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.
 |
Source | Oncotarget (2018). Figure 5. FH535 |
| Method | cell proliferation assay | |
| Cell Lines | EOC cells | |
| Concentrations | 10 mg/kg | |
| Incubation Time | 48 h | |
| Results | We have determined sub-optimal doses of thiostrepton and FH535 that can be used in combination to inhibit cell viability, clonogenicity and induce apoptosis. |
| 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 | |
| Molecular Weight | 361.20 |
| Formula | C13H10Cl2N2O4S |
| CAS Number | 108409-83-2 |
| Solubility (25°C) | DMSO ≥ 20 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
| Related PPAR Products |
|---|
| DSO-5a
DSO-5a is a potent, selective, orally active BB3 agonist. |
| Carfloglitazar sodium
Carfloglitazar sodium is a dual agonist of the pan peroxisome proliferator-activated receptor (PPARα/γ) with EC50 values of 1.2, 0.08, and 1.7 μM for PPARα, PPARγ, and PPARδ, respectively.It can be used in studies related to nonalcoholic steatohepatitis (NASH). |
| Seladelpar
Seladelpar is a potent, orally active, specific PPAR-δ agonist with an EC50 of 2 nM. |
| 4'-O-Methylhonokiol
4-O-Methyl honokiol is a natural neolignan isolated from Magnolia officinalis, acts as a PPARγ agonist, and inhibtis NF-κB activity, used for cancer and inflammation research. |
| 3-Phenyl-2-propen-1-ol
trans-Cinnamyl alcohol is a trans-isomer of Cinnamyl alcohol. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
