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Description
Overview
FT-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 Number
500587
Brand Family
Calbiochem®
Synonyms
2-[3-(3,5-dichlorophenoxy)phenyl]propanoic acid
References
References
Sala Frigerio, C., et al. 2009. Biochemistry48, 10894. Kukar, TL., et al. 2008. Nature453, 925.
Product Information
Form
Off-white powder
Hill Formula
C₁₅H₁₂Cl₂O₃
Chemical formula
C₁₅H₁₂Cl₂O₃
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 Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Sala Frigerio, C., et al. 2009. Biochemistry48, 10894. Kukar, TL., et al. 2008. Nature453, 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.
Revision
28-June-2013 JSW
Synonyms
2-[3-(3,5-dichlorophenoxy)phenyl]propanoic acid
Description
FT-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.
Form
Off-white powder
Chemical formula
C₁₅H₁₂Cl₂O₃
Purity
≥97% by HPLC
Solubility
DMSO (100 mg/ml)
Storage
+2°C to +8°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity
Standard Handling
References
Sala Frigerio, C., et al. 2009. Biochemistry48, 10894. Kukar, TL., et al. 2008. Nature453, 925.