General description

A cell-permeable sulfonamide compound that acts as a dual pathway inhibitor against Wnt/β-catenin (≥80% inhibition at 15 µM in β-catenin/Tcf-dependent cellular reporter assays) and PPARγ/δ (≥30% inhibition at 0.5 µM in PPRE cellular reporter assays) signalings. Although both FH535 and the structurally similar PPARγ-selective inhibitor GW9662 (Cat. No. 370700) inhibit coactivator/PPAR binding, only FH535 blocks β-catenin/PPARγ 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/β-catenin (≥80% inhibition at 15 µM in β-catenin/Tcf-dependent cellular reporter assays) and PPARγ/δ (≥30% inhibition at 0.5 µM in PPRE cellular reporter assays) signalings. Although both FH535 and the structurally similar PPARγ-selective inhibitor GW9662 (Cat. No. 370700) inhibit coactivator/PPAR binding, only FH535 blocks β-catenin/PPARγ 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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Handeli, S., and Simon, J.A. 2008. Mol. Cancer Ther.7, 521.

Packaging

Packaged under inert gas

10 mg in Plastic ampoule

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)