DAPT

Pricing Availability Delivery Time Qty
Cat.No. 2634 - DAPT | C23H26F2N2O4 | CAS No. 208255-80-5
Description: γ-secretase inhibitor
Chemical Name: N-[(3,5-Difluorophenyl)acetyl]-L-alanyl-2-phenyl]glycine-1,1-dimethylethyl ester
Purity: ≥99% (HPLC)
Datasheet
Citations (26)
Literature

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.

Compound Libraries

DAPT is also offered as part of the Tocriscreen Plus and Tocriscreen Stem Cell Toolbox. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 432.46
Formula C23H26F2N2O4
Storage Store at +4°C
Purity ≥99% (HPLC)
CAS Number 208255-80-5
PubChem ID 5311272
InChI Key DWJXYEABWRJFSP-XOBRGWDASA-N
Smiles CC(C)(C)OC([C@H]([C@]2=CC=CC=C2)NC([C@H](C)NC(CC1=CC(F)=CC(F)=C1)=O)=O)=O

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 43.24 100

Preparing Stock Solutions

The following data is based on the product molecular weight 432.46. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.31 mL 11.56 mL 23.12 mL
5 mM 0.46 mL 2.31 mL 4.62 mL
10 mM 0.23 mL 1.16 mL 2.31 mL
50 mM 0.05 mL 0.23 mL 0.46 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

Dovey et al (2001) Functional gamma-secretase inhibitors reduce beta-amyloid peptide levels in brain. J.Neurochem. 76 173 PMID: 11145990

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 3498 PMID: 16030192

Crawford and Roelink (2007) The notch response inhibitor DAPT enhances neuronal differentiation in embryonic stem cell-derived embryoid bodies independently of sonic hedgehog signaling. Dev.Dyn. 236 886 PMID: 17295317


If you know of a relevant reference for DAPT, please let us know.

View Related Products by Product Action

View all γ-Secretase Inhibitors

Keywords: γ-secretase gamma-secretase inhibitors inhibits reduces Aβ4 β42 beta42 levels Proteinases Proteases β-Amyloid beta-Amyloid b-amyloid Precursor Protein APP beta Peptides amyloidbeta amyloidb amyloidβ organoids Gamma-Secretase

26 Citations for DAPT

Citations are publications that use Tocris products. Selected citations for DAPT include:

Scheppke et al (2012) Notch promotes vascular maturation by inducing integrin-mediated smooth muscle cell adhesion to the endothelial basement membrane. Cell Stem Cell 119 2149 PMID: 22134168

Valdez et al (2012) Notch and TGFβ form a reciprocal positive regulatory loop that suppresses murine prostate basal stem/progenitor cell activity. RNA Biol 11 676 PMID: 23122291

Bejjani and Hammarlund (2012) Notch signaling inhibits axon regeneration. PLoS One 73 268 PMID: 22284182

Berndt et al (2011) Mindbomb 1, an E3 ubiquitin ligase, forms a complex with RYK to activate Wnt/β-catenin signaling. J Cell Biol 194 737 PMID: 21875946

Kolegraff et al (2011) Characterization of full-length and proteolytic cleavage fragments of desmoglein-2 in native human colon and colonic epithelial cell lines. Cell Adh Migr 5 306 PMID: 21715983

Kim et al (2010) Group II metabotropic glutamate receptor stimulation triggers production and release of Alzheimer's amyloid(β)42 from isolated intact nerve terminals. Neuron 30 3870 PMID: 20237257

Schumacher (2017) ErbB4 signaling stimulates pro-inflammatory macrophage apoptosis and limits colonic inflammation. Cell Death Dis 8 e2622 PMID: 28230865

Lu et al (2016) Generation of serotonin neurons from human pluripotent stem cells. Nat Biotechnol 34 89 PMID: 26655496

Campbell et al (2016) Canonical Notch signaling plays an instructive role in auditory supporting cell development. Zoological Lett 6 19484 PMID: 26786414

Guest et al (2016) Notch3 drives development and progression of cholangiocarcinoma Proc Natl Acad Sci U S A. 113 12250 PMID: 27791012

Kerr et al (2015) A small molecule targeting ALK1 prevents Notch cooperativity and inhibits functional angiogenesis. Angiogenesis 18 209 PMID: 25557927

Wang et al (2015) Generation of clinical-grade human induced pluripotent stem cells in Xeno-free conditions. Stem Cell Res Ther 6 223 PMID: 26564165

Edri et al (2015) Analysing human neural stem cell ontogeny by consecutive isolation of Notch active neural progenitors. Nat Commun 6 6500 PMID: 25799239

Gomez et al (2015) Neurogenin 3 Expressing Cells in the Human Exocrine Pancreas Have the Capacity for Endocrine Cell Fate. Sci Rep 10 e0133862 PMID: 26288179

Onai et al (2015) On the origin of vertebrate somites. Blood 1 33 PMID: 26613046

Hammond et al (2014) Astrocyte-derived endothelin-1 inhibits remyelination through notch activation. Neuron 81 588 PMID: 24507193

Greife et al (2014) Canonical Notch signalling is inactive in urothelial carcinoma. BMC Cancer 14 628 PMID: 25167871

Gioia et al (2014) Mir-23a and mir-125b regulate neural stem/progenitor cell proliferation by targeting Musashi1. Anticancer Res 11 1105 PMID: 25483045

Sundvik et al (2013) Presenilin1 regulates histamine neuron development and behavior in zebrafish, danio rerio. J Neurosci 33 1589 PMID: 23345232

Kirkeby et al (2013) Generating regionalized neuronal cells from pluripotency, a step-by-step protocol. Front Cell Neurosci 6 64 PMID: 23316134

Díaz et al (2013) Notch increases the shedding of HB-EGF by ADAM12 to potentiate invadopodia formation in hypoxia. J Cell Biol 201 279 PMID: 23589494

Du et al (2013) Inflammation-mediated notch signaling skews fanconi anemia hematopoietic stem cell differentiation. J Immunol 191 2806 PMID: 23926327

Shah et al (2013) The role of Notch and γ-secretase inhibition in an ovarian cancer model. J Neurosci 33 801 PMID: 23482747

Boulter et al (2012) Macrophage-derived Wnt opposes Notch signaling to specify hepatic progenitor cell fate in chronic liver disease. Nat Med 18 572 PMID: 22388089

Hu et al (2012) Fibulin-3 promotes glioma growth and resistance through a novel paracrine regulation of Notch signaling. Cancer Res 72 3873 PMID: 22665268

Campos et al (2012) Opposing effects of bacitracin on human papillomavirus type 16 infection: enhancement of binding and entry and inhibition of endosomal penetration. J Virol 86 4169 PMID: 22345461


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Pathways for DAPT

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