GSK4112

GSK4112 is a potent and selective small molecule agonist of the nuclear receptor REV-ERBα (NR1D1). Developed by GSK, it serves as a primary chemical probe for investigating the role of the circadian clock in physiological processes, including metabolism, adipogenesis, and immune response. By binding to the ligand-binding domain of REV-ERBα, GSK4112 facilitates the recruitment of corepressors, thereby suppressing the transcription of target genes such as BMAL1. In preclinical research, GSK4112 has demonstrated the ability to attenuate inflammatory cytokine production (e.g., IL-6, TNFα) and modulate macrophage polarization, suggesting potential therapeutic utility in treating myeloid-driven inflammation in conditions like allergic asthma.

Other names

SR6452SR-6452SR 6452