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.
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Handeli, S., and Simon, J.A. 2008. Mol. Cancer Ther.7, 521.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
- UPC:
- 41116113
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 219330-10MG
