citations

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