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Aryl hydrocarbon receptor (AhR) ligands act on a ligand-activated transcription factor of the bHLH-PAS family. Cloning of the receptor complementary DNA in 1992 showed that AhR combines a basic helix-loop-helix (bHLH) domain with a Per-Arnt-Sim (PAS) domain. The tryptophan metabolite kynurenine was later described as an endogenous agonist produced by tryptophan 2,3-dioxygenase. Antagonists of AhR were shown to support the expansion of human hematopoietic stem cells in culture, which made StemRegenin 1 a common tool in that work. CH-223191, ITE, tapinarof and L-Kynurenine complete a set that covers both receptor activation and blockade in reporter and gene expression assays.
