GSK-4112

GSK-4112 is a selective agonist for REV-ERBα (EC₅₀ = 0.4 μM). At 10 μM, GSK-4112 can reset the circadian rhythm in a phasic manner by inhibiting expression of the circadian target gene bmal1 and reduce glucose output by 30% in mouse primary hepatocytes by repressing the expression of several gluconeogenic genes. GSK-4112 is useful as a chemical tool to probe the function of REV-ERbα in transcriptional repression, regulation of circadian biology, and metabolic pathways.