β-Catenin/Tcf Inhibitor, FH535 is a sulfonamide-based and cell-permeable compound that exhibits a dual pathway inhibition against Wnt/β-catenin and PPAR. FH535 and its structurally similar analog, PPAR inhibitor GW9662, both exhibit inhibition of coactivator/PPAR binding, though only FH535 blocks β-catenin/PPAR interaction. Further, the antagonistic activity of FH535 does not involve the covalent modification of non-covalent interaction with the PPR ligand-binding site cysteine residue, which has been experimentally shown to be crucial for GW9662 action. β-Catenin/Tcf Inhibitor, FH535 is an inhibitor of GRIP1, PPAR-β, and PPAR-γ.
1. Handeli, Shlomo., et al., 2008. A small-molecule inhibitor of Tcf/beta-catenin signaling down-regulates PPARgamma and PPARdelta activities. Molecular cancer therapeutics. 7(3): 521-9. PMID: 18347139
See how others have used beta-Catenin/Tcf Inhibitor, FH535. Click on the entry to view the PubMed entry .
PMID: # 27718127 Hou, R. et al. 2016. Tumour Biol.
PMID: # 27481517 Yu, L. et al. 2016. Tumour biology : the journal of the International Society for Oncodevelopmental Biology and Medicine. 37: 13821-13829.
PMID: # 25765854 Vega, SL. et al. 2015. Integr Biol (Camb). 7: 435-46.
PMID: # 24781517 2014. Psychopharmacology (Berl.). 231: 4383-91.
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