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-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-N6264
    26-Deoxyactein
    		Inhibitor 99.76%
    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
  • 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-16031
    AFP464 free base
    		Agonist
    AFP464 (NSC710464) free base is a prodrug of Aminoflavone (HY-132974) and an agonist of the aryl hydrocarbon receptor (AhR). AFP464 free base 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 free base is rapidly converted to Aminoflavone by nonspecific esterases in plasma and cell culture media. AFP464 free base is applicable to research related to breast cancer.
    AFP464 free base
  • 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-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-16031B
    AFP464 dihydrochloride
    		Agonist 99.67%
    AFP464 (NSC710464) dihydrochloride is a prodrug of Aminoflavone (HY-132974) and an agonist of the aryl hydrocarbon receptor (AhR). AFP464 dihydrochloride 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 dihydrochloride is rapidly converted to Aminoflavone by nonspecific esterases in plasma and cell culture media. AFP464 dihydrochloride is applicable to research related to breast cancer.
    AFP464 dihydrochloride
  • 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-23499
    Indeno[1,2,3-cd]pyrene
    		Activator 99.66%
    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
  • 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-W095381
    N-Methylscatole
    		Agonist 98.45%
    N-Methylscatole (compound 70130) is a weak aryl hydrocarbon receptor (AhR) agonist exhibiting no significant antagonistic activity.
    N-Methylscatole
  • 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-12028R
    PD98059 (Standard)
    		Antagonist
    PD98059 (Standard) is the analytical standard of PD98059. This product is intended for research and analytical applications. PD98059 is a potent and selective MEK inhibitor with an IC50 of 5 µM. PD98059 binds to the inactive form of MEK, thereby preventing the activation of MEK1 (IC50 of 2-7 µM) and MEK2 (IC50 of 50 µM) by upstream kinases. PD98059 is a ERK1/2 signaling inhibitor. PD98059 is a ligand for the aryl hydrocarbon receptor (AHR), and suppresses TCDD binding (IC50 of 4 μM) and AHR transformation (IC50 of 1 μM). PD98059 also inhibits Mycobacterium bovis Bacillus CalmetteGuerin (BCG)-induced autophagy.
    PD98059 (Standard)
  • HY-125833R
    Alpha-Naphthoflavone (Standard)
    		Antagonist
    Alpha-Naphthoflavone (Standard) is the analytical standard of Alpha-Naphthoflavone. This product is intended for research and analytical applications. Alpha-Naphthoflavone is an orally active flavonoid that is a potent, competitive inhibitor of aromatase< b>aromatase. < b > IC < sub > 50 < / sub > < / b > and < b > K < sub > I < / sub > < / b > value were 0.5 and 0.2 microns. Alpha-Naphthoflavone can inhibit cell proliferation and induce apoptosis.
    Alpha-Naphthoflavone (Standard)
  • HY-154825
    20-Hydroxyvitamin D3
    		≥98.0%
    20-Hydroxyvitamin D3 (20(OH)D3), a product of vitamin D3 hydroxylation, is a noncalcemic immunomodulator. 20-Hydroxyvitamin D3 binds to vitamin D receptor (VDR), activates VDR and aryl hydrocarbon receptor (AhR) signaling, stimulates CYP24A1 expression, and drives VDR nuclear translocation. 20-Hydroxyvitamin D3 inhibits NF-κB activity via IκBα upregulation. 20-Hydroxyvitamin D3 acts as a substrate for CYP27B1 and rat CYP24A1, undergoing hydroxylation to form dihydroxy-derivatives. 20-Hydroxyvitamin D3 inhibits cell proliferation, colony formation, migration, and tumor growth, and induces cell differentiation in cancer cells. 20-Hydroxyvitamin D3 can be used for the research of inflammatory and autoimmune diseases, melanoma, breast carcinomas, and hepatocarcinoma.
    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-133677S
    Mono(2-ethyl-5-hydroxyhexyl) phthalate-d4
    		Activator
    Mono(2-ethyl-5-hydroxyhexyl) phthalate-d4 (MEHHP-d4) is a deuterium labeled Mono(2-ethyl-5-hydroxyhexyl) phthalate (HY-133677). Mono (2-ethyl-5-hydroxyhexyl) phthalate is a biomarker for human exposure to DEHP (HY-B1945). By activating the tryptophan-kynurenine-aryl hydrocarbon receptor (AhR) pathway, mono (2-ethyl-5-hydroxyhexyl) phthalate significantly increases the viability of primary uterine leiomyoma cells and reduces cell apoptosis. Mono (2-ethyl-5-hydroxyhexyl) phthalate correlates with decreased sperm DNA damage. Mono (2-ethyl-5-hydroxyhexyl) phthalate can be used in studies related to uterine leiomyoma.
    Mono(2-ethyl-5-hydroxyhexyl) phthalate-d<sub>4</sub>
Cat. No. Product Name / Synonyms Application Reactivity