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Treatment of HepG2 cells with SR8278 results in increased expression of REV-ERBα target genes consistent with the compound blocking the action of the endogenous agonist, heme. In a cell-based assay, SR8278 is considerably more potent than the other synthetic REV-ERBα ligand, GSK4112, which functions as an agonist. Like GSK4112, SR8278 displayed poor pharmacokinetic properties that will likely limit its use to biochemical and cell-based assays. SR8278 is a competitive nuclear heme receptor REV-ERB synthetic antagonist. SR8278 inhibits the REV-ERBα transcriptional repression activity with an EC50 of 0.47μM. SR8278 is used to regulate the metabolism in organisms and study biological rhythm.
| Cell Experiment | |
|---|---|
| Cell lines | HepG2 cells |
| Preparation method | Sixteen h post-transfection, the cells were treated with vehicle or compound. 24 h post-treatment, the luciferase activity was measured using the Dual-GloTM luciferase assay system. |
| Concentrations | 10 μM |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 361.48 |
| Formula | C18H19NO3S2 |
| CAS Number | 1254944-66-5 |
| Solubility (25°C) | DMSO 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related REV-ERB Products |
|---|
| Stenabolic (SR9009)
Stenabolic (SR9009) is an agonist of REV-ERB, with IC50 of 670 nM and 800 nM for REV-ERBα and REV-ERBβ respectively. |
| GSK 4112
GSK 4112 is a selective Rev-Erbα agonist with an EC50 value of 0.4 μM, which can be used to explore the function of Rev-erbα in transcriptional repression, biological regulation of circadian rhythms and metabolic pathways. |
| SR9011
SR9011 is a REV-ERBα/β agonist with IC50s of 790 nM and 560 nM for REV-ERBα and REV-ERBβ, respectively. |
| SR9011 hydrochloride
SR9011 hydrochloride is a REV-ERBα/β agonist with IC50s of 790 nM and 560 nM for REV-ERBα and REV-ERBβ, respectively. |
| STL1267
STL1267 is a potent REV-ERB agonist that crosses the blood-brain barrier with a Ki value of 0.16 µM for REV-ERBα. STL1267 showed no cytotoxicity and inhibited BMAL1 gene expression. |
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