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-100242
    Mivotilate
    		Activator 99.58%
    Mivotilate is a nontoxic, potent activator of the aryl hydrocarbon receptor (AhR), and acts as a hepatoprotective agent.
    Mivotilate
  • HY-N10123
    Indolokine A5
    		Agonist ≥98.0%
    Indolokine A5, a catabolite of L-cysteine, is a potent AhR agonist.
    Indolokine A5
  • HY-B0311A
    Carbidopa monohydrate
    		Modulator ≥98.0%
    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
  • HY-W014075S
    1-Hydroxypyrene-d9
    		Agonist 99.95%
    1-Hydroxypyrene-d9 is the deuterium labeled 1-Hydroxypyrene (HY-W014075). 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-d<sub>9</sub>
  • HY-W007355R
    Skatole (Standard)
    		Activator
    Skatole (Standard) is the analytical standard of Skatole. This product is intended for research and analytical applications. Skatole (3-methylindole) is a heterocyclic compound naturally found in the feces of vertebrates and can be found in certain plants. Skatole can be produced by intestinal bacteria, inducing apoptosis of intestinal epithelial cells through activating aryl hydrocarbon receptors (AhR) and p38. Skatole has been used in specific products of the perfume industry or as a flavor additive in ice cream.
    Skatole (Standard)
  • HY-W764758
    3-OH-Kynurenamine dihydroiodide
    		Activator 99.56%
    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-136220
    AHR antagonist 5
    		Antagonist 98.05%
    AHR antagonist 5, a potent and orally active aryl hydrocarbon receptor (AHR) antagonist extracted from patent WO2018195397, example 39, has an IC50 of < 0.5 μΜ. AHR antagonist 5 significantly inhibits tumor growth combined with checkpoint inhibitor anti-PD-1.
    AHR antagonist 5
  • HY-118780
    CHD-5
    		Antagonist ≥98.0%
    CHD-5 is a potent AhR (aryl hydrocarbon receptor) antagonist.
    CHD-5
  • HY-116214R
    Cyprodinil (Standard)
    		Activator
    Cyprodinil (Standard) (CGA-219417 (Standard)) is the analytical standard of Cyprodinil (HY-116214). This product is intended for research and analytical applications. 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 (Standard)
  • HY-104026CS
    L-Kynurenine-13C10 sulfate hemihydrate
    		Agonist 99.90%
    L-Kynurenine-13C10 (sulfate hemihydrate) is the 13C labeled L-Kynurenine sulfate. L-Kynurenine sulfate hemihydrate, 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 hemihydrate
  • HY-118474
    GW 610
    		Activator 99.78%
    GW 610 (NSC 721648), an antitumor agent, is a potent AhR ligand with a Ki of 6.8 nM. GW 610 induces CYP1A1 expression in MCF-7 cells. GW 610 shows potent and selective anticancer activity against lung, colon, and breast cancer cell lines.
    GW 610
  • HY-103222
    DiMNF
    		Modulator 98.46%
    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
  • 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-W046846
    Corannulene
    		Agonist
    Corannulene is an agonist of aryl hydrocarbon receptor (AhR). Corannulene causes less cytotoxic responses than Benzo[a]pyrene (HY-107377) in hepatoma cells. Corannulene is promising for research of cancers.
    Corannulene
  • 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-154825
    20-Hydroxyvitamin D3
    		≥98.0%
    20-Hydroxyvitamin D3 (20(OH)D3) is a hydroxy metabolite of vitamin D3. 20-Hydroxyvitamin D3 functions as a ligand for vitamin D receptor (VDR), aryl hydrocarbon receptor (AhR), liver X receptor (LXR), and retinoic acid-related orphan receptor (ROR). 20-Hydroxyvitamin D3 inhibits cell proliferation, induces differentiation. 20-Hydroxyvitamin D3 can be used for inflammatory and autoimmune diseases study.
    20-Hydroxyvitamin D3
  • HY-N8445
    Glucoerucin potassium
    		99.73%
    Glucoerucin potassium is an aryl hydrocarbon receptor antagonist and is the 4-methylthio-butyl glucosinolate found in the seeds of Eruca sativa Mill.
    Glucoerucin potassium
  • HY-N10295
    Flavipin
    		Agonist
    Flavipin is an aryl hydrocarbon receptor (Ahr) agonist that induces the expression of Ahr downstream genes in mouse CD4+ T cells and CD11b+ macrophages. Flavipin inhibits the stabilizing function of Arid5a on Il23a 3′UTR, a newly identified target mRNA. Flavipin exhibits the DPPH free radical scavenging ability with IC50 value of 7.2 μM, and has potent α-glucosidase inhibition with IC50 value of 33.8 μM.
    Flavipin
  • HY-B0973
    Dibenzothiophene
    		99.88%
    Dibenzothiophene is an orally active and a noncompetitive CYP1A inhibitor. Dibenzothiophene inhibits CYP1A-mediated EROD activity with a 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
  • HY-136220A
    AHR antagonist 5 hemimaleate
    		Antagonist
    AHR antagonist 5 hemimaleate, a potent and orally active aryl hydrocarbon receptor (AHR) antagonist, has an IC50 of < 0.5 µΜ. AHR antagonist 5 hemimaleate significantly inhibits tumor growth combined with checkpoint inhibitor anti-PD-1 (WO2018195397, example 39).
    AHR antagonist 5 hemimaleate
Cat. No. Product Name / Synonyms Application Reactivity