FH535

Catalog No.S7484 Batch:S748401

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Technical Data

Formula

C13H10Cl2N2O4S
Molecular Weight 361.20 CAS No. 108409-83-2
Solubility (25°C)* In vitro DMSO 72 mg/mL (199.33 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description FH535 is a Wnt/β-catenin signaling inhibitor and also a dual PPARγ and PPARδ antagonist.
Targets
Wnt/β-catenin [1] PPARγ [1] PPARδ [1]
In vitro FH535 antagonizes β-Catenin/Tcf–mediated transcription, and inhibits recruitment of the coactivators GRIP1 and β-catenin to PPARδ and PPARγ. FH535 shows selective anti-proliferation effect on some cancer cells expressing high or active Wnt/β-catenin pathway. [1] FH535 increases cigarette smoke condensate cytotoxicity, and causes changes in β-catenin and EGR-1 signaling. [2] FH535 has potential therapeutic value in treatment of liver cancer by targeting liver cancer stem cells and hepatocellular carcinoma cell lines. [3]

Protocol (from reference)

Kinase Assay:[1]
  • 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.
Cell Assay:[1]
  • Cell lines

    HCT116, SW48, RKO, LoVo, COLO205, IEC6, A427, HCC15, NCI-H1703, A549, HepG2, Hep3b, Huh7, Fibroblasts

  • Concentrations

    30 μM

  • Incubation Time

    48 hours

  • Method

    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.

Customer Product Validation

Data from [Data independently produced by , , J Cancer, 2017, 8(16):3142-3153]

Data from [Data independently produced by , , Cancer Med, 2018, 7(2):285-296]

Data from [Data independently produced by , , Gene, 2019, 684:95-103]

Data from [Data independently produced by , , Int J Clin Exp Pathol, 2016, 9(3):2857-2868.]

Selleck's FH535 has been cited by 20 publications

N6-Methyladenosine-Mediated Up-Regulation of FZD10 Regulates Liver Cancer Stem Cells' Properties and Lenvatinib Resistance Through WNT/β-Catenin and Hippo Signaling Pathways [ Gastroenterology, 2023, S0016-5085(23)00114-2] PubMed: 36764493
N6-Methyladenosine-Mediated Up-Regulation of FZD10 Regulates Liver Cancer Stem Cells' Properties and Lenvatinib Resistance Through WNT/β-Catenin and Hippo Signaling Pathways [ Gastroenterology, 2023, 164(6):990-1005] PubMed: 36764493
Disruption of β-catenin-mediated negative feedback reinforces cAMP-induced neuronal differentiation in glioma stem cells [ Cell Death Dis, 2022, 13(5):493] PubMed: 35610201
Combinatorial treatment with statins and niclosamide prevents CRC dissemination by unhinging the MACC1-β-catenin-S100A4 axis of metastasis [ Oncogene, 2022, 41(39):4446-4458] PubMed: 36008464
Establishment and characterization of immortalized sweat gland myoepithelial cells [ Sci Rep, 2022, 12(1):7] PubMed: 34997030
Immuno-genomic classification of colorectal cancer organoids reveals cancer cells with intrinsic immunogenic properties associated with patient survival [ J Exp Clin Cancer Res, 2021, 40(1):230] PubMed: 34256801
COX2 confers bone marrow stromal cells to promoting TNFα/TNFR1β-mediated myeloma cell growth and adhesion [ Cell Oncol (Dordr), 2021, 10.1007/s13402-021-00590-4] PubMed: 33646559
MicroRNA-506-3p increases the response to PARP inhibitors and cisplatin by targeting EZH2/β-catenin in serous ovarian cancers [ Transl Oncol, 2020, 14(2):100987] PubMed: 33360300
A novel human colon signet-ring cell carcinoma organoid line: establishment, characterization and application [ Carcinogenesis, 2020, 41(7):993-1004] PubMed: 31740922
Wnt signaling mediates oncogenic synergy between Akt and Dlx5 in T-cell lymphomagenesis by enhancing cholesterol synthesis [ Sci Rep, 2020, 10(1):15837] PubMed: 32985581

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.