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

500587
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      Overview

      Replacement Information

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      Catalogue NumberAvailability Packaging Qty/Pack Price Quantity
      500587-10MG
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      In Stock 
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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
          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

          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.