The aryl hydrocarbon receptor (AhR) is a ligand-dependent intracellular transcription factor whose ligands include some of the most infamous xenobiotics, including dioxin, benzo[a]pyrene, and numerous polyaromatics from soot and coal tar.1 PDM 2 is an analog of resveratrol acting as a potent and selective AhR antagonist, with a Ki of 1.2 nM.2 PDM 2 is inactive as a ligand for the estrogen receptor even at 100 µM. As AhR knockout mice are insensitive to the carcinogenic effects of classical AhR ligands, PDM 2 is a potential therapeutic for the treatment for dioxin and other aryl hydrocarbon poisonings.
1
Denison, M.S., and Nagy, S.R. Activation of the aryl hydrocarbon receptor by structurally diverse exogenous and endogenous chemicals.. Annu Rev Pharmacol Toxicol43309-334(2003).
2
de Medina, P., Casper, R., Savouret, J., et al. Synthesis and biological properties of new stilbene derivatives of resveratrol as new selective aryl hydrocarbon modulators. J Med Chem48287-291(2005).
Room temperature
in continental US; may vary elsewhere
SMILES
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Clc1ccc(cc1)\C=C/c1cc(Cl)cc(Cl)c1
Background Reading
Denison, M.S., and Nagy, S.R. Activation of the aryl hydrocarbon receptor by structurally diverse exogenous and endogenous chemicals.. Annu Rev Pharmacol Toxicol43309-334(2003).
de Medina, P., Casper, R., Savouret, J., et al. Synthesis and biological properties of new stilbene derivatives of resveratrol as new selective aryl hydrocarbon modulators. J Med Chem48287-291(2005).
PDM 2 is available in the following screening
library: