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565790 γ-Secretase Inhibitor XXI, Compound E - CAS 209986-17-4 - Calbiochem

This g-secretase inhibitor, CAS 209986-17-4, is a cell-permeable, potent, selective, non-transition-state analog inhibitor of γ-secretase and Notch processing. Lowers Aβ levels in APP transgenic mice

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: (S,S)- 2-[2-(3,5-Difluorophenyl)-acetylamino]-N-(1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)-propionamide, Compound E

Primary Target: γ-secretase and Notch processing Ab40 in CHO cells overexpressing wild type bAPP
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565790
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Overview

Key Spec Table

CAS #Empirical Formula
209986-17-4C₂₇H₂₄F₂N₄O₃

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      Description
      OverviewA cell-permeable, potent, selective, peptidomimetic, non-transition-state analog inhibitor of γ-secretase and Notch processing (IC50 = 300 pM for Aβ40 in CHO cells overexpressing wild type βAPP; 240 pM for Aβ40, 370 pM for Aβ42, and 320 pM for NICD, respectively, in HEK293 cells stably transfected with βAPP695 and mNotchΔE(M1727V); 100 pM for both Aβ40 and Aβ42 in SH-SY5Y cells stably transfected with SPA4CT). Lowers Aβ levels in several APP transgenic mouse models. Reported to bind to presenilins and suppress the proteolytic cleavage of transmembrane protein substrates, including APLP1 and APLP2, CD44, ErbB4, E-cadherin, low density lipoprotein receptor-related proteins, Notch ligands, and p75NTR. Only weakly affects presenilinase activity at much higher concentrations (200-400 µM).
      Catalogue Number565790
      Brand Family Calbiochem®
      Synonyms(S,S)- 2-[2-(3,5-Difluorophenyl)-acetylamino]-N-(1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)-propionamide, Compound E
      References
      ReferencesMilano, J., et al. 2004. Toxicol. Sci. 82, 341.
      Jung, K.M., et al. 2003. J. Biol. Chem. 278, 42161.
      Murakami, D., et al. 2003. Oncogene 22, 1511.
      Campbell, W.A., et al. 2003. J. Neurochem. 85, 1563.
      Berechid, B.E., et al., 2002. J. Biol. Chem. 277, 8154.
      Lee, H.J., et al. 2002. J. Biol. Chem. 277, 6318.
      May, P., et al. 2002. J. Biol. Chem. 277, 18736.
      Scheinfeld, M.H., et al. 2002. J. Biol. Chem. 277, 44195.
      Ni, C. Y., et al. 2001. Science 294, 2179.
      Beher, D., et al. 2001. J. Biol. Chem. 276, 45394.
      Doerfler, P., et al. 2001. Proc. Natl. Acad. Sci. USA 98, 9312.
      Seiffert, D., et al. 2000. J. Biol. Chem. 275, 34086.
      Product Information
      CAS number209986-17-4
      ATP CompetitiveN
      FormWhite solid
      Hill FormulaC₂₇H₂₄F₂N₄O₃
      Chemical formulaC₂₇H₂₄F₂N₄O₃
      ReversibleN
      Structure formula ImageStructure formula Image
      Biological Information
      Primary Targetγ-secretase and Notch processing Ab40 in CHO cells overexpressing wild type bAPP
      Primary Target IC<sub>50</sub>300 pM for Aβ40 in CHO cells overexpressing wild typeβAPP; 240 pM for Aβ40, 370 pM for Aβ42, and 320 pM for NICD, respectively, in HEK293 cells stably transfected with βAPP695 and mNotchΔE(M1727V); 100 pM for both Aβ40
      Purity≥95% by HPLC
      Physicochemical Information
      Cell permeableY
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°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 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Global Trade Item Number
      Catalogue Number GTIN
      565790-1MG 04055977191851