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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Kojetin, D., et al. 2010, Chem Bio in press

Packaging

5 mg in Glass bottle

Packaged under inert gas

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to months at -20°C.

Warning

Toxicity: Regulatory Review (Z)