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-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-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-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-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-B0311CS
    (Rac)-Carbidopa-13C,d3
    (Rac)-Carbidopa-13C,d3 is the 13C- and deuterium labeled DL-Carbidopa[1].
    (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-158168
    AhR agonist 6
    		Agonist
    AhR agonist 6 (Compound 6) is an agonist for aryl hydrocarbon receptor (AhR), with an EC50 of 0.01 nM.
    AhR agonist 6
  • 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-15001A
    Stemregenin 1 hydrochloride
    		Antagonist
    Stemregenin 1 hydrochloride is a purine derivative that antagonizes aryl hydrocarbon receptor signaling in CD34+ cells. IC50 The value is 127 nM. Stemregenin 1 hydrochloride can be used to expand the pluripotency of hematopoietic stem cells (HSC) in stem cell studies.
    Stemregenin 1 hydrochloride
  • HY-155061
    hCYP1B1-IN-1
    		Antagonist
    hCYP1B1-IN-1 (compound B18) is a hCYP1B1 inhibitor (IC50=3.6 nM)，as well as an antagonist of Aryl Hydrocarbon Receptor. hCYP1B1-IN-1 exhibtis suitable metabolic stability and good cell-permeability. hCYP1B1-IN-1 inhibits migration of MCF-7 cells.
    hCYP1B1-IN-1
  • HY-156908
    3-OH-Kynurenamine
    		Activator
    3-OH-Kynurenamine is a lateral metabolite in Tryptophan (HY-N0623) metabolism. 3-OH-Kynurenamine induces a concentration-dependent AhR activation, around 6.5 times higher than L-kynurenine (HY-104026). 3-OH-Kynurenamine confers immunosuppressive properties on dendritic cells (DCs). 3-OH-Kynurenamine can be used for psoriasis research.
    3-OH-Kynurenamine
  • HY-155505
    AHR agonist 4
    		Agonist
    AHR agonist 4 (compound 24e) is an agonist of Aryl hydrocarbon receptor (AHR), assocaited with the immune balance of Th17/22 and Treg cells. AHR agonist 4 serves as a lead compound for anti-psoriasis drug, alleviates imiquimod (IMQ)-induced psoriasis-like skin lesion. AHR agonist 4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    AHR agonist 4
  • HY-158169
    AhR agonist 7
    		Agonist
    AhR agonist 7 (Compound 8) has a good activation activity against AhR (ECsub>50 = 13nM).
    AhR agonist 7
  • HY-N0178R
    Diosmin (Standard)
    		Agonist
    Diosmin (Standard) is the analytical standard of Diosmin. This product is intended for research and analytical applications. Diosmin is a flavonoid found in a variety of citrus fruits and also an agonist of the aryl hydrocarbon receptor (AhR).
    Diosmin (Standard)
  • HY-104026R
    L-Kynurenine (Standard)
    		Agonist
    L-Kynurenine (Standard) is the analytical standard of L-Kynurenine. This product is intended for research and analytical applications. L-Kynurenine is a metabolite of the amino acid L-tryptophan. L-Kynurenine is an aryl hydrocarbon receptor agonist.
    L-Kynurenine (Standard)
  • HY-103222
    DiMNF
    		Modulator 98.01%
    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
Cat. No. Product Name / Synonyms Application Reactivity