ahr antagonist-1

Bindarit (AF2838)is an aryl hydrocarbon receptor (AHR) antagonist with IC50 of 39.9 nM in the human glioblastoma U87 cell line. BAY-218 inhibition of AhR stimulates pro-inflammatory monocyte and T cell responses in vitro and drives anti-tumor immune responses, leading to reduced tumor growth in vivo.

AHR antagonist 5 is a potent and orally active aryl hydrocarbon receptor (AHR) antagonist(example 39; IC50 < 0.5 μΜ). It significantly inhibits tumor growth combined with checkpoint inhibitor anti-PD-1.

PDM11 (1-[2-(4-Chloro-phenyl)-vinyl]-3,5-diMeth) is an antagonist of aryl hydrocarbon receptor (AhR)

AHR antagonist 5 hemimaleate is a potent antagonist (IC50 < 0.5 μM) of the orally active aryl hydrocarbon receptor (AHR). aHR antagonist 5 hemimaleate in combination with the detection site inhibitor anti-PD-1 exhibited inhibitory effects on tumor growth.

Kynurenic acid, an active metabolite of tryptophan, is synthesized through a kynurenine intermediate by kynurenine aminotransferases (KATs). It acts as an antagonist of both NMDA and AMPA receptors, as well as α7 nicotinic acetylcholine receptors (nAChRs; EC50s = 235, 101, and 7 µM, respectively), and functions as an agonist for the aryl hydrocarbon receptor (AhR) and G protein-coupled receptor 35 (GPR35; EC50s = 1.4 and 39 µM, respectively). In a neonatal rat model of cerebral hypoxic-ischemia, induced by carotid artery ligation, administration of kynurenic acid at 300 mg kg prevents weight loss in the lesioned hemisphere. Additionally, at concentrations of 1 and 5 mg ml, it protects against neurodegeneration in the rhabdomere of the eye in an Htt93QtransgenicDrosophila model of Huntington's disease. Elevated levels of kynurenic acid in the cerebrospinal fluid have been observed in patients with schizophrenia.

CB7993113 is a potent AHR antagonist with an IC50 of 0.33 μM, directly binding the AHR protein and blocking its nuclear translocation. It inhibits polycyclic aromatic hydrocarbon (PAH)- and TCDD-induced reporter activity by 75% and 90%, respectively [1].

WAY-605471 is a AHR antagonist with IC50 of 0.5 - 1 μM.