FH 535

FH-535 (108409-83-2) suppresses Wnt/β-catenin signaling. It antagonizes PPARγ and PPARδ ligand-dependent activation which is mediated by inhibition of recruitment of the coactivators β-catenin and GRIP1 but not the corepressors NCoR and SMRT.1Inhibits the migration and growth of breast cancer cell lines2 as well as colon, lung and liver cell lines1. FH-535 is a useful tool for probing the involvement of Wnt signaling pathway.3,4

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Antagonizes Wnt/β-catenin/Tcf-mediated transcription as well as PPARγ and δ activity. Able to inhibit the recruitment of the co-activators β-catenin and GRIP1, both of which are activators for both pathways.

A cell-permeable compound that inhibits Wnt/β-catenin and PPAR

ChEBI: 2,5-dichloro-N-(2-methyl-4-nitrophenyl)benzenesulfonamide is a sulfonamide.

FH535 has the ability to block the development of colon cancer cells. It can change several cancer-associated biological processes. FH535 can also prevent PARylation of Axin2 in osteosarcoma cells.

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[1] SHLOMO HANDELI  Julian A S. A small-molecule inhibitor of Tcf/beta-catenin signaling down-regulates PPARgamma and PPARdelta activities.[J]. Molecular Cancer Therapeutics, 2008, 7 3: 521-529. DOI:10.1158/1535-7163.mct-07-2063
[2] JOJI IIDA. FH535 inhibited migration and growth of breast cancer cells.[J]. PLoS ONE, 2012: e44418. DOI:10.1371/journal.pone.0044418
[3] KATHRYN A FREWER. A role for WISP2 in colorectal cancer cell invasion and motility.[J]. Cancer Genomics & Proteomics, 2013, 10 4: 187-196.
[4] POLK W W. FH535 potentiation of cigarette smoke condensate cytotoxicity is associated with changes in β-catenin and EGR-1 signaling.[J]. International Journal of Toxicology, 2012, 31 4: 380-389. DOI:10.1177/1091581812447956
[5] TSUYOSHI MORITA  Ken’ichiro H. Tumor Progression Is Mediated by Thymosin-β4 through a TGFβ/MRTF Signaling Axis.[J]. Molecular Cancer Research, 2018, 16 5: 880-893. DOI:10.1158/1541-7786.mcr-17-0715