General description
A cell-permeable REV-ERB antagonist that inhibits REV-ERBα transcriptional repression activity (EC50 = 0.47 µM) in a REV-ERB target gene assay. It is also shown to block the ability of GSK4112 to enhance REV-ERB-&alpha-dependent repression (EC50 = 0.35 µM) in a co-transfection assay. Treatment of HepG2 cells with SR8278 at 10 µM results in a significant increase in the expression of either G6Pase and PEPCK mRNA expression, consistent with its antagonistic role against endogenous heme.
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to months at -20°C.
Other Notes
Kojetin, D., et al. 2010, Chem Bio in press
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Regulatory Review (Z)
| Quality Segment | 100 |
| assay | >95% (HPLC) |
| form | gum,solid |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,protect from light |
| color | white to yellow-brown |
| solubility | DMSO: 25 mg/mL |
| shipped in | ambient |
| storage temp. | −20°C |
| SMILES string | n1c2c(ccc1COc3cc(ccc3)C(O)CCCCC)cccc2 |
| InChI key | JRLOEMCOOZSCQP-UHFFFAOYSA-N |
