AhR

AhR製品

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  • AhR阻害剤 (2)
  • AhR拮抗剤(7)
  • AhR作動薬(9)
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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.
Nat Commun, 2024, 15(1):987
Adv Sci (Weinh), 2024, 11(4):e2304987
Cancer Cell Int, 2024, 24(1):54
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).
Cell Death Dis, 2023, 14(10):672
iScience, 2023, 26(7):107090
Int J Mol Sci, 2023, 24(20)15258
S7711 CH-223191 CH-223191 is a potent and specific aryl hydrocarbon receptor (AhR) antagonist with IC50 of 30 nM.
Cell Rep Med, 2023, 4(8):101128
MedComm (2020), 2023, 4(2):e242
MedComm (2020), 2023, 4(2):e242
S2858 SR1 (StemRegenin 1) SR1 (StemRegenin 1) is an aryl hydrocarbon receptor (AhR) inhibitor with IC50 of 127 nM in a cell-free assay.
Transl Oncol, 2024, 42:101900
Microbiome, 2023, 10.1186/s40168-023-01551-9
Microbiome, 2023, 11(1):102
S1247 Leflunomide Leflunomide 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.
EMBO J, 2023, e110620.
Respir Res, 2023, 24(1):319
Transl Cancer Res, 2023, 12(9):2294-2307
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.
Cell Death Dis, 2023, 14(1):18
Front Microbiol, 2022, 13:934786
J Agric Food Chem, 2020, 10.1021/acs.jafc.0c06319
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.
EMBO Mol Med, 2022, 14(3):e14552
Acta Biochim Biophys Sin (Shanghai), 2021, gmab017
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.
J Med Chem, 2022, 2
Mol Cancer Ther, 2022, molcanther.0841.2021
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.
Cell Death Dis, 2023, 14(1):18
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
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
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.
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.
S0154 CAY10465 CAY 10465 is a selective and high-affinity agonist on aryl hydrocarbon receptor (AhR) with Ki of 0.2 nM.
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.
S9092 Norisoboldine Norisoboldine (Laurelliptine), a natural aryl hydrocarbon receptor (AhR) agonist, attenuates ulcerative colitis (UC) and induces the generation of Treg cells.
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.
E0143 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.
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).
Cell Death Dis, 2023, 14(10):672
iScience, 2023, 26(7):107090
Int J Mol Sci, 2023, 24(20)15258
S1247 Leflunomide Leflunomide 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.
EMBO J, 2023, e110620.
Respir Res, 2023, 24(1):319
Transl Cancer Res, 2023, 12(9):2294-2307
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.
Cell Death Dis, 2023, 14(1):18
Front Microbiol, 2022, 13:934786
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.
J Med Chem, 2022, 2
Mol Cancer Ther, 2022, molcanther.0841.2021
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
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.
Int J Mol Sci, 2020, 21(14):5025
Mol Biol Rep, 2020, 47(3):2217-2230
S0154 CAY10465 CAY 10465 is a selective and high-affinity agonist on aryl hydrocarbon receptor (AhR) with Ki of 0.2 nM.
S9092 Norisoboldine Norisoboldine (Laurelliptine), a natural aryl hydrocarbon receptor (AhR) agonist, attenuates ulcerative colitis (UC) and induces the generation of Treg cells.
E0143 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.
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.
EMBO Mol Med, 2022, 14(3):e14552
Acta Biochim Biophys Sin (Shanghai), 2021, gmab017
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.
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.
Nat Commun, 2024, 15(1):987
Adv Sci (Weinh), 2024, 11(4):e2304987
Cancer Cell Int, 2024, 24(1):54
S7711 CH-223191 CH-223191 is a potent and specific aryl hydrocarbon receptor (AhR) antagonist with IC50 of 30 nM.
Cell Rep Med, 2023, 4(8):101128
MedComm (2020), 2023, 4(2):e242
MedComm (2020), 2023, 4(2):e242
S2858 SR1 (StemRegenin 1) SR1 (StemRegenin 1) is an aryl hydrocarbon receptor (AhR) inhibitor with IC50 of 127 nM in a cell-free assay.
Transl Oncol, 2024, 42:101900
Microbiome, 2023, 10.1186/s40168-023-01551-9
Microbiome, 2023, 11(1):102
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.
Cell Death Dis, 2023, 14(1):18
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
S6560 PDM2 PDM2 is a potent and selective aryl hydrocarbon receptor (AhR) antagonist.
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.
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).
Cell Death Dis, 2023, 14(10):672
iScience, 2023, 26(7):107090
Int J Mol Sci, 2023, 24(20)15258
S1247 Leflunomide Leflunomide 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.
EMBO J, 2023, e110620.
Respir Res, 2023, 24(1):319
Transl Cancer Res, 2023, 12(9):2294-2307
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.
Cell Death Dis, 2023, 14(1):18
Front Microbiol, 2022, 13:934786
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.
J Med Chem, 2022, 2
Mol Cancer Ther, 2022, molcanther.0841.2021
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
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.
Int J Mol Sci, 2020, 21(14):5025
Mol Biol Rep, 2020, 47(3):2217-2230
S0154 CAY10465 CAY 10465 is a selective and high-affinity agonist on aryl hydrocarbon receptor (AhR) with Ki of 0.2 nM.
S9092 Norisoboldine Norisoboldine (Laurelliptine), a natural aryl hydrocarbon receptor (AhR) agonist, attenuates ulcerative colitis (UC) and induces the generation of Treg cells.
E0143 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.

AhR阻害剤の選択性比較

Tags: AhR inhibitor|AhR agonist|AhR activator|AhR inducer|AhR antagonist|AhR signaling pathway|AhR assay kit