Potent aryl hydrocarbon receptor (AhR) agonist; orally bioavailable
Potent aryl hydrocarbon receptor (AhR) agonist, discovered as a screening hit (IC50 = 2.6 nM). Directly binds CD4+ T cells to induce AhR-dependent Tregs. Suppresses IL-17 production and prevents insulitis in NOD mice. In vivo half llife ~ 2 hours, orally bioavailable.
Punj et al (2014) Benzimidazoisoquinolines: a new class of rapidly metabolized aryl hydrocarbon receptor (AhR) ligands that induce AhR-dependent Tregs and prevent murine graft-versus-host disease. PLoS One 9 e88726 PMID:24586378 |Ehrlich et al (2016) Activation of the aryl hydrocarbon receptor by 10-Cl-BBQ prevents insulitis and effector T cell development independently of Foxp3+ regulatory T Cells in nonobese diabetic mice. J.Immunol. 196 264 PMID:26573835
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