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AhR Agonists/Antagonist

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Cat.No. Product Name Information Product Use Citations Product Validations
S8995 BAY 2416964 BAY 2416964 (compound 192) is a potent and orally active antagonist of aryl hydrocarbon receptor (AhR) with IC50 of 341 nM. This compound has the potential in the treatment of solid tumors.
Ecotoxicol Environ Saf, 2025, 290:117743
JBMR Plus, 2025, 9(6):ziaf067
NAR Genom Bioinform, 2025, 7(2):lqaf052
S2858 Stemregenin 1 (SR1) StemRegenin 1 (SR1) is an aryl hydrocarbon receptor (AhR) inhibitor with IC50 of 127 nM in a cell-free assay.
Cell, 2025, S0092-8674(25)01149-3
Nat Commun, 2025, 16(1):2384
Cell Rep Med, 2025, 6(8):102297
Verified customer review of Stemregenin 1 (SR1)
S2929 Pifithrin-α (PFTα) Hhydrobromide Pifithrin-α is an inhibitor of p53, inhibiting p53-dependent transactivation of p53-responsive genes. Pifithrin-α is also a potent agonist of the aryl hydrocarbon receptor (AhR).
J Adv Res, 2025, S2090-1232(25)00192-4
Front Pharmacol, 2025, 16:1608156
J Cell Mol Med, 2025, 29(11):e70641
Verified customer review of Pifithrin-α (PFTα) Hhydrobromide
S7711 CH-223191 CH-223191 is a potent and specific aryl hydrocarbon receptor (AhR) antagonist with IC50 of 30 nM.
Cells, 2025, 14(8)605
Chem Biol Interact, 2025, 412:111478
Front Nutr, 2025, 12:1500293
Verified customer review of CH-223191
S8842 BAY-218 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.
Sci Rep, 2025, 15(1):8826
Scientific Reports, 2025, 8826
Cancer Commun (Lond), 2024, 10.1002/cac2.12545
S9700 Tapinarof (Benvitimod, WBI-1001) Tapinarof (GSK2894512, Benvitimod, WBI 1001, DHPS, DMVT 505) is a natural agonist of aryl hydrocarbon receptor (AhR) and induces nuclear translocation of AhR in immortalized keratinocytes (HaCaT) with EC50 of 0.16 nM. Tapinarof induces cellular apoptosis in CD4+ T cells in a dosedependent manner with IC50 of 5.2 μM.
Pharmaceutics, 2025, 17(6)731
Molecular Cancer Therapeutics, 2024, MCT-24-0211
Mol Cancer Res, 2024, 10.1158/1541-7786.MCR-24-0151
S9682 FICZ (6-Formylindolo[3,2-b]carbazole) FICZ (6-Formylindolo[3,2-b]carbazole) is a potent agonist of aryl hydrocarbon receptor (AhR) that is efficiently metabolized by AHR-regulated cytochrome P4501 enzymes.
Biochem Pharmacol, 2025, 236:116872
Front Immunol, 2024, 15:1513595
Cell Death Dis, 2023, 14(1):18
S2292 Diosmin Diosmin is an agonist of the aryl hydrocarbon receptor (AhR). This compound is a semisynthetic phlebotropic agent and a flavonoid found in a variety of citrus fruits.
Int J Mol Sci, 2020, 21(14):5025
Mol Biol Rep, 2020, 47(3):2217-2230
S6560 PDM2 PDM2 is a potent and selective aryl hydrocarbon receptor (AhR) antagonist.
Cancer Cell Int, 2021, 21(1):538
Cancer Cell International, 2021, 538
S6926 GNF351 GNF351 is a potent antagonist of aryl hydrocarbon receptor (AHR). This compound interacts directly with the AHR ligand binding pocket and competes with a well-characterized photoaffinity AHR ligand for binding to the AHR with IC50 of 62 nM.
Frontiers in Pharmacology, 2021, 655281
Front Pharmacol, 2021, 12:655281