FT-9, a cell-permeable NSAID-like compound, is a partially selective gamma-Secretase Inhibitor in both microsomes and whole cells. Displays dose-dependent inhibition of the gamma-secretase cleavage of beta-Amyloid Precursor Protein (APP) and APLP2 with IC50 values against APP ICD (intracellular domain) and APLP2 ICD of ~260uM, but there is a less potent effect on gamma-secretase processing of APLP1. The concentration of FT-9 required to cause a 2-fold increase in APP CTFs, 3.4 +/- 0.4uM, is significantly lower than that for APLP1 (25.7 +/- 8.9uM) (P = 0.001). For comparison, the concentration of another gamma-Secretase inhibitor compound E needed for a 2-fold increase in the magnitude of the CTF band signal is not significantly different, being 0.27nM for APP versus 0.24nM for APLP1. This is the first example that a GSI can preferentially target APP processing while sparing other gamma-substrates. Synonyms: 2-[3-(3,5-dichlorophenoxy)phenyl]propanoic acid Molecular Formula: C15H12Cl2O3 Solubility: DMSO Molar Mass: 311.2 Storage and Stability: May be stored at 4C. For long-term storage, aliquot and store at 4C. Do not freeze. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer.
Molecular Weight:
311.2
Purity:
97% (HPLC)
Form:
Supplied as an off-white powder.
* VAT and and shipping costs not included. Errors and price changes excepted
