化合物FH535 T2413

Product Introduction
Bioactivity


英文名: FH535

描述: FH535 是一种具有抗肿瘤活性的Wnt/β-catenin 和PPAR 抑制剂。

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抑制β-连环蛋白/Tcf介导的转录,同时还具有抑制共激活剂GRIP1和β-连环蛋白对PPARδ 和 PPAR的聚集作用。在表达较高的或活跃的Wnt/β-连环蛋白通路癌细胞中,FH535能够抑制细胞增殖。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 27.1 mg/mL (75 mM)


关键字: FH535 | Beta catenin | FH 535 | β-catenin | inhibit | FH-535 | PPAR | Wnt | Inhibitor | Peroxisome proliferator-activated receptors

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