名称 | FH535 |
描述 | FH535, a Wnt/β-catenin signaling and PPAR inhibitor, exhibits anti-tumor activities. |
细胞实验 | 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) |
激酶实验 | 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. |
体内活性 | 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. |
存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 65 mg/mL (179.96 mM), Sonication is recommended.
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关键字 | FH535 | Beta catenin | FH 535 | β-catenin | inhibit | FH-535 | PPAR | Wnt | Inhibitor | Peroxisome proliferator-activated receptors |
相关产品 | PHYTOL | (S)-(+)-Ibuprofen | BADGE | Daidzein | Fenofibrate | Pioglitazone hydrochloride | 5-Aminosalicylic Acid | Naringenin | Fisetin | 2,3-Butanediol | Icariin | Nefopam hydrochloride |
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