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

565790
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Key Spec Table

Empirical FormulaCAS #
C₂₇H₂₄F₂N₄O₃209986-17-4

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565790-1MGCN
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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
      Quality LevelMQ100
      Applications
      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
      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 +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
      Transport Information
      Supplemental Information
      Specifications

      Documentation

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

      Title

      Safety Data Sheet (SDS) 

      γ-Secretase Inhibitor XXI, Compound E - CAS 209986-17-4 - Calbiochem Certificates of Analysis

      TitleLot Number
      565790

      References

      Reference overview
      Milano, 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.
      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.

      Revision04-April-2011 RFH
      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
      DescriptionA 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).
      FormWhite solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number209986-17-4
      Chemical formulaC₂₇H₂₄F₂N₄O₃
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (10 mg/ml)
      Storage +2°C to +8°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 6 months at -20°C.
      Toxicity Standard Handling
      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.