GSK-4112 explained

GSK-4112 is an experimental drug that was developed by GlaxoSmithKline as an agonist of Rev-ErbAα.^[1] It is used for studying regulation of the circadian rhythm and its influence on diverse processes such as adipogenesis,^{[2] [3]} regulation of bone density,^[4] and inflammation.^{[5] [6] [7] [8]}

See also

• SR8278
• SR9009
• SR9011

Notes and References

1. Grant D, Yin L, Collins JL, Parks DJ, Orband-Miller LA, Wisely GB, Joshi S, Lazar MA, Willson TM, Zuercher WJ . 6 . GSK4112, a small molecule chemical probe for the cell biology of the nuclear heme receptor Rev-erbα . ACS Chemical Biology . 5 . 10 . 925–32 . October 2010 . 20677822 . 10.1021/cb100141y .
2. Kojetin DJ, Burris TP . A role for rev-erbα ligands in regulation of adipogenesis . Current Pharmaceutical Design . 2011 . 17 . 4 . 320–4 . 21375499 . 10.2174/138161211795164211 .
3. Chu G, Zhou X, Hu Y, Shi S, Yang G . Rev-erbα Inhibits Proliferation and Promotes Apoptosis of Preadipocytes through the Agonist GSK4112 . International Journal of Molecular Sciences . 20 . 18 . September 2019 . 4524 . 31547330 . 10.3390/ijms20184524 . 6769707 . free .
4. Kim K, Kim JH, Kim I, Seong S, Kim N . Rev-erbα Negatively Regulates Osteoclast and Osteoblast Differentiation through p38 MAPK Signaling Pathway . Molecules and Cells . 43 . 1 . 34–47 . January 2020 . 31896234 . 10.14348/molcells.2019.0232 . 6999712 .
5. Sato S, Sakurai T, Ogasawara J, Takahashi M, Izawa T, Imaizumi K, Taniguchi N, Ohno H, Kizaki T . 6 . A circadian clock gene, Rev-erbα, modulates the inflammatory function of macrophages through the negative regulation of Ccl2 expression . Journal of Immunology . 192 . 1 . 407–17 . January 2014 . 24307731 . 10.4049/jimmunol.1301982 . free .
6. Sundar IK, Rashid K, Sellix MT, Rahman I . The nuclear receptor and clock gene REV-ERBα regulates cigarette smoke-induced lung inflammation . Biochemical and Biophysical Research Communications . 493 . 4 . 1390–1395 . December 2017 . 28974420 . 10.1016/j.bbrc.2017.09.157 . 5756581 .
7. Guo DK, Zhu Y, Sun HY, Xu XY, Zhang S, Hao ZB, Wang GH, Mu CC, Ren HG . 6 . Pharmacological activation of REV-ERBα represses LPS-induced microglial activation through the NF-κB pathway . Acta Pharmacologica Sinica . 40 . 1 . 26–34 . January 2019 . 29950615 . 10.1038/s41401-018-0064-0 . 6318300 . free .
8. Morioka N, Kodama K, Tomori M, Yoshikawa K, Saeki M, Nakamura Y, Zhang FF, Hisaoka-Nakashima K, Nakata Y . 6 . Stimulation of nuclear receptor REV-ERBs suppresses production of pronociceptive molecules in cultured spinal astrocytes and ameliorates mechanical hypersensitivity of inflammatory and neuropathic pain of mice . Brain, Behavior, and Immunity . 78 . 116–130 . May 2019 . 30682503 . 10.1016/j.bbi.2019.01.014 . 59273997 .