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AhR

AhR Products

All (18)
AhR Inhibitors (2)
AhR Antagonists (7)
AhR Agonists (9)
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Catalog No.	Product Name	Information	Product Use Citations
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 Cell Commun Signal, 2024, 22(1):473
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).	Int J Biol Sci, 2024, 20(6):2008-2026 Cell Mol Life Sci, 2024, 81(1):101 Cell Mol Life Sci, 2024, 81(1):384
S7711	CH-223191	CH-223191 is a potent and specific aryl hydrocarbon receptor (AhR) antagonist with IC50 of 30 nM.	Cancer Commun (Lond), 2024, 10.1002/cac2.12545 Theranostics, 2024, 14(7):2719-2735 Proc Natl Acad Sci U S A, 2024, 121(11):e2317658121
S2858	SR1 (StemRegenin 1)	SR1 (StemRegenin 1) is an aryl hydrocarbon receptor (AhR) inhibitor with IC50 of 127 nM in a cell-free assay.	Nat Biotechnol, 2024, 10.1038/s41587-024-02360-7 Biochem Pharmacol, 2024, 223:116172 iScience, 2024, 27(5):109682
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.	Nat Commun, 2024, 15(1):8708 bioRxiv, 2024, 2024.07.02.601567 EMBO J, 2023, e110620.
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.	Cancer Commun (Lond), 2024, 10.1002/cac2.12545 Commun Biol, 2024, 7(1):442 EMBO Mol Med, 2022, 14(3):e14552
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.	Mol Cancer Res, 2024, 10.1158/1541-7786.MCR-24-0151 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.	iScience, 2024, 27(5):109682
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.
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.	Cancer Commun (Lond), 2024, 10.1002/cac2.12545 Commun Biol, 2024, 7(1):442 EMBO Mol Med, 2022, 14(3):e14552
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 Cell Commun Signal, 2024, 22(1):473
S7711	CH-223191	CH-223191 is a potent and specific aryl hydrocarbon receptor (AhR) antagonist with IC50 of 30 nM.	Cancer Commun (Lond), 2024, 10.1002/cac2.12545 Theranostics, 2024, 14(7):2719-2735 Proc Natl Acad Sci U S A, 2024, 121(11):e2317658121
S2858	SR1 (StemRegenin 1)	SR1 (StemRegenin 1) is an aryl hydrocarbon receptor (AhR) inhibitor with IC50 of 127 nM in a cell-free assay.	Nat Biotechnol, 2024, 10.1038/s41587-024-02360-7 Biochem Pharmacol, 2024, 223:116172 iScience, 2024, 27(5):109682
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).	Int J Biol Sci, 2024, 20(6):2008-2026 Cell Mol Life Sci, 2024, 81(1):101 Cell Mol Life Sci, 2024, 81(1):384
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.	Nat Commun, 2024, 15(1):8708 bioRxiv, 2024, 2024.07.02.601567 EMBO J, 2023, e110620.
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.	Mol Cancer Res, 2024, 10.1158/1541-7786.MCR-24-0151 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.	iScience, 2024, 27(5):109682
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.

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