GSK4112
Rev-Erbα agonist / Selective Rev-Erbα agonist (EC50=250 nM).1,2 It induces circadian clock phase shifts in isolated primary lung fibroblasts as well as in lung slices (10 µM).1 GSK4112 showed an inhibitory effect on the amplitude of circadian oscillations and caused an arrhythmic expression of canonical clock genes.3 In murine RAW264 macrophages it suppressed inflammatory functions via repressing Ccl2 expression.4 It protected RANKL-induced bone loss via inhibition of osteoclast differentiation in vivo.5
Biochemicals & reagents
1216744-19-2
SR-6452
1 Meng et al. (2008), Ligand modulation of REV-ERBalpha function resets the peripheral circadian clock in a phasic manner; J. Cell. Science, 121 3629 2 Grant et al. (2010), GSK4112, a small molecule chemical probe for the cell biology of the nuclear heme receptor Rev-erbα; ACS Chem. Biol., 5 925 3 Chen et al. (2015), Integration of the nuclear receptor REV-ERBα linked with circadian oscillators in the expressions of Alas1, Ppargc1a, and Il6 genes in rat granulosa cells; Chronobiol. Int., 32 739 4 Sato et al. (2014), A circadian clock gene, Rev-erbα, modulates the inflammatory function of macrophages through the negative regulation of Ccl2 expression; J. Immunol., 192 407 5 Kim et al. (2020), Rev-erbα Negatively Regulates Osteoclast and Osteoblast Differentiation through p38 MAPK Signaling Pathway; Mol. Cells, 43 34
-20°C
TARGET: Transcription factor -- PATHWAY: Transcription; Fatty acid metabolism -- RESEARCH AREA: Circadian clock -- DISEASE AREA: Inflammation; Osteoporosis