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FH535

Cat. No. M3635

FH535 Structure
Size Price Availability Quantity
10mg USD 65 In stock
50mg USD 190 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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.

Protocol
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 361.20
Formula C13H10Cl2N2O4S
CAS Number 108409-83-2
Purity >99%
Solubility DMSO
Storage at -20°C
References

A small-molecule inhibitor of Tcf/beta-catenin signaling down-regulates PPARgamma and PPARdelta activities.
Handeli S, et al. Mol Cancer Ther. 2008 Mar;7(3):521-9. PMID: 18347139.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: FH535 supplier, PPAR, inhibitors

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