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Description

A cell-permeable REV-ERB antagonist that inhibits REV-ERBalpha transcriptional repression activity (EC50 = 0.47 µ,M) 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 µ,M) in a co-transfection assay. Treatment of HepG2 cells with SR8278 at 10 µ,M results in a significant increase in the expression of either G6Pase and PEPCK mRNA expression, consistent with its antagonistic role against endogenous heme.