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-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-23499R
    Indeno[1,2,3-cd]pyrene (Standard)
    		Activator
    Indeno[1,2,3-cd]pyrene (Standard) is the analytical standard of Indeno[1,2,3-cd]pyrene. This product is intended for research and analytical applications. Indeno[1,2,3-cd]pyrene is a polycyclic aromatic hydrocarbon with moderate cytotoxicity in human pulmonary alveolar epithelial cells HPAEpiC. Indeno[1,2,3-cd]pyrene enhances allergic lung infammation via aryl hydrocarbon receptor.
    Indeno[1,2,3-cd]pyrene (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-116214S
    Cyprodinil-d5
    		Activator
    Cyprodinil-d5(CGA-219417-d5) is the deuterium 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-d<sub>5</sub>
  • 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-136930
    6-Iododiosmin
    		Control
    6-Iododiosmin is a impurity of Diosmin (HY-N0178) raw materials.
    6-Iododiosmin
  • HY-104026B
    L-Kynurenine sulfate
    		Agonist
    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 sulfate
  • 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.
    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-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-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-B0311R
    Carbidopa (Standard)
    		Modulator
    Carbidopa (Standard) is the analytical standard of Carbidopa. This product is intended for research and analytical applications. Carbidopa ((S)-(-)-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 (Standard)
  • 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
Cat. No. Product Name / Synonyms Application Reactivity