| Name | FH535 |
| Description | FH535, a Wnt/β-catenin signaling and PPAR inhibitor, exhibits anti-tumor activities. |
| Cell Research | Cell viability is determined by the modified 3H-thymidine incorporation assay. Briefly, cells are plated in 96-well microplates for 24 h and treated in triplicate with various concentrations of the test compound. After 48 h of compound exposure, the cells are incubated for an additional 48 h in compound-free medium. The cells are then incubated in medium containing 3H-thymidine for 24 h, washed and mixed with the scintillant in the 96-well plate. Individual wells are counted with a 96-well scintillation counter and the LC50 is calculated.(Only for Reference) |
| Kinase Assay | High-throughput Library Screen: Three copies of the optimized or mutated Tcf-binding element from TOPFLASH or FOPFLASH driving a secreted alkaline phosphatase reporter gene are cloned into pCEP4 plasmid, replacing the cytomegalovirus promoter. The plasmids are transfected into HepG2 cells, and hygromycin-resistant clones are pooled. Library screening is done at 20 μmol/L concentration in HepG2 serum-free media. Hits are tested in the HCT116 cell line for inhibition of TOPFLASH luciferase activity but not for inhibition of a reporter activity controlled from β-actin promoter. |
| In vivo | FH535 inhibits β-catenin/Tcf-mediated transcription and also suppresses the aggregation of co-activator GRIP1 and β-catenin with PPARδ and PPARγ. In cancer cells with elevated or active Wnt/β-catenin pathways, FH535 can inhibit cell proliferation. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 65 mg/mL (179.96 mM), Sonication is recommended. 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (5.54 mM), Sonication is recommended.
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| Keywords | β-catenin | βcatenin | Wnt/β-catenin | Wnt/betacatenin | Wnt/b-catenin | Wnt | PPARδ | PPARγ | PPAR | Peroxisome proliferator-activated receptors | Inhibitor | inhibit | FH-535 | FH535 | FH 535 | beta-catenin | betacatenin | Beta catenin | bcatenin |
| Inhibitors Related | PHYTOL | Rosiglitazone | Urea | Daidzein | Fenofibrate | Neohesperidin | Ethyl linoleate | Maltitol | Naringenin | 2,3-Butanediol | NPC 15199 | Cloxiquine |
| Related Compound Libraries | Bioactive Compound Library | Anti-Neurodegenerative Disease Compound Library | Cancer Cell Differentiation Compound Library | Membrane Protein-targeted Compound Library | Inhibitor Library | Neuroprotective Compound Library | Anti-Prostate Cancer Compound Library | NO PAINS Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Active Compound Library | Neuronal Differentiation Compound Library |