GSK4112, also known as SR6452, is identified as a Rev-erbα agonist with an EC50 value of 0.4 μM. It serves as a valuable chemical tool for investigating the role of Rev-erbα in various biological processes, including transcriptional repression, the regulation of circadian rhythms, and metabolic pathways.
- Interacts with Rev-erbα with an EC50 of 0.4 μM.
- Represses the expression of bmal1 and target genes associated with gluconeogenesis, recruits HDAC3, and modulates Rev-erbα's effect on hepatic gene expression oscillation.
- Reduces glucose output in murine hepatocytes.
- Attenuates Fas-induced hepatic damage in male C57BL/6 mice.