DAPTA potent and specific inhibitor of γ-secretase

DAPT (CAS 208255-80-5)

DAPT | CAS 208255-80-5 is rated 5.0 out of 5 by 2.
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Synonym: Gamma-Secretase Inhibitor IX;N-[N-(3,5-Difluorophenacetyl-L-alanyl)]-S-phenylglycine t-butyl ester
Application: A potent and specific inhibitor of γ-secretase
CAS Number: 208255-80-5
Purity: ≥95%
Molecular Weight: 432.46
Molecular Formula: C23H26F2N2O4
* Refer to Certificate of Analysis for lot specific data (including water content).
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DAPT is a potent and specific inhibitor of γ-secretase. It has been shown to cause a reduction in Aβ40 and Aβ42 levels in human primary neuronal cultures (IC50 values are 115 and 200 nM for total Aβ40 and Aβ42 respectively). There is evidence that DAPT does not effect APPα and APPβ levels. It mimics notch signaling deficiencies at morphological, molecular and biochemical levels and has been shown to block notch signaling in hybrid human-mouse foetal thymus organ culture (FTOC).


References

1. Dovey, H F., et al., 2001. Functional gamma-secretase inhibitors reduce beta-amyloid peptide levels in brain. Journal of neurochemistry. 76(1): 173-81. PMID: 11145990
2. Geling, Andrea., et al., 2002. A gamma-secretase inhibitor blocks Notch signaling in vivo and causes a severe neurogenic phenotype in zebrafish. EMBO reports. 3(7): 688-94. PMID: 12101103
3. Lanz, Thomas A., et al., 2003. The gamma-secretase inhibitor N-[N-(3,5-difluorophenacetyl)-L-alanyl]-S-phenylglycine t-butyl ester reduces A beta levels in vivo in plasma and cerebrospinal fluid in young (plaque-free) and aged (plaque-bearing) Tg2576 mice. The Journal of pharmacology and experimental therapeutics. 305(3): 864-71. PMID: 12626636
4. Gowrishankar, Kavitha., et al., 2004. Release of a membrane-bound death domain by gamma-secretase processing of the p75NTR homolog NRADD. Journal of cell science. 117(Pt 18): 4099-111. PMID: 15280425
5. De Smedt, Magda., et al., 2005. Different thresholds of Notch signaling bias human precursor cells toward B-, NK-, monocytic/dendritic-, or T-cell lineage in thymus microenvironment. Blood. 106(10): 3498-506. PMID: 16030192
6. El Mouedden, Mohammed., et al., 2006. Reduction of Abeta levels in the Sprague Dawley rat after oral administration of the functional gamma-secretase inhibitor, DAPT: a novel non-transgenic model for Abeta production inhibitors. Current pharmaceutical design. 12(6): 671-6. PMID: 16472156

Usage :
DAPT is soluble in DMSO.
Appearance :
Powder
Physical State :
Solid
Solubility :
Soluble in DMSO (15 mg/mL), ethanol (~1 mg/mL), dichloromethane, DMF (~25 mg/mL), and 1:9 solution of DMF:PBS(pH 7.2) (~0.1 mg/mL).
Storage :
Store at -20° C
Boiling Point :
~612.2° C at 760 mmHg (Predicted)
Density :
~1.2 g/cm3 (Predicted)
Refractive Index :
n20D 1.53 (Predicted)
IC50 :
total Aβ: IC50 = 115 nM (human); Aβ42: IC50 = 200 nM (human)
pK Values :
pKa: 12.82 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
5311272
MDL Number :
MFCD04974585
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

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Certificate of Analysis

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DAPT  Product Citations

See how others have used DAPT. Click on the entry to view the PubMed entry .

Citations 1 to 10 of 29 total

PMID: # 30839137  Niu, Y. et al. 2019. Cell Biol. Int.

PMID: # 30951821  Bruno, A. et al. 2019. Biochim Biophys Acta Mol Basis Dis. 1865: 1642-1650.

PMID: # 29636838  Yu, L. et al. 2018. Oxid Med Cell Longev. 2018: 2750695.

PMID: # 29286081  Liu, Z. et al. 2018. Int. J. Mol. Med. 41: 1560-1572.

PMID: # 29345284  Li, L. et al. 2018. Int. J. Oncol. 52: 473-484.

PMID: # 29393429  Chen, DW. et al. 2018. Mol Med Rep. 17: 4965-4972.

PMID: # 28771710  Lee, ML. et al. 2017. J. Neurochem.

PMID: # 26523864  Zhao, E. et al. 2016. Nat. Immunol. 17: 95-103.

PMID: # 26648098  Gao, Y. et al. 2016. International journal of oncology. 48: 281-92.

PMID: # 27901069  Mariscal, J. et al. 2016. Sci Rep. 6: 37820.

Citations 1 to 10 of 29 total

Is this chemical cell permeable?

Asked by: Diniz
Yes, sc-201315/A is cell permeable. Please refer to the below below reference. Dovey, H F., et al., 2001. Functional gamma-secretase inhibitors reduce beta-amyloid peptide levels in brain. Journal of neurochemistry. 76(1): 173-81. PMID: 11145990 https://www.ncbi.nlm.nih.gov/pubmed/?term=11145990
Answered by: Technical Support
Date published: 2019-03-22

What are the shipping conditions?

Asked by: SCchem16
Thank you for your question. This chemical, DAPT: sc-201315, ships via ambient temperature.
Answered by: Chemical Support 2
Date published: 2017-03-06

Does this chemical inhibit any other targets besides y-secretase?

Asked by: SCchem16
Thank you for your question. This chemical, DAPT (CAS 208255-80-5), also indirectly inhibits Notch which is a γ-secretase substrate.
Answered by: Chemical Support 2
Date published: 2017-03-06
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Rated 5 out of 5 by from γ-secretase inhibitor A potent and specific inhibitor of γ-secretase. a good positive in γ-secretase research.
Date published: 2016-11-18
Rated 5 out of 5 by from Chen et al Chen et al. (PubMed ID 20145246) used the -secretase inhibitor DAPT to elevate the level of -amyloid precursor protein (APP) C-terminal fragments (CTF). -SCBT Publication Review
Date published: 2015-01-03
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