500587 γ-Secretase Inhibitor XXV, FT-9 - Calbiochem

500587
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500587-10MG
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      Glass bottle 10 mg
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      Description
      OverviewFT-9, a cell-permeable NSAID-like compound, is a partially selective γ-Secretase Inhibitor in both microsomes and whole cells. Displays dose-dependent inhibition of the γ-secretase cleavage of β-Amyloid Precursor Protein (APP) and APLP2 with IC50 values against APP ICD (intracellular domain) and APLP2 ICD of ˜260 µM, but there is a less potent effect on γ-secretase processing of APLP1. The concentration of FT-9 required to cause a 2-fold increase in APP CTFs, 3.4 +/- 0.4 µM, is significantly lower than that for APLP1 (25.7 +/- 8.9 µM) (P = 0.001). For comparison, the concentration of another γ-Secretase inhibitor compound E (EMD Chemicals, Inc. Cat. No. 565790) needed for a 2-fold increase in the magnitude of the CTF band signal is not significantly different, being 0.27 nM for APP versus 0.24 nM for APLP1. This is the first example that a GSI can preferentially target APP processing while sparing other γ-substrates.
      Catalogue Number500587
      Brand Family Calbiochem®
      Synonyms2-[3-(3,5-dichlorophenoxy)phenyl]propanoic acid
      References
      ReferencesSala Frigerio, C., et al. 2009. Biochemistry 48, 10894.
      Kukar, TL., et al. 2008. Nature 453, 925.
      Product Information
      FormOff-white powder
      Hill FormulaC₁₅H₁₂Cl₂O₃
      Chemical formulaC₁₅H₁₂Cl₂O₃
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥97% by HPLC
      Physicochemical Information
      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
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Packaging Information
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      γ-Secretase Inhibitor XXV, FT-9 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Sala Frigerio, C., et al. 2009. Biochemistry 48, 10894.
      Kukar, TL., et al. 2008. Nature 453, 925.
      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.

      Revision28-June-2013 JSW
      Synonyms2-[3-(3,5-dichlorophenoxy)phenyl]propanoic acid
      DescriptionFT-9, a cell-permeable NSAID-like compound, is a partially selective γ-Secretase Inhibitor in both microsomes and whole cells. Displays dose-dependent inhibition of the γ-secretase cleavage of β-Amyloid Precursor Protein (APP) and APLP2 with IC50 values against APP ICD (intracellular domain) and APLP2 ICD of ˜260 µM, but there is a less potent effect on γ-secretase processing of APLP1. The concentration of FT-9 required to cause a 2-fold increase in APP CTFs, 3.4 +/- 0.4 µM, is significantly lower than that for APLP1 (25.7 +/- 8.9 µM) (P = 0.001). For comparison, the concentration of another γ-Secretase inhibitor compound E (EMD Chemicals, Inc. Cat. No. 565790) needed for a 2-fold increase in the magnitude of the CTF band signal is not significantly different, being 0.27 nM for APP versus 0.24 nM for APLP1. This is the first example that a GSI can preferentially target APP processing while sparing other γ-substrates.
      FormOff-white powder
      Chemical formulaC₁₅H₁₂Cl₂O₃
      Purity≥97% by HPLC
      SolubilityDMSO (100 mg/ml)
      Storage +2°C to +8°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesSala Frigerio, C., et al. 2009. Biochemistry 48, 10894.
      Kukar, TL., et al. 2008. Nature 453, 925.