GSK-4112
GSK-4112
GSK-4112 is a synthetic chemical compound that acts as a selective ligand for the nuclear receptor Rev-ErbA alpha. It is primarily used in research to study the physiological roles of Rev-ErbA alpha, which is involved in the regulation of circadian rhythm, metabolism, and inflammation.
Mechanism of Action
GSK-4112 functions as an agonist of the Rev-ErbA alpha receptor. By binding to this receptor, GSK-4112 influences the transcription of genes involved in various biological processes. The activation of Rev-ErbA alpha by GSK-4112 leads to the repression of target genes, which can affect the circadian clock, lipid metabolism, and glucose homeostasis.
Biological Effects
The activation of Rev-ErbA alpha by GSK-4112 has been shown to have several biological effects:
- Circadian Rhythm Regulation: GSK-4112 can modulate the expression of core clock genes, thereby influencing the circadian rhythm.
- Metabolic Effects: It affects lipid and glucose metabolism, potentially offering insights into the treatment of metabolic disorders.
- Inflammation: GSK-4112 has been studied for its role in modulating inflammatory responses, which could have implications for diseases characterized by chronic inflammation.
Research Applications
GSK-4112 is used extensively in biomedical research to explore the functions of Rev-ErbA alpha. It serves as a tool compound to dissect the pathways regulated by this nuclear receptor and to understand its role in various physiological and pathological conditions.
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Contributors: Prab R. Tumpati, MD