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

Overview

Key Specifications Table

CAS #Empirical Formula
209986-17-4C₂₇H₂₄F₂N₄O₃

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565790-1MG
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      Glass bottle 1 mg
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      565790-500UG
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          Plastic ampoule 500 μg
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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
          Catalog Number GTIN
          565790-1MG 04055977191851
          565790-500UG 04055977191868