AhR

Choose Selective AhR Inhibitors

AhR Products

  • All (18)
  • AhR Inhibitors (2)
  • AhR Antagonists (7)
  • AhR Agonists (9)
  • New AhR Products
Catalog No. Product Name Information Product Use Citations Product Validations
S3205 Perillaldehyde Perillaldehyde (Perilladehyde, Perillal, PAE, PA), the main component of Perilla frutescens (a traditional medicinal antioxidant herb), inhibits BaP-induced AHR activation and ROS production, inhibits BaP/AHR-mediated release of the CCL2 chemokine, and activats the NRF2/HO1 antioxidant pathway.
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.
Acta Biochim Biophys Sin (Shanghai), 2021, gmab017
S0155 PDM-11 PDM-11 is a derivative of resveratrol that exhibits stronger antagonist affinity for arylhydrocarbon receptors (AhR) than resveratrol, without any affinity for the estrogen receptor.
S1177 PD98059 PD98059 is a non-ATP competitive MEK inhibitor with IC50 of 2 μM in a cell-free assay, specifically inhibits MEK-1-mediated activation of MAPK; does not directly inhibit ERK1 or ERK2. PD98059 is a ligand for the aryl hydrocarbon receptor (AHR) and functions as an AHR antagonist.
Cells, 2022, 11(1)134
Microbiol Spectr, 2022, e0188121
Cancer Immunol Immunother, 2022, 10.1007/s00262-021-03126-9
S2858 StemRegenin 1 (SR1) StemRegenin 1 (SR1) is an aryl hydrocarbon receptor (AhR) inhibitor with IC50 of 127 nM in a cell-free assay.
Stem Cell Res, 2021, 53:102287
Mol Cancer Ther, 2021, molcanther.0029.2021
Acta Biochim Biophys Sin (Shanghai), 2021, gmab122
S6560 PDM2 PDM2 is a potent and selective aryl hydrocarbon receptor (AhR) antagonist.
S6926 GNF351 GNF351 is a potent antagonist of aryl hydrocarbon receptor (AHR). GNF351 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.
Front Pharmacol, 2021, 12:655281
S7711 CH-223191 CH-223191 is a potent and specific aryl hydrocarbon receptor (AhR) antagonist with IC50 of 30 nM.
EMBO Mol Med, 2021, e13466
J Immunol, 2021, 207(6):1672-1682
Mol Hum Reprod, 2021, 27(3)gaab003
S8995 BAY 2416964 BAY 2416964 (compound 192) is a potent and orally active antagonist of aryl hydrocarbon receptor (AhR) with IC50 of 341 nM. BAY 2416964 has the potential in the treatment of solid tumors.
E0143New ITE

ITE (2-(1′H-indole-3′-carbonyl)-thiazole-4-carboxylic acid methyl ester) is a potent endogenous agonist of aryl hydrocarbon receptor (AhR) that directly binds to AHR with a Ki of 3 nM.

S0154 CAY10465 CAY 10465 is a selective and high-affinity agonist on aryl hydrocarbon receptor (AhR) with Ki of 0.2 nM.
S1247 Leflunomide (HWA486) Leflunomide (HWA486, RS-34821, SU101, Arava) is a pyrimidine synthesis and protein tyrosine kinase inhibitor belonging to the DMARD, used as an immunosuppressant agent. The active metabolite of Leflunomide is A77 1726, which inhibits dihydroorotate dehydrogenase (DHODH). Leflunomide is also an agonist of the AhR.
Cell Death Dis, 2021, 12(9):821
Front Immunol, 2021, 12:685984
Cell Transplant, 2021, 30:9636897211054503
S2292 Diosmin Diosmin is an agonist of the aryl hydrocarbon receptor (AhR). Diosmin is a semisynthetic phlebotropic agent and a flavonoid found in a variety of citrus fruits.
Mol Biol Rep, 2020, 47(3):2217-2230
Int J Mol Sci, 2020, 21(14):5025
S2929 Pifithrin-α (PFTα) HBr 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).
Br J Pharmacol, 2021, 10.1111/bph.15385
Development, 2021, dev.188276
Biochim Biophys Acta Mol Cell Res, 2021, 1869(2):119174
S5839 L-Kynurenine L-Kynurenine ((S)-Kynurenine) is a aryl hydrocarbon receptor agonist. L-Kynurenine is a metabolite of the amino acid L-tryptophan used in the production of niacin and a central compound of the tryptophan metabolism pathway.
Theranostics, 2021, 11(19):9623-9651
S9092 Norisoboldine Norisoboldine (Laurelliptine), a natural aryl hydrocarbon receptor (AhR) agonist, attenuates ulcerative colitis (UC) and induces the generation of Treg cells.
S9682 FICZ 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.
J Agric Food Chem, 2020, 10.1021/acs.jafc.0c06319
S9700 Tapinarof 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.
S3205 Perillaldehyde Perillaldehyde (Perilladehyde, Perillal, PAE, PA), the main component of Perilla frutescens (a traditional medicinal antioxidant herb), inhibits BaP-induced AHR activation and ROS production, inhibits BaP/AHR-mediated release of the CCL2 chemokine, and activats the NRF2/HO1 antioxidant pathway.
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.
Acta Biochim Biophys Sin (Shanghai), 2021, gmab017
S0155 PDM-11 PDM-11 is a derivative of resveratrol that exhibits stronger antagonist affinity for arylhydrocarbon receptors (AhR) than resveratrol, without any affinity for the estrogen receptor.
S1177 PD98059 PD98059 is a non-ATP competitive MEK inhibitor with IC50 of 2 μM in a cell-free assay, specifically inhibits MEK-1-mediated activation of MAPK; does not directly inhibit ERK1 or ERK2. PD98059 is a ligand for the aryl hydrocarbon receptor (AHR) and functions as an AHR antagonist.
Cells, 2022, 11(1)134
Microbiol Spectr, 2022, e0188121
Cancer Immunol Immunother, 2022, 10.1007/s00262-021-03126-9
S2858 StemRegenin 1 (SR1) StemRegenin 1 (SR1) is an aryl hydrocarbon receptor (AhR) inhibitor with IC50 of 127 nM in a cell-free assay.
Stem Cell Res, 2021, 53:102287
Mol Cancer Ther, 2021, molcanther.0029.2021
Acta Biochim Biophys Sin (Shanghai), 2021, gmab122
S6560 PDM2 PDM2 is a potent and selective aryl hydrocarbon receptor (AhR) antagonist.
S6926 GNF351 GNF351 is a potent antagonist of aryl hydrocarbon receptor (AHR). GNF351 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.
Front Pharmacol, 2021, 12:655281
S7711 CH-223191 CH-223191 is a potent and specific aryl hydrocarbon receptor (AhR) antagonist with IC50 of 30 nM.
EMBO Mol Med, 2021, e13466
J Immunol, 2021, 207(6):1672-1682
Mol Hum Reprod, 2021, 27(3)gaab003
S8995 BAY 2416964 BAY 2416964 (compound 192) is a potent and orally active antagonist of aryl hydrocarbon receptor (AhR) with IC50 of 341 nM. BAY 2416964 has the potential in the treatment of solid tumors.
E0143New ITE

ITE (2-(1′H-indole-3′-carbonyl)-thiazole-4-carboxylic acid methyl ester) is a potent endogenous agonist of aryl hydrocarbon receptor (AhR) that directly binds to AHR with a Ki of 3 nM.

S0154 CAY10465 CAY 10465 is a selective and high-affinity agonist on aryl hydrocarbon receptor (AhR) with Ki of 0.2 nM.
S1247 Leflunomide (HWA486) Leflunomide (HWA486, RS-34821, SU101, Arava) is a pyrimidine synthesis and protein tyrosine kinase inhibitor belonging to the DMARD, used as an immunosuppressant agent. The active metabolite of Leflunomide is A77 1726, which inhibits dihydroorotate dehydrogenase (DHODH). Leflunomide is also an agonist of the AhR.
Cell Death Dis, 2021, 12(9):821
Front Immunol, 2021, 12:685984
Cell Transplant, 2021, 30:9636897211054503
S2292 Diosmin Diosmin is an agonist of the aryl hydrocarbon receptor (AhR). Diosmin is a semisynthetic phlebotropic agent and a flavonoid found in a variety of citrus fruits.
Mol Biol Rep, 2020, 47(3):2217-2230
Int J Mol Sci, 2020, 21(14):5025
S2929 Pifithrin-α (PFTα) HBr 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).
Br J Pharmacol, 2021, 10.1111/bph.15385
Development, 2021, dev.188276
Biochim Biophys Acta Mol Cell Res, 2021, 1869(2):119174
S5839 L-Kynurenine L-Kynurenine ((S)-Kynurenine) is a aryl hydrocarbon receptor agonist. L-Kynurenine is a metabolite of the amino acid L-tryptophan used in the production of niacin and a central compound of the tryptophan metabolism pathway.
Theranostics, 2021, 11(19):9623-9651
S9092 Norisoboldine Norisoboldine (Laurelliptine), a natural aryl hydrocarbon receptor (AhR) agonist, attenuates ulcerative colitis (UC) and induces the generation of Treg cells.
S9682 FICZ 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.
J Agric Food Chem, 2020, 10.1021/acs.jafc.0c06319
S9700 Tapinarof 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.
E0143New ITE

ITE (2-(1′H-indole-3′-carbonyl)-thiazole-4-carboxylic acid methyl ester) is a potent endogenous agonist of aryl hydrocarbon receptor (AhR) that directly binds to AHR with a Ki of 3 nM.