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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).

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

Synonyms: 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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565771
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₃₉H₅₂N₄O₆

Pricing & Availability

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565771-250UG
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      		 Plastic ampoule 250 μg
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      565771-500UG
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          		 Plastic ampoule 500 μg
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          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
          Catalogue Number GTIN
          565771-250UG 04055977267839
          565771-500UG 04055977267846

          Documentation

          InSolution™ γ-Secretase Inhibitor X - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          InSolution™ γ-Secretase Inhibitor X - Calbiochem Certificates of Analysis

          TitleLot Number
          565771

          References

          Reference overview
          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.
          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.

          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.