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Stenabolic (SR9009) is an agonist of REV-ERB, with IC50 of 670 nM and 800 nM for REV-ERBα and REV-ERBβ respectively. Stenabolic (SR9009) inhibits the activity of the SCN clock, with reversible inhibition of circadian oscillations in SCN explants cultured from the Per2:luc reporter mouse. Stenabolic (SR9009) dose-dependently increases the REV-ERB-dependent repressor activity assessed in HEK293 cells expressing a chimeric Gal4 DNA Binding Domain (DBD) - REV-ERB ligand binding domain (LBD) α or β and a Gal4-responsive luciferase reporter. Stenabolic (SR9009) potently and efficaciously suppresses transcription in a cotransfection assay using full-length REV-ERBα along with a luciferase reporter driven by the Bmal1 promoter (SR9009 IC50=710 nM).
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Source | Cell Physiol Biochem (2018). Figure 4. SR9009 |
| Method | MTT assay | |
| Cell Lines | The human monocytic leukemia cell line | |
| Concentrations | 1, 5, 10, and 50 µM | |
| Incubation Time | 12 h | |
| Results | Expression of hMMP-9 mRNA also decreased when cells were treated with SR9009 alone, without Ang II stimulation (P < 0.05). The effect of SR9009 was further confirmed on mouse MMP-9 (mMMP-9) mRNA expression in RAW264.7 macrophages |
| Cell Experiment | |
|---|---|
| Cell lines | L929 cell |
| Preparation method | Cells were treated with 100 ng/ml IFNg (Millipore) and 10 ng/ml LPS(Millipore) for M1 polarization. M2 differentiation was induced by incubating macrophages with 15 ng/ml IL-4 (Millipore). |
| Concentrations | 10 μM |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | homozygous LDL receptor deficient (ldlr−/−) male mice |
| Formulation | PBS |
| Dosages | 100 mg/kg |
| Administration | |
| Molecular Weight | 437.94 |
| Formula | C20H24ClN3O4S |
| CAS Number | 1379686-30-2 |
| Solubility (25°C) | DMSO ≥ 60 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 |
|---|
| SR8278
SR8278 represents a unique chemical tool for probing REV-ERB function and may serve as a point for initiation of further optimization to develop REV-ERB antagonists with the ability to explore circadian and metabolic functions. |
| 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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