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-W517076
    1,2,3,6,7,8-Hexachlorodibenzo-p-dioxin
    		Agonist
    1,2,3,6,7,8-Hexachlorodibenzo-p-dioxin (1,2,3,6,7,8-HxCDD) is an AHR agonist, with reported gene assay EC50 values of 5.4 nM at 4 hours and 9.3 nM at 8 hours. 1,2,3,6,7,8-Hexachlorodibenzo-p-dioxin (at doses of 0.5 and 2 µg/kg) has been shown to reduce the production of antibodies against sheep red blood cells in mice. 1,2,3,6,7,8-Hexachlorodibenzo-p-dioxin is an environmental pollutant, found in animal feed and detected in the air near municipal waste incinerators.
    1,2,3,6,7,8-Hexachlorodibenzo-p-dioxin
  • HY-W014701R
    1,4-Dihydroxy-2-naphthoic acid (Standard)
    		Activator
    1,4-Dihydroxy-2-naphthoic acid (Standard) is the analytical standard for 1,4-Dihydroxy-2-naphthoic acid (HY-W014701). 1,4-Dihydroxy-2-naphthoic acid is an orally active aryl hydrocarbon receptor (AhR) agonist and a bifidogenic growth stimulator. 1,4-Dihydroxy-2-naphthoic acid can improve the motor dysfunction in parkinson's disease (PD) model through AhR-dependent and -independent pathways. 1,4-Dihydroxy-2-naphthoic acid exerts anti-inflammatory effects by regulating the gut microbiota (such as promoting the proliferation of Bifidobacterium) and directly regulating the host immune system. 1,4-Dihydroxy-2-naphthoic acid induces apoptosis through G0/G1 cell cycle arrest in human keratinocyte to inhibit psoriasis.
    1,4-Dihydroxy-2-naphthoic acid (Standard)
  • HY-116214S1
    Cyprodinil-13C6
    		Activator
    Cyprodinil-13C6 (CGA-219417-13C6) is the 13C6 labeled Cyprodinil (HY-116214). Cyprodinil (CGA-219417) is a broad-spectrum anilinopyrimidine fungicide and an activator of the aryl hydrocarbon receptor. Cyprodinil also has anti-androgenic and androgenic activities. Cyprodinil can inhibit the biosynthesis of methionine in plant-pathogenic fungi and protect fruits and vegetables from a variety of pathogens.
    Cyprodinil-<sup>13</sup>C<sub>6</sub>
  • HY-161649
    hCYP1B1-IN-2
    		Inhibitor
    hCYP1B1-IN-2 (compound 3n) is a potent human cytochrome P450 1B1 enzyme hCYP1B1 inhibitor. hCYP1B1-IN-2 shows the extremely potent anti-hCYP1B1 activity (IC50=0.040 nM) and blocks AhR transcription activity. hCYP1B1-IN-2 potently inhibits hCYP1B1 via a mix inhibition manner, showing a Ki value of 21.71 pM.
    hCYP1B1-IN-2
  • HY-B0311D
    Carbidopa hydrochloride
    		Modulator
    Carbidopa hydrochloride ((S)-(-)-Carbidopa hydrochloride) is a drug used to inhibit Parkinson's disease, which has the activity of inhibiting the peripheral metabolism of levodopa. Carbidopa hydrochloride can increase the proportion of peripheral levodopa penetrating the blood-brain barrier, thereby enhancing its effect on the central nervous system. Carbidopa hydrochloride has also been found to be an aryl hydrocarbon receptor (AhR) ligand with anticancer activity, which can inhibit the growth of pancreatic cancer cells and tumors. The selective AhR regulation properties of carbidopa hydrochloride provide potential prospects for its clinical application.
    Carbidopa hydrochloride
  • HY-B0311AR
    Carbidopa monohydrate (Standard)
    		Modulator
    Carbidopa (monohydrate) (Standard) is the analytical standard of Carbidopa (monohydrate). This product is intended for research and analytical applications. 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.
    Carbidopa monohydrate (Standard)
  • HY-169753
    AHR-IN-1
    		Inhibitor
    AHR-IN-1 (1-103) is an aryl hydrocarbon receptor (AHR) inhibitor with IC50 < 0.5 μM.
    AHR-IN-1
  • HY-124021
    Benzyl 2-naphthyl ether
    Benzyl 2-naphthyl ether is a compound mentioned in the study of the effects of aromatic sensitizers on zebrafish embryos. It can cause morphological abnormalities and changes in gene expression in zebrafish embryos. Its toxicity mechanism is partly related to AHR, and there may be other mechanisms independent of AHR.
    Benzyl 2-naphthyl ether
  • HY-W028393R
    Indole-3-pyruvic acid (Standard)
    		Agonist
    Indole-3-pyruvic acid (Standard) is the analytical standard of Indole-3-pyruvic acid. This product is intended for research and analytical applications. Indole-3-pyruvic acid, a keto analogue of tryptophan, is an orally active AHR agonist. Indole-3-pyruvic acid has antioxidant properties, and can be used in the research of inflammation, anxiety[1][2][3].
    Indole-3-pyruvic acid (Standard)
  • HY-135671
    AhR modulator-1
    		Modulator
    AhR modulator-1 (compound 6-MCDF) is a selective and orally active aryl hydrocarbon receptor (AhR) modulator. AhR modulator-1 inhibits metastasis, in part, by inhibiting prostatic VEGF production prior to tumor formation. AhR modulator-1 also possess anti-estrogenic properties in rat uterus.
    AhR modulator-1
  • HY-W014502R
    D-Kynurenine (Standard)
    		Agonist
    D-Kynurenine (Standard) is the analytical standard of D-Kynurenine. This product is intended for research and analytical applications. D-kynurenine, a metabolite of D-tryptophan, can serve as the bioprecursor of kynurenic acid (KYNA) and 3-hydroxykynurenine. D-Kynurenine is an agonist for G protein-coupled receptor, GPR109B. D-Kynurenine is a substrate in a fluorometric assay of D-amino acid oxidase. D-kynurenine promotes epithelial-to-mesenchymal transition via activating aryl hydrocarbon receptor (AHR).
    D-Kynurenine (Standard)
  • HY-W011338R
    Benzyl butyl phthalate (Standard)
    		Activator
    Benzyl butyl phthalate (Standard) is the analytical standard of Benzyl butyl phthalate. This product is intended for research and analytical applications. Benzyl butyl phthalate, a member of phthalic acid esters (PAEs), can trigger the migration and invasion of hemangioma (HA) cells via upregulation of Zeb1. Benzyl butyl phthalate activates aryl hydrocarbon receptor (AhR) in breast cancer cells to stimulate SPHK1/S1P/S1PR3 signaling and enhances formation of metastasis-initiating breast cancer stem cells (BCSCs).
    Benzyl butyl phthalate (Standard)
  • HY-135830
    AHR antagonist 4
    		Antagonist
    AHR antagonist 4 is a 2-heteroaryl-3-oxo-2,3-dihydropyridazine-4-carboxamide compound and a potent aryl hydrocarbon receptor (AHR) antagonist extracted from patent WO2018146010A1, example 293, has an IC50 of 82.2 nM. AHR antagonist 4 has anti-cancer effects.
    AHR antagonist 4
  • HY-158167
    AhR agonist 5
    		Agonist
    AhR agonist 5 is an AHR agonist (EC50 = 6 nM). From patent WO2024061187A1, compound 5.
    AhR agonist 5
  • HY-N12537A
    (2R,3S)-PD-1/PD-L1-IN-38
    		Antagonist
    (2R,3S)-PD-1/PD-L1-IN-38 (Compound (±)-13e) is an orally active Ah receptor (AhR) antagonist with in vivo and in vitro anticancer activity. (2R,3S)-PD-1/PD-L1-IN-38 promotes the secretion of INF-γ by CD8+T cells and inhibits the signal transduction of PD-1/PD-L1.
    (2R,3S)-PD-1/PD-L1-IN-38
  • HY-B0973S
    Dibenzothiophene-d8
    Dibenzothiophene-d8 is the deuterium labeled Dibenzothiophene (HY-B0973). 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-d<sub>8</sub>
  • HY-B0311CS
    (Rac)-Carbidopa-13C,d3
    (Rac)-Carbidopa-13C,d3 is the 13C- and deuterium labeled DL-Carbidopa.
    (Rac)-Carbidopa-<sup>13</sup>C,d<sub>3</sub>
  • HY-168033
    AhR agonist 8
    		Agonist
    AhR agonist 8 (compound 9) is a potent Aryl Hydrocarbon Receptor (AhR) agonist with an EC50 of 0.154 nM. AhR agonist 8 can be used in the study of psoriasis and atopic dermatitis.
    AhR agonist 8
  • HY-B0311S1
    Carbidopa-d3-1
    		Modulator
    Carbidopa-d3-1 is the deuterium labeled Carbidopa (HY-B0311). 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-d<sub>3</sub>-1
  • HY-139117
    6,2′,4′-Trimethoxyflavone
    		Antagonist
    6,2′,4′-Trimethoxyflavone is an AhR antagonist and has failed to show effective protective effects against cerebral ischemia/reperfusion injury in Sprague-Dawley rats.
    6,2′,4′-Trimethoxyflavone
Cat. No. Product Name / Synonyms Application Reactivity