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-175554
    CYP1B1-IN-10
    		Inhibitor
    CYP1B1-IN-10 (Compound 15C) is a highly selective human cytochrome P450 1B1 (hCYP1B1) inhibitor (IC50=0.11 μM). CYP1B1-IN-10 is promising for research of hormone-dependent tumors (e.g., breast and ovarian cancers).
    CYP1B1-IN-10
  • HY-G0007S
    Omeprazole sulfone-d3
    		Control
    Omeprazole sulfone-d3 is the deuterium labeled Omeprazole sulfone. Omeprazole sulfone (Omeprazole sulphone) is one of the major circulating metabolites of Omeprazole (HY-B0113) in vivo, and belongs to class 4 non-mutagenic impurities. Omeprazole sulfone does not bind to the aryl hydrocarbon receptor (AhR), nor does it induce the expression of CYP1A1 or CYP1A2. However, Omeprazole sulfone promotes the migration of gastric epithelial cells under basal conditions and reverses the inhibitory effect of Indomethacin (HY-14397) on cell migration. Omeprazole sulfone does not promote cell proliferation, nor does it upregulate COX-2 expression or activate signaling pathways such as ERK, P38 MAPK and PI3K. Omeprazole sulfone maintains basal ulcer healing under non-acid-dependent conditions and can be used in studies related to gastric ulcer repair.
    Omeprazole sulfone-d<sub>3</sub>
  • 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
  • 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-16031A
    AFP464
    		Agonist
    AFP464 (NSC710464) is a prodrug of Aminoflavone (HY-132974) and an agonist of the aryl hydrocarbon receptor (AhR). AFP464 downregulates the expression of α6-integrin (α6-integrin), inhibits breast tumor growth, reduces the population of tumor-initiating cells, disrupts mammosphere structure, induces the formation of mucin lake clusters, triggers DNA damage, and exerts antiproliferative activity. AFP464 is rapidly converted to Aminoflavone by nonspecific esterases in plasma and cell culture media. AFP464 is applicable to research related to breast cancer.
    AFP464
  • 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-182495
    Penisimplicissin
    		Inhibitor
    Penisimplicissin is a funicone-like compound and antiviral agent. Penisimplicissin reduces the expression of AhR and viral nucleocapsid protein. Penisimplicissin improves the cell viability and morphological characteristics of CCoV-infected cells. Penisimplicissin inhibits CCoV infection. Penisimplicissin can be used in studies related to canine coronavirus infection.
    Penisimplicissin
  • 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 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
  • 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-G0007S1
    Omeprazole sulfone-13C,d3
    		Control
    Omeprazole sulfone-13C,d3 is the deuterium and 13C labeled Omeprazole sulfone. Omeprazole sulfone (Omeprazole sulphone) is one of the major circulating metabolites of Omeprazole (HY-B0113) in vivo, and belongs to class 4 non-mutagenic impurities. Omeprazole sulfone does not bind to the aryl hydrocarbon receptor (AhR), nor does it induce the expression of CYP1A1 or CYP1A2. However, Omeprazole sulfone promotes the migration of gastric epithelial cells under basal conditions and reverses the inhibitory effect of Indomethacin (HY-14397) on cell migration. Omeprazole sulfone does not promote cell proliferation, nor does it upregulate COX-2 expression or activate signaling pathways such as ERK, P38 MAPK and PI3K. Omeprazole sulfone maintains basal ulcer healing under non-acid-dependent conditions and can be used in studies related to gastric ulcer repair.
    Omeprazole sulfone-<sup>13</sup>C,d<sub>3</sub>
  • 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-104026S1
    L-Kynurenine-d4-1
    		Agonist 99.24%
    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-132974
    Aminoflavone
    		Activator
    Aminoflavone is an anti-tumor agent. Aminoflavone inhibits the expression of ITGA6/SOX2 by activating the AhR-miR-125b-2-3p axis, thereby targeting breast cancer stem cells. Aminoflavone induces an increase in intracellular ROS, increases the level of oxidative DNA damage marker 8-oxodG and DNA-protein cross-links. Aminoflavone causes S-phase arrest, activates caspase-3/8/9 and induces apoptosis (apoptosis). Aminoflavone inhibits HIF-1α expression in a manner independent of AhR. Aminoflavone can be used for the study of breast cancer.
    Aminoflavone
  • HY-G0007R
    Omeprazole sulfone (Standard)
    		Control
    Omeprazole sulfone (Standard) is the analytical standard of Omeprazole sulfone. This product is intended for research and analytical applications. Omeprazole sulfone (Omeprazole sulphone) is one of the major circulating metabolites of Omeprazole (HY-B0113) in vivo, and belongs to class 4 non-mutagenic impurities. Omeprazole sulfone does not bind to the aryl hydrocarbon receptor (AhR), nor does it induce the expression of CYP1A1 or CYP1A2. However, Omeprazole sulfone promotes the migration of gastric epithelial cells under basal conditions and reverses the inhibitory effect of Indomethacin (HY-14397) on cell migration. Omeprazole sulfone does not promote cell proliferation, nor does it upregulate COX-2 expression or activate signaling pathways such as ERK, P38 MAPK and PI3K. Omeprazole sulfone maintains basal ulcer healing under non-acid-dependent conditions and can be used in studies related to gastric ulcer repair.
    Omeprazole sulfone (Standard)
Cat. No. Product Name / Synonyms Application Reactivity