GSK-4112 is an experimental drug that was developed by
GlaxoSmithKline
GSK plc (an acronym from its former name GlaxoSmithKline plc) is a British Multinational corporation, multinational Pharmaceutics, pharmaceutical and biotechnology company with headquarters in London. It was established in 2000 by a Mergers an ...
as an agonist of
Rev-ErbAα. It is used for studying regulation of the
circadian rhythm
A circadian rhythm (), or circadian cycle, is a natural oscillation that repeats roughly every 24 hours. Circadian rhythms can refer to any process that originates within an organism (i.e., Endogeny (biology), endogenous) and responds to the env ...
and its influence on diverse processes such as
adipogenesis
Adipogenesis is the formation of adipocytes (fat cells) from stem cells. It involves 2 phases, determination, and terminal differentiation. Determination is mesenchymal stem cells committing to the adipocyte precursor cells, also known as lipoblast ...
, regulation of
bone density
Bone density, or bone mineral density, is the amount of bone mineral in bone tissue. The concept is of mass of mineral per volume of bone (relating to density in the physics sense), although medicine#Clinical practice, clinically it is measured by ...
, and
inflammation
Inflammation (from ) is part of the biological response of body tissues to harmful stimuli, such as pathogens, damaged cells, or irritants. The five cardinal signs are heat, pain, redness, swelling, and loss of function (Latin ''calor'', '' ...
.
See also
*
SR8278
SR-8278 is an experimental drug that was developed as an antagonist of Rev-ErbAα. It has been used to demonstrate potential applications of Rev-ErbAα antagonists in the treatment of conditions such as Duchenne muscular dystrophy and Alzheimer' ...
*
SR9009
SR9009, also known as Stenabolic, is a research drug that was developed by professor Thomas Burris of the Scripps Research Institute as an agonist of Rev-ErbA (i.e., increases the constitutive repression of genes regulated by Rev-ErbA) with a ...
*
SR9011
SR9011 is a research drug that was developed by Professor Thomas Burris of Scripps as an agonist of Rev-ErbAα
with a half-maximum inhibitory concentration ( IC50) = 790 nM for Rev-Erbα and IC50 = 560 nM for Rev-ErbAβ. It has been used in th ...
References
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Thiophenes
Tert-butyl compounds
Nitroarenes
4-Chlorophenyl compounds
Amines
Esters