Inhibitor of γ-secretase
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Contained In
44676Hepatocyte Maintenance Reagent Set
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DAPT

Item No. 13197

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[2S-(3,5-difluorophenyl)acetyl]-L-alanyl-2-phenyl-glycine, 1,1-dimethylethyl ester
CAS Number
208255-80-5
Synonyms
  • GSI-IX
Molecular Formula
C23H26F2N2O4
Formula Weight
432.5
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMF:PBS (pH 7.2) (1:9): 0.1 mg/mlDMSO: 25 mg/mlEthanol: 1 mg/ml
SMILES
Fc1cc(F)cc(c1)CC(=O)N[C@@H](C)C(=O)N[C@@H](c1ccccc1)C(=O)OC(C)(C)C
InChi Code
InChI=1S/C23H26F2N2O4/c1-14(26-19(28)12-15-10-17(24)13-18(25)11-15)21(29)27-20(16-8-6-5-7-9-16)22(30)31-23(2,3)4/h5-11,13-14,20H,12H2,1-4H3,(H,26,28)(H,27,29)/t14-,20-/m0/s1
InChi Key
DWJXYEABWRJFSP-XOBRGWDASA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $65

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    10 mg

    $117

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    25 mg

    $212

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    50 mg

    $390

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    Product Description

    DAPT is an inhibitor of γ-secretase, blocking the production of total Aβ in human primary neuronal cultures with an IC50 value of 115 nM and Aβ42 with an IC50 value of 200 nM.1 DAPT is also effective in vivo, reducing brain levels of Aβ when given orally to mice that are transgenic for human APPV717F or to rats.1,2,3 Through its effects on γ-secretase, DAPT indirectly inhibits Notch, affecting cell signaling and cell differentiation.4,5 This product is also available as part of Cayman's Hepatocyte Maintenance Reagent Kit (Item No. 44676).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Dovey, H.F., John, V., Anderson, J.P., et al. Functional γ-secretase inhibitors reduce β-amyloid peptide levels in brain. J. Neurochem. 76(1), 173-181 (2001).

    2. Portelius, E., Zhang, B., Gustavsson, M.K., et al. Effects of γ-secretase inhibition on the amyloid β isoform pattern in a mouse model of Alzheimer’s disease. Neurodegener.Dis. 6, 258-262 (2009).

    3. El Mouedden, M., Vandermeeren, M., Meert, T., et al. 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. Pharm. Des. 12, 671-676 (2006).

    4. Kanungo, J., Zheng, Y.L., Amin, N.D., et al. The Notch signaling inhibitor DAPT down-regulates cdk5 activity and modulates the distribution of neuronal cytoskeletal proteins. J. Neurochem. 106, 2236-2248 (2008).

    5. De Smedt, M., Hoebeke, I., Reynvoet, K., et al. Different thresholds of Notch signaling bias human precursor cells toward B-, NK-, monocytic/dendritic-, or T-cell lineage in thymus microenvironment. Blood 106(10), 3498-3506 (2005).