565770 γ-Secretase Inhibitor IX - CAS 208255-80-5 - Calbiochem

565770
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Overview

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Key Spec Table

Empirical FormulaCAS #
C₂₃H₂₆F₂N₂O₄208255-80-5

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565770-5MGCN
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      Glass bottle 5 mg
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      Description
      OverviewA cell-permeable dipeptide that suppresses Aβ production by blocking γ-secretase (Aβtotal IC50 = 115 nM, Aβ42 IC50 = 200 nM). Prevents Aβ34 generation in murine N2a cells and hAPP/hBACE-1 transfected human HEK 293 cells. Reported to be functionally active in both HEK 293 cells and neuronal cultures without affecting the secretion of amyloid-β precursor protein (APP). Also shown to lower Aβ levels acutely in APP-transgenic mice. Reported to reduce extracellular Aβ plaques and intracellular Aβ accumulation in 3xTgAD transgenic mice. A 25 mM (5 mg/462 µl) solution of γ-Secretase Inhibitor IX (Cat. No. 565784) in DMSO is also available.
      Catalogue Number565770
      Brand Family Calbiochem®
      SynonymsDAPT, N-[N-(3,5-Difluorophenacetyl-L-alanyl)]-S-phenylglycine t-Butyl Ester
      References
      ReferencesMorohashi, Y., et al. 2006. J. Bio. Chem. Vol. 281, 14670.
      Nishitomo, K. et al. 2006 J. Neurochem. 99, 1555.
      Oddo, S., et al. 2004. Neuron 43, 321.
      Dovey, H.F., et al. 2001. J. Neurochem. 76, 173.
      Sastre, M., et al. 2001. EMBO Rep. 2, 835.
      Vandermeeren, M., et al. 2001. Neurosci. Lett. 315, 145.
      Product Information
      CAS number208255-80-5
      ATP CompetitiveN
      FormLyophilized
      Hill FormulaC₂₃H₂₆F₂N₂O₄
      Chemical formulaC₂₃H₂₆F₂N₂O₄
      ReversibleN
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary Targettotal
      Primary Target IC<sub>50</sub>115 nM suppressing Aβtotal production; 200 nM suppressing Aβ42 production
      Purity≥98% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage -20°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      γ-Secretase Inhibitor IX - CAS 208255-80-5 - Calbiochem Certificates of Analysis

      TitleLot Number
      565770

      References

      Reference overview
      Morohashi, Y., et al. 2006. J. Bio. Chem. Vol. 281, 14670.
      Nishitomo, K. et al. 2006 J. Neurochem. 99, 1555.
      Oddo, S., et al. 2004. Neuron 43, 321.
      Dovey, H.F., et al. 2001. J. Neurochem. 76, 173.
      Sastre, M., et al. 2001. EMBO Rep. 2, 835.
      Vandermeeren, M., et al. 2001. Neurosci. Lett. 315, 145.

      Citations

      Title
    • Yunzhou Dong, et al. (2006) Calpain inhibitor MDL28170 modulates Aβ formation by inhibiting the formation of intermediate Aβ46 and protecting Aβ from degradation. FASEB Journal in press,.
    • Aurelie Olivier, et al. (2005) The Notch ligand delta-1 is a hematopoietic development co- factor for plasmacytoid dendritic cells. Blood 107, 2694-2701.
    • Data Sheet

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision12-November-2007 JSW
      SynonymsDAPT, N-[N-(3,5-Difluorophenacetyl-L-alanyl)]-S-phenylglycine t-Butyl Ester
      DescriptionA cell-permeable dipeptide that inhibits γ-secretase activity and suppresses Aβ production (Aβ total IC50 = 115 nM; Aβ42 IC50 = 200 nM). Reported to be functionally active in both HEK293 cells overexpressing human APP751 and neuronal cultures, however, it does not affect the secretion of amyloid-b precursor protein (APP). Effective in acutely lowering Ab in APPV717F-transgenic mice. Also effective in inhibiting the production of an ~6 kDa C-terminal cleavage product (CTFg) in HEK293 cells stably transfected with the Swedish mutant, βAPP695. Reported to reduce extracellular Aβ plaques and intracellular Aβ accumulation in 3xTgAD transgenic mice.
      FormLyophilized
      Intert gas (Yes/No) Packaged under inert gas
      CAS number208255-80-5
      Chemical formulaC₂₃H₂₆F₂N₂O₄
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (20 mg/ml)
      Storage -20°C
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesMorohashi, Y., et al. 2006. J. Bio. Chem. Vol. 281, 14670.
      Nishitomo, K. et al. 2006 J. Neurochem. 99, 1555.
      Oddo, S., et al. 2004. Neuron 43, 321.
      Dovey, H.F., et al. 2001. J. Neurochem. 76, 173.
      Sastre, M., et al. 2001. EMBO Rep. 2, 835.
      Vandermeeren, M., et al. 2001. Neurosci. Lett. 315, 145.
      Citation
    • Yunzhou Dong, et al. (2006) Calpain inhibitor MDL28170 modulates Aβ formation by inhibiting the formation of intermediate Aβ46 and protecting Aβ from degradation. FASEB Journal in press,.
    • Aurelie Olivier, et al. (2005) The Notch ligand delta-1 is a hematopoietic development co- factor for plasmacytoid dendritic cells. Blood 107, 2694-2701.