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
Warning
Toxicity: Regulatory Review (Z)
Reconstitution
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
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
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Cellular and molecular gastroenterology and hepatology, 12(2), 395-425 (2021-03-07)
Rev-erbα represents a powerful transcriptional repressor involved in immunity. However, the regulation, function, and clinical relevance of Rev-erbα in Helicobacter pylori infection are presently unknown. Rev-erbα was examined in gastric samples from H pylori-infected patients and mice. Gastric epithelial cells (GECs)
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