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FH535 antagonizes β-Catenin/Tcf–mediated transcription, and inhibits recruitment of the coactivators GRIP1 and β-catenin to PPARδ and PPARγ. FH535 increases cigarette smoke condensate cytotoxicity, and causes changes in β-catenin and EGR-1 signaling. FH535 inhibits β-catenin and GRIP1 recruitment to PPARγ and δ. FH535 Exhibits antiproliferative effects in transformed colon, lung and liver cancer cell lines.
 |
Source | Oncotarget (2018). Figure 5. FH535 |
| Method | cell proliferation assay | |
| Cell Lines | EOC cells | |
| Concentrations | 10 mg/kg | |
| Incubation Time | 48 h | |
| Results | We have determined sub-optimal doses of thiostrepton and FH535 that can be used in combination to inhibit cell viability, clonogenicity and induce apoptosis. |
| Cell Experiment | |
|---|---|
| Cell lines | HCT116, SW48, RKO, LoVo, COLO205, IEC6, A427, HCC15, NCI-H1703, A549, HepG2, Hep3b, Huh7, Fibroblasts |
| Preparation method | Determining cell viability by the modified 3H-thymidine incorporation assay. Briefly, plating cells in 96-well microplates for 24 h and treating in triplicate with various concentrations of the test compound. After 48 h of compound exposure, incubating the cells for an additional 48 h in compound-free medium. Then incubating the cells in medium containing 3H-thymidine for 24 h, washing and mixing with the scintillant in the 96-well plate. Counting Individual wells with a 96-well scintillation counter and calculating the LC50. |
| Concentrations | 30 μM |
| Incubation time | 48 hours |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 361.20 |
| Formula | C13H10Cl2N2O4S |
| CAS Number | 108409-83-2 |
| Solubility (25°C) | DMSO ≥ 20 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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