2. Signaling Pathways
  3. Immunology/Inflammation
  4. Aryl Hydrocarbon Receptor

Aryl Hydrocarbon Receptor

AhR

Aryl Hydrocarbon Receptor

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Aryl Hydrocarbon Receptor (AhR or AHR) is a cytoplasmic receptor and transcription factor that belongs to the family of basic helix-loop-helix transcription factors. The AhR is activated or inhibited by various types of exogenous and endogenous ligands. AhR is an important factor in immunity and tissue homeostasis, and structurally diverse compounds from the environment, diet, microbiome, and host metabolism can induce AhR activity, such as 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD).

Endogenous ligands include indigoids, heme metabolites, eicosanoids, tryptophan derivatives, and equilenin. Exogenous ligands include polycyclic aromatic hydrocarbons, polychlorinated biphenyls, natural compounds, and small molecule compounds. The different structures and properties of AhR ligands mean that when they combine with AhR they have distinct biological effects.

Unliganded AHR is sequestered in the cytoplasm by chaperone proteins including Hsp90, AHR-interacting protein (AIP), and p23. Upon ligand binding, AHR translocates to the nucleus and heterodimerizes with ARNT. The AHR-ARNT complex regulates transcription by binding with high affinity to specific DNA sequences termed aryl hydrocarbon response elements located in the regulatory regions of target genes including CYP1A1, CYP1B1, and TIPARP.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-W517092
    1,2,3,4,7,8,9-Heptachlorodibenzofuran
    		Inhibitor
    1,2,3,4,7,8,9-Heptachlorodibenzofuran (1,2,3,4,7,8,9-HpCDF) is a compound that induces the expression of CYP1A1 and CYP1B1 genes in human peripheral blood lymphocytes, while also promoting the expression of the aryl hydrocarbon receptor repressor (AhRR). 1,2,3,4,7,8,9-Heptachlorodibenzofuran can increase ethoxyresorufin-O-deethylase (EROD) activity in isolated human peripheral blood lymphocytes in a concentration-dependent manner, which serves as a marker of CYP1A1 activity. Furthermore, 1,2,3,4,7,8,9-Heptachlorodibenzofuran exhibits immunosuppressive effects by reducing the number of splenic plaque-forming cells in mice and increasing aryl hydrocarbon hydroxylase (AHH) activity in liver microsomes of mice injected with sheep red blood cells. 1,2,3,4,7,8,9-Heptachlorodibenzofuran can be used in research in the fields of immunology, metabolic diseases, and environmental toxicology.
    1,2,3,4,7,8,9-Heptachlorodibenzofuran
  • HY-W775354
    1,2,3,4,7,8-Hexachlorodibenzofuran
    		Inhibitor
    1,2,3,4,7,8-Hexachlorodibenzofuran (1,2,3,4,7,8-HxCDF) promotes the gene expressions of CYP1A1, CYP1B1, and aryl hydrocarbon receptor repressor (AhRR) in human peripheral blood lymphocytes (PBLs). 1,2,3,4,7,8-Hexachlorodibenzofuran activates the ethoxyresorufin-Odeethylase, achieves 20% of the maximum response caused by TCDD with a BMR20TCDD of 0.115-0.143 nM.
    1,2,3,4,7,8-Hexachlorodibenzofuran
  • HY-N6264R
    26-Deoxyactein (Standard)
    		Inhibitor
    26-Deoxyactein (Standard) is the analytical standard of 26-Deoxyactein. This product is intended for research and analytical applications. 26-Deoxyactein is a constituent isolated from Cimicifuga racemosa, prevents TCDD-induced osteoblasts damage. 26-Deoxyactein inhibits increased AhR, CYP1A1 and ERK levels.
    26-Deoxyactein (Standard)
  • HY-B0311R
    Carbidopa (Standard)
    		Modulator
    Carbidopa (Standard) is the analytical standard of Carbidopa. This product is intended for research and analytical applications. Carbidopa ((S)-(-)-Carbidopa), a peripheral decarboxylase inhibitor, can be used for the research of Parkinson's disease. Carbidopa is a selective aryl hydrocarbon receptor (AhR) modulator. Carbidopa inhibits pancreatic cancer cell and tumor growth.
    Carbidopa (Standard)
  • HY-100242R
    Mivotilate (Standard)
    		Activator
    Mivotilate (Standard) is the analytical standard of Mivotilate. This product is intended for research and analytical applications. Mivotilate is a nontoxic, potent activator of the aryl hydrocarbon receptor (AhR), and acts as a hepatoprotective agent.
    Mivotilate (Standard)
  • HY-163665
    AHR antagonist 8
    		Antagonist
    AHR antagonist 8 (compound SG-02) is a regulator of utrophin, a homolog of dystrophin, and an AhR antagonist (Kd: 41.68 nM). Studies have shown that 800 nM of AHR antagonist 8 can upregulate utrophin by 2.7 times. AHR antagonist 8 also stimulates increased MyHC expression, suggesting that it has the potential to enhance myogenesis. After ADME evaluation, AHR antagonist 8 also has a certain oral bioavailability.
    AHR antagonist 8
  • HY-109044R
    Tapinarof (Standard)
    		Agonist
    Tapinarof (Standard) is the analytical standard of Tapinarof. This product is intended for research and analytical applications. Tapinarof (WBI-1001) is a natural aryl hydrocarbon receptor (AhR) agonist with an EC50 of 13 nM. Tapinarof resolves skin inflammation in mice.
    Tapinarof (Standard)
  • HY-N4095R
    Brevifolincarboxylic acid (Standard)
    		Inhibitor
    Brevifolincarboxylic acid (Standard) is the analytical standard of Brevifolincarboxylic acid (HY-N4095). This product is intended for research and analytical applications. Brevifolincarboxylic acid is a phenolic compound. Brevifolincarboxylic acid can be isolated from Duchesnea chrysantha. Brevifolincarboxylic acid inhibits α-glucosidase with an IC50 value of 323.46 μM. Brevifolincarboxylic acid has an inhibitory effect on the aryl hydrocarbon receptor (AhR). Brevifolincarbacid scavenges ROS. Brevifolincarbacid restores the glucose uptake activity of myotubes. Brevifolincarboxylic acid has antitumor activity against lung and gastric cancer. Brevifolincarbacid can be used in the study of diabetes and inflammatory diseases.
    Brevifolincarboxylic acid (Standard)
  • HY-W011910R
    Potassium 1H-indol-3-yl sulfate (Standard)
    		Agonist
    Potassium 1H-indol-3-yl sulfate (Standard) is the analytical standard of Potassium 1H-indol-3-yl sulfate (HY-W011910). This product is intended for research and analytical applications. Potassium 1H-indol-3-yl sulfate is a metabolite of tryptophan, produced by intestinal microorganisms and combined with sulfate in the liver before entering the circulatory system. Potassium 1H-indol-3-yl sulfate is a potent endogenous agonist of the aryl hydrocarbon receptor (AhR) and a urinary toxin. Potassium 1H-indol-3-yl sulfate can be used for research on kidney diseases.
    Potassium 1H-indol-3-yl sulfate (Standard)
  • HY-124421R
    5F-203 (Standard)
    		Inducer
    5F-203 (Standard) is the analytical standard of 5F-203. This product is intended for research and analytical applications. 5F-203 (NSC-703786) is a cytotoxic molecule that forms DNA adducts and cell cycle arrest. 5F-203 induces aryl hydrocarbon receptor (AhR) signaling and elevates expression of CYP1A1. 5F-203 also increases the levels of reactive oxygen species as well as activates JNK, ERK, and p38.
    5F-203 (Standard)
  • HY-W587465
    9,10-Dichlorophenanthrene
    9,10-Dichlorophenanthrene is a chlorinated polycyclic aromatic hydrocarbon and is generally regarded as a carcinogen. It could activate the aryl hydrocarbon receptor (AhR) .
    9,10-Dichlorophenanthrene
  • HY-177563
    AhR modulator-2
    		Activator
    AhR modulator-2 (Compound Example 1) is an AHR activator, with an EC50 of 0.028 μM in HepG2-Lucia cells. AhR modulator-2 can be used for the study of diseases mediated by AHR protein, such as skin diseases and cancer.
    AhR modulator-2
  • HY-B0973R
    Dibenzothiophene (Standard)
    Dibenzothiophene (Standard) is the analytical standard of Dibenzothiophene (HY-B0973). This product is intended for research and analytical applications. Dibenzothiophene is an orally active and a noncompetitive CYP1A inhibitor. Dibenzothiophene inhibits CYP1A-mediated EROD activity with Km of 0.592 μM. Dibenzothiophene interacts with the AHR pathway. Dibenzothiophene enhances the embryotoxicity of β-naphthoflavone (HY-114740). Dibenzothiophene shows acute toxicity in mice. Dibenzothiophene is mainly used for the study of the mechanism of developmental toxicity in organisms.
    Dibenzothiophene (Standard)
  • HY-20888
    3'-Methoxy-4'-nitroflavone
    		Antagonist
    3'-Methoxy-4'-nitroflavone (MNF) is a specific aryl hydrocarbon receptor (AhR) antagonist. 3'-Methoxy-4'-nitroflavone activates AhR by inhibiting CYP1, the metabolic enzyme of the endogenous ligand FICZ (HY-12451), leading to the accumulation of FICZ. 3'-Methoxy-4'-nitroflavone reverses the anti-apoptotic effect of TCDD, attenuates the activation of Akt and Erk1/2 kinases and the expression of TGFα induced by TCDD. 3'-Methoxy-4'-nitroflavone can be used in research related to breast tumor promotion, rheumatoid arthritis, multiple sclerosis and inflammatory bowel disease.
    3'-Methoxy-4'-nitroflavone
  • HY-103222R
    DiMNF (Standard)
    		Modulator
    DiMNF (Standard) is the analytical standard of DiMNF (HY-103222). This product is intended for research and analytical applications. DiMNF (3',4'-Dimethoxy-αNF) is a selective aryl hydrocarbon receptor (AHR) modulator. DiMNF is a competitive AHR ligand (IC50 = 21 nM) with apparent antagonistic activity. DiMNF can be used as an anti-inflammatory agent.
    DiMNF (Standard)
  • HY-N1939R
    Icariside I (Standard)
    Icariside I (Standard) is the analytical standard of Icariside I (HY-N1939). This product is intended for research and analytical applications. Icariside I (GH01) is an orally active metabolite of icalin. Icariside I improves estrogen deficiency-induced osteoporosis by simultaneously regulating osteoblast and osteoclast differentiation. Icariside I promotes ATP (HY-B2176) or Nigericin (HY-127019)-induced mtROS production and NLRP3 inflammasome activation and causes idiosyncratic hepatotoxicity. Icariside I does not alter the activation of NLRC4 and AIM2 inflammasomes. Icariside I inhibits breast cancer proliferation, apoptosis, invasion, and metastasis by targeting the IL-6/STAT3 pathway. Icariside I is a kynurenine-AhR pathway inhibitor that alleviates cancer by blocking tumor immune escape.
    Icariside I (Standard)
  • HY-109044S
    Tapinarof-d5
    		Agonist
    Tapinarof-d5 (WBI-1001-d5) is deuterium labeled Tapinarof. Tapinarof (WBI-1001) is a natural aryl hydrocarbon receptor (AhR) agonist with an EC50 of 13 nM. Tapinarof resolves skin inflammation in mice.
    Tapinarof-d<sub>5</sub>
  • HY-15600B
    UPF-648 sodium salt
    UPF-648 sodium salt is an effective inhibitor of kynurenine 3-monooxygenase (KMO), achieving approximately 81% inhibition at a concentration of 1uM, with no inhibitory effect on kynurenine aminotransferase (KAT).
    UPF-648 sodium salt
  • HY-102023R
    GNF351 (Standard)
    		Antagonist
    GNF351 (Standard) is the analytical standard of GNF351 (HY-102023). This product is intended for research and analytical applications. GNF351 is a full aryl hydrocarbon receptor (AHR) antagonist. GNF351 competes with a photoaffinity AHR ligand for binding to the AHR with an IC50 of 62 nM. GNF351 is minimal toxicity in mouse or human keratinocytes.
    GNF351 (Standard)
  • HY-104026BS
    L-Kynurenine-13C10 sulfate
    		Agonist
    L-Kynurenine-13C10 (sulfate) is the 13C labeled L-Kynurenine sulfate. L-Kynurenine sulfate, an aryl hydrocarbon receptor (AHR) agonist that activates AHR-directed, naive T cell polarization to the anti-inflammatory Treg phenotype.
    L-Kynurenine-<sup>13</sup>C<sub>10</sub> sulfate
Cat. No. Product Name / Synonyms Application Reactivity