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

565790
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₇H₂₄F₂N₄O₃ 209986-17-4

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      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
              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.