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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

Products

Catalogue NumberPackaging Qty/Pack
565771-250UGCN Plastic ampoule 250 μg
565771-500UGCN Plastic ampoule 500 μg
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
565771-250UGCN 04055977267839
565771-500UGCN 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.