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-W014075R
    1-Hydroxypyrene (Standard)
    		Agonist
    1-Hydroxypyrene (Standard) is the analytical standard of 1-Hydroxypyrene (HY-W014075). This product is intended for research and analytical applications. 1-Hydroxypyrene, a biomarker of exposure to polycyclic aromatic hydrocarbons (PAHs), is analyzed in urine samples. 1-Hydroxypyrene is the major biomarker of exposure to pyrenes. 1-Hydroxypyrene is the orally active agonist for aryl hydrocarbon receptor (AhR) and can lead to renal fibrosis.
    1-Hydroxypyrene (Standard)
  • HY-B0311AS
    Carbidopa-d3 monohydrate
    		Modulator ≥98.0%
    Carbidopa-d3 (monohydrate) is the deuterium labeled Carbidopa monohydrate. Carbidopa ((S)-(-)-Carbidopa) monohydrate, a peripheral decarboxylase inhibitor, can be used for the research of Parkinson's disease. Carbidopa monohydrate is a selective aryl hydrocarbon receptor (AhR) modulator. Carbidopa monohydrate inhibits pancreatic cancer cell and tumor growth[1][2].
    Carbidopa-d<sub>3</sub> monohydrate
  • HY-104026S1
    L-Kynurenine-d4-1
    		Agonist
    L-Kynurenine-d4-1 is deuterium labeled L-Kynurenine. L-Kynurenine is a metabolite of the amino acid L-tryptophan. L-Kynurenine is an aryl hydrocarbon receptor agonist.
    L-Kynurenine-d<sub>4</sub>-1
  • HY-W338764
    AHR agonist 3
    		Antagonist 99.79%
    AHR agonist 3 is an aryl hydrocarbon receptor (AhR) agonist, that can induces cell cycle arrest or apoptosis via activation of tumor-suppressive transcriptional programs. AHR agonist 3 inhibits triple-negative breast cancer (TNBC) stem cell growth via AhR while exhibits minimal cytotoxicity against normal human primary cells and can be used for cancer research.
    AHR agonist 3
  • 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-104026S5
    L-Kynurenine-13C10 sulfate hydrate
    L-Kynurenine-13C10 sulfate hydrate is the C13 labeled L-Kynurenine sulfate hydrate. L-Kynurenine is an aryl hydrocarbon receptor agonist.
    L-Kynurenine-<sup>13</sup>C<sub>10</sub> sulfate hydrate
  • HY-D0932R
    Sudan IV (Standard)
    		Agonist
    Sudan IV (Standard) (Solvent Red 24 (Standard)) is the analytical standard of Sudan IV (HY-D0932). This product is intended for research and analytical applications. Sudan IV is an agonist of the aryl hydrocarbon receptor (AhR) that activates downstream signaling pathways and induces CYP1A1 expression. Sudan IV promotes CYP1A1 gene transcription by activating AhR-ARNT heterodimers and binding to exogenous response elements (XREs) on DNA, thereby enhancing drug metabolizing enzyme activity. Sudan IV can be used to study the toxicity mechanisms of industrial dyes and the effects of interactions with serum proteins (such as bovine serum albumin (BSA)) on their distribution in vivo. Sudan IV is a fat-soluble diazo dye that can be used to stain lipids, triglycerides, and lipoproteins on frozen sections.
    Sudan IV (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-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-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-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
  • HY-B0845R
    Prochloraz (Standard)
    		Activator
    Prochloraz (Standard) is the analytical standard of Prochloraz. This product is intended for research and analytical applications. Prochloraz is an imidazole antifungal. Prochloraz is as an estrogen receptor (ER) and androgen receptor (AR) antagonist and an aromatase inhibitor with IC50 values of 25 μM, 4 μM and 0.3 μM, respectively. Prochloraz is able to activate the aryl hydrocarbon receptor (AhR) having an EC50 of 1 μM.
    Prochloraz (Standard)
  • HY-W764758
    3-OH-Kynurenamine dihydroiodide
    		Activator
    3-OH-Kynurenamine dihydroiodide is the dihydroiodide form of 3-OH-Kynurenamine (HY-156908). 3-OH-Kynurenamine dihydroiodide is an activator for aryl hydrocarbon receptor (AhR), and thus regulates the immune response. 3-OH-Kynurenamine dihydroiodide upregulates the expressions of Ido1 and Tgfb1, ameliorates the skin inflammation in psoriasis mouse model and kidney damage in nephrotoxic lupus mouse model.
    3-OH-Kynurenamine dihydroiodide
  • HY-N4069
    Lupinalbin A
    		Agonist
    Lupinalbin A (Boeravinone L) is a dipeptidyl peptidase 4 (DPP4) and α-glucosidase inhibitor with IC50 values ​​of 45.2 and 53.4 µM, respectively. Lupinalbin A exhibits antidiabetic activity.
    Lupinalbin A
  • HY-170514
    1,2,3,7,8,9-Hexachlorodibenzofuran
    		Ligand
    1,2,3,7,8,9-Hexachlorodibenzofuran is a polychlorinated dibenzofuran homologue. 1,2,3,7,8,9-Hexachlorodibenzofuran can interact with AhR. 1,2,3,7,8, 9-hexachlorodibenzofuran is highly toxic, teratogenic, carcinogenic and mutagenic.
    1,2,3,7,8,9-Hexachlorodibenzofuran
Cat. No. Product Name / Synonyms Application Reactivity