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Description

A cell-permeable sulfonamide compound that acts as a dual pathway inhibitor against Wnt/beta-catenin (>=80% inhibition at 15 µ,M in beta-catenin/Tcf-dependent cellular reporter assays) and PPARgamma/delta (>=30% inhibition at 0.5 µ,M in PPRE cellular reporter assays) signalings. Although both FH535 and the structurally similar PPARgamma-selective inhibitor GW9662 (Cat. No. 370700) inhibit coactivator/PPAR binding, only FH535 blocks beta-catenin/PPARgamma interaction and the antagonistic activity of FH535 does not involve the covalent modification of or non-covalent interaction with the PPAR ligand-binding site cystein residue that is crucial for GW9662 action., A cell-permeable sulfonamide compound that acts as a dual pathway inhibitor against Wnt/beta-catenin (>=80% inhibition at 15 µ,M in beta-catenin/Tcf-dependent cellular reporter assays) and PPARgamma/delta (>=30% inhibition at 0.5 µ,M in PPRE cellular reporter assays) signalings. Although both FH535 and the structurally similar PPARgamma-selective inhibitor GW9662 (Cat. No. 370700) inhibit coactivator/PPAR binding, only FH535 blocks beta-catenin/PPARgamma interaction and the antagonistic activity of FH535 does not involve the covalent modification of or non-covalent interaction with the PPAR ligand-binding site cystein residue that is crucial for GW9662 action.