AhR

Inhibitory Selectivity

AhR Products

Catalog No. Information Product Use Citations Product Validations
S3205New

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.

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.

S2858

StemRegenin 1 (SR1)

StemRegenin 1 (SR1) is an aryl hydrocarbon receptor (AhR) inhibitor with IC50 of 127 nM in a cell-free assay.

S7711

CH-223191

CH-223191 is a potent and specific aryl hydrocarbon receptor (AhR) antagonist with IC50 of 30 nM.

S8995New

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.

S6560

PDM2

PDM2 is a potent and selective aryl hydrocarbon receptor (AhR) antagonist.

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).

S1247

Leflunomide

Leflunomide (HWA486) 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.

S9700New

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.

S0154New

CAY10465

CAY 10465 is a selective and high-affinity agonist on aryl hydrocarbon receptor (AhR) with Ki of 0.2 nM.

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.

S9092

Norisoboldine

Norisoboldine, a natural aryl hydrocarbon receptor (AhR) agonist, attenuates ulcerative colitis (UC) and induces the generation of Treg cells.

S5839

L-Kynurenine

L-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.

Catalog No. Information Product Use Citations Product Validations
S3205New

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.

Catalog No. Information Product Use Citations Product Validations
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.

S2858

StemRegenin 1 (SR1)

StemRegenin 1 (SR1) is an aryl hydrocarbon receptor (AhR) inhibitor with IC50 of 127 nM in a cell-free assay.

S7711

CH-223191

CH-223191 is a potent and specific aryl hydrocarbon receptor (AhR) antagonist with IC50 of 30 nM.

S8995New

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.

S6560

PDM2

PDM2 is a potent and selective aryl hydrocarbon receptor (AhR) antagonist.

Catalog No. Information Product Use Citations Product Validations
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).

S1247

Leflunomide

Leflunomide (HWA486) 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.

S9700New

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.

S0154New

CAY10465

CAY 10465 is a selective and high-affinity agonist on aryl hydrocarbon receptor (AhR) with Ki of 0.2 nM.

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.

S9092

Norisoboldine

Norisoboldine, a natural aryl hydrocarbon receptor (AhR) agonist, attenuates ulcerative colitis (UC) and induces the generation of Treg cells.

S5839

L-Kynurenine

L-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.