CB7993113 is a potent AHR antagonist, with an IC50 of 0.33 μM. CB7993113 directly binds AHR protein and blocks AHR nuclear translocation. CB7993113 inhibits polycyclic aromatic drocarbon (PAH)- and TCDD-induced reporter activity by 75% and 90% respectively.
CB7993113 exhibits no toxicity when added at concentrations at least up to 20 μM to several human cells including HepG2 hepatoma cells, BP1, D3, Hs578T, or MDA-MB-231 breast cancer cells, and primary human-induced pluripotent stem cells[1].CB7993113 significantly reduces the invasive phenotype of ER-/PR-/HER2- breast cancer cells in vitro[1].
CB7993113 effectively blocks acute, 50 mg/kg DMBA-induced hepatic CYP1A1 induction and bone marrow toxicity in vivo[1].
References:
[1]. Parks AJ, et al. In silico identification of an aryl drocarbon receptor antagonist with biological activity in vitro and in vivo. Mol Pharmacol. 2014 Nov;86(5):593-608.