FH535 _PPAR 抑制剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEFH535Cat. No.: HY-15721CAS No.: 108409-83-2分式: CHClNOS分量: 361.2作靶点: PPAR; Wnt; -catenin作通路: Cell Cycle/DNA Damage; Stem Cell/Wnt储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 33.33 mg/mL (

2、92.28 mM; Need ultrasonic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.92 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (6.92 mM); Suspended solution; Need ultrasonic1/3 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性

3、 FH535是Wnt/-catenin 和 PPAR 的抑制剂，具有抗肿瘤活性。IC50 & Target PPAR Wnt -catenin体外研究 FH535 is an inhibitor of Wnt/-catenin and PPAR. FH535 inhibits PPAR and PPAR transactivation inHCT116 cells. FH535 (15 M) activities depend on functional PPAR but does not require a cysteine residuein the PPAR ligand-binding

4、 domain. FH535 inhibits recruitment of the coactivators GRIP1 and -catenin toPPAR and PPAR. FH535 shows toxic effects on 12 carcinoma cell lines expressing wnt/-catenin pathway1. FH535 (20 M) suppresses the -catenin pathway in pancreatic cancer cells, and inhibits pancreaticcancer cell migration. Fu

5、rthermore, FH535 (20, 40 M) inhibits pancreatic cancer cell invasion and cellgrowth 2. FH535 represses angiogenesis-related genes in pancreatic cancer cells 3.体内研究 FH535 (25 mg/kg, i.p.) exhibits an anti-tumor effect on pancreatic cancer xenografts in mice. FH535 alsorepresses angiogenesis in pancre

6、atic cancer xenografts 2.PROTOCOLCell Assay 2 Cell growth is evaluated using the MTT assay. Cells (5 104/well) are seeded in 24-well tissue cultureplates. Blank control is treated with DMSO. After FH535 treatment, MTT is added to each well (finalconcentration, 0.5 mg/mL), followed by 4-hour incubati

7、on at 37C. The medium is removed, and 800 L ofDMSO is added to each well. The absorbance of the mixture is measured at 490 nm using a microplateenzyme-linked immunosorbent assay reader. The relative cell viability is calculated as follows: relative cellviability = (mean experimental absorbance/mean

8、control absorbance) 100% 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Four-week-old female BALB/c athymic nude mice receive humane care. PANC-1 cells stably expressingAdministration 3 firefly luciferase are injected into the left flanks of t

9、he mice in a total volume of 100 L (0.5 107 cells), andthe mice are randomly assigned to a DMSO intraperitoneally injected with 100 L DMSO/DMEM (1:1) orFH535 group intraperitoneally injected with 25 mg/kg FH535 dissolved in 100 L DMSO/DMEM (1:1).Treatment is conducted every 2 days for 20 days; tumor

10、 volume is measured with a caliper using the formula:volume = length width2/2. At the end of the experiment, the mice are anaesthetized and given D-luciferin inPBS. Twenty minutes after the injection, bioluminescence is imaged with a charge-coupled device camera.Then, the tumor tissue is stripped an

11、d formalin-fixed, paraffin-embedded, cut into 4-m sections, andimmunohistochemically stained 3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Oncol Lett. 2019 Jun.See more customer validations on HYPERLINK / www.MedChemE2/3 Master of Small

12、Molecules 您边的抑制剂师www.MedChemEREFERENCES1. Handeli S, et al. A small-molecule inhibitor of Tcf/beta-catenin signaling down-regulates PPARgamma and PPARdelta activities. MolCancer Ther. 2008 Mar;7(3):521-9.2. Wu MY, et al. FH535 inhibited metastasis and growth of pancreatic cancer cells. Onco Targets Ther. 2015 Jul 6;8:1651-70.3. Liu L, et al. FH535, a -catenin pathway inhibitor, represses pancreatic cancer xenograft growth and angiogenesis. Oncotarget. 2016 Jul26;7(30):47145-47162.McePdfHeightC