BAY-218 is a potent and selective small-molecule AhR inhibitor, inhibiting AhR nuclear translocation, dioxin response element (DRE)-luciferase reporter expression and AhR-regulated target gene expression induced by both exogenous and endogenous AhR ligand
BAY-218 is a potent and selective small-molecule AhR inhibitor, inhibiting AhR nuclear translocation, dioxin response element (DRE)-luciferase reporter expression and AhR-regulated target gene expression induced by both exogenous and endogenous AhR ligands.
Mechanistically, BAY-218 inhibits AhR nuclear translocation, dioxin response element (DRE)-luciferase reporter expression and AhR-regulated target gene expression induced by both exogenous and endogenous AhR ligands. In vitro, BAY-218 rescues TNFα production from kynurenic acid(KA)-suppressed LPS-treated primary human monocytes[1].
In vivo, BAY-218 enhances anti-tumoral immune responses and reduced tumor growth in the syngeneic mouse tumor models CT26 and B16-OVA. Furthermore, BAY-218 enhances therapeutic efficacy of an anti-PD-L1 antibody in the CT26 model[1].
[1] Ilona Gutcher, et al. AACR Cancer Res. 2019, 79(13 Suppl):Abstract nr 1288.
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