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-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-111441
    1,4-Chrysenequinone
    		Activator 98.42%
    1,4-Chrysenequinone, a polycyclic aromatic quinone, acts as an activator of aryl hydrocarbon receptor (AhR).
    1,4-Chrysenequinone
  • 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-111450
    CB7993113
    		Antagonist ≥98.0%
    CB7993113 is a potent AHR antagonist, with an IC50 of 0.33 μM. CB7993113 directly binds AHR protein and blocks AHR nuclear translocation. CB7993113 inhibits polycyclic aromatic hydrocarbon (PAH)- and TCDD-induced reporter activity by 75% and 90% respectively.
    CB7993113
  • 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-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-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-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
    		99.47%
    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
  • 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-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-W011338S
    Benzyl butyl phthalate-d4
    Benzyl butyl phthalate-d4 is the deuterium labeled Benzyl butyl phthalate[1]. 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)[2][3][4].
    Benzyl butyl phthalate-d<sub>4</sub>
  • 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
Cat. No. Product Name / Synonyms Application Reactivity