Nuclear receptors are ligand-gated transcription factors that regulate various physiological processes such as reproduction, inflammation, metabolism, development, and immune function. The 48 human nuclear receptors are controlled by lipophilic signaling molecules: endocrine nuclear receptors bind various steroid hormones, thyroid hormone, or the biologically active forms of vitamins A and D and retinoic acid, adopted orphan nuclear receptors bind to various lipids, metabolic intermediates, or xenobiotics, and orphan receptors have no known endogenous ligand but still operate as transcription factors. Because of their ability to directly interact with and control DNA expression, they play a significant role in cancer, diabetes, immune disorders, and other pathologies.
Endogenous ligand of the human arylhydrocarbon receptor
CH-223191 is a potent arylhydrocarbon receptor antagonist
6-Formylindolo[3,2-b]carbazole
Ultrapotent arylhydrocarbon receptor agonist
GW-501516 is a potent and selective PPARδ agonist
Potent and selective PPARγ agonist
WY-14643 is a selective PPARα agonist
Endogenous ligand for LXR
Endogenous ligand for LXR
SR9243 is an LXR inverse agonist that reduces glycolytic and lipogenic gene expression
SR1001 is an inverse agonist for both RORα and RORγt.
SR0987 is an RORγt agonist that drives proliferation of Th17 cells ansd decreases PD-1 levels
Stable retinoic acid analog that acts as a selective RARβ and RARγ agonist.
Ro 41-5253 is a selective RARα antagonist