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565771 InSolution™ γ-Secretase Inhibitor X - Calbiochem

InSolution™ γ-Secretase Inhibitor X is a 1 mM solution in DMSO. A highly potent inhibitor of g-secretase (IC₅₀ = 17, 48, 67 nM for Aβtotal, Aβ40 & Aβ42 in SHSY5Y cells overexpressing spβA4CTF).

SDB (Sicherheitsdatenblätter), Analysenzertifikate und Qualitätszertifikate, Dossiers, Broschüren und andere verfügbare Dokumente.

Synonyme: L-685,458, {1S-Benzyl-4R-[1-(1S-carbamoyl-2-phenethylcarbamoyl)-1S-3-methylbutylcarbamoyl]-2R-hydroxy-5-phenylpentyl}carbamic Acid tert-butyl Ester

Primary Target: Aβtotal
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      Übersicht

      Replacement Information

      Key Spec Table

      Empirical Formula
      C₃₉H₅₂N₄O₆
      Description
      OverviewA cell-permeable hydroxyethylene dipeptide isostere that acts as a highly specific and a potent inhibitor of γ-secretase (Aβtotal IC50 = 17 nM, Aβ40 IC50 = 48 nM, and Aβ42 IC50 = 67 nM in SHSY5Y cells overexpressing spβA4CTF). Binds to presenilin and blocks Notch intracellular domain production. Functions as a transition state analog mimic at the catalytic site of an aspartyl protease, however, it exhibits over 100-fold greater selectivity for γ-secretase than for cathepsin D.
      Catalogue Number565771
      Brand Family Calbiochem®
      SynonymsL-685,458, {1S-Benzyl-4R-[1-(1S-carbamoyl-2-phenethylcarbamoyl)-1S-3-methylbutylcarbamoyl]-2R-hydroxy-5-phenylpentyl}carbamic Acid tert-butyl Ester
      References
      ReferencesWeidemann, A., et al. 2002. Biochemistry 41, 2825.
      Doerfler, P., et al. 2001. Proc. Natl. Acad. Sci. USA 98, 9312.
      Li, Y.M., et al. 2000. Proc. Natl. Acad. Sci. USA 97, 6138.
      Shearman, M.S., et al. 2000. Biochemistry 39, 8698.
      Product Information
      ATP CompetitiveN
      FormLiquid
      FormulationA 1 mM (250 µg in 372 µl or 500 µg in 744 µl) solution in DMSO.
      Hill FormulaC₃₉H₅₂N₄O₆
      Chemical formulaC₃₉H₅₂N₄O₆
      ReversibleN
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetAβtotal
      Primary Target IC<sub>50</sub>Aβtotal 17 nM, Aβ40 48 nM, and Aβ42 67 nM in SHSY5Y cells overexpressing spβA4CTF
      Purity≥90% 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
      Protect from Moisture Protect from moisture
      Do not freeze Ok to freeze
      Special InstructionsFollowing initial thaw, aliquot and freeze (-20°C).
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Bestellnummer GTIN
      565771 0

      Documentation

      InSolution™ γ-Secretase Inhibitor X - Calbiochem SDB

      Titel

      Sicherheitsdatenblatt (SDB) 

      InSolution™ γ-Secretase Inhibitor X - Calbiochem Analysenzertifikate

      TitelChargennummer
      565771

      Literatur

      Übersicht
      Weidemann, A., et al. 2002. Biochemistry 41, 2825.
      Doerfler, P., et al. 2001. Proc. Natl. Acad. Sci. USA 98, 9312.
      Li, Y.M., et al. 2000. Proc. Natl. Acad. Sci. USA 97, 6138.
      Shearman, M.S., et al. 2000. Biochemistry 39, 8698.
      Datenblatt

      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.

      Revision10-September-2008 RFH
      SynonymsL-685,458, {1S-Benzyl-4R-[1-(1S-carbamoyl-2-phenethylcarbamoyl)-1S-3-methylbutylcarbamoyl]-2R-hydroxy-5-phenylpentyl}carbamic Acid tert-butyl Ester
      DescriptionA cell-permeable hydroxyethylene dipeptide isostere that acts as a potent and highly specific inhibitor of γ-secretase (Aβ total IC50 = 17 nM; Aβ40 IC50 = 48 nM; and Aβ42 IC50 = 67 nM in SH-SY5Y cells overexpressing spβA4CTF). Binds to presenilin and blocks Notch intracellular domain production. Also reported to block the formation of εCTF, resulting in the accumulation of α- and βCTF. Functions as a transition state analog mimic at the catalytic site of an aspartyl protease, however, it exhibits over 100-fold greater selectivity for γ-secretase than for cathepsin D.
      FormLiquid
      FormulationA 1 mM (250 µg in 372 µl or 500 µg in 744 µl) solution in DMSO.
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₃₉H₅₂N₄O₆
      Structure formulaStructure formula
      Purity≥90% by HPLC
      Storage Protect from moisture
      Protect from light
      -20°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing initial thaw, aliquot and freeze (-20°C).
      Toxicity Standard Handling
      ReferencesWeidemann, A., et al. 2002. Biochemistry 41, 2825.
      Doerfler, P., et al. 2001. Proc. Natl. Acad. Sci. USA 98, 9312.
      Li, Y.M., et al. 2000. Proc. Natl. Acad. Sci. USA 97, 6138.
      Shearman, M.S., et al. 2000. Biochemistry 39, 8698.