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-109044R
    Tapinarof (Standard)
    		Agonist
    Tapinarof (Standard) is the analytical standard of Tapinarof. This product is intended for research and analytical applications. Tapinarof (WBI-1001) is a natural aryl hydrocarbon receptor (AhR) agonist with an EC50 of 13 nM. Tapinarof resolves skin inflammation in mice.
    Tapinarof (Standard)
  • HY-N4095R
    Brevifolincarboxylic acid (Standard)
    		Inhibitor
    Brevifolincarboxylic acid (Standard) is the analytical standard of Brevifolincarboxylic acid (HY-N4095). This product is intended for research and analytical applications. Brevifolincarboxylic acid is a phenolic compound. Brevifolincarboxylic acid can be isolated from Duchesnea chrysantha. Brevifolincarboxylic acid inhibits α-glucosidase with an IC50 value of 323.46 μM. Brevifolincarboxylic acid has an inhibitory effect on the aryl hydrocarbon receptor (AhR). Brevifolincarbacid scavenges ROS. Brevifolincarbacid restores the glucose uptake activity of myotubes. Brevifolincarboxylic acid has antitumor activity against lung and gastric cancer. Brevifolincarbacid can be used in the study of diabetes and inflammatory diseases.
    Brevifolincarboxylic acid (Standard)
  • HY-N0170R
    Indole-3-carbinol (Standard)
    		Agonist
    Indole-3-carbinol (Standard) is the analytical standard of Indole-3-carbinol. This product is intended for research and analytical applications. Indole-3-carbinol (I3C) inhibits NF-κB activity and also is an Aryl hydrocarbon receptor (AhR) agonist, and an inhibitor of WWP1 (WW domain-containing ubiquitin E3 ligase 1).
    Indole-3-carbinol (Standard)
  • HY-124421R
    5F-203 (Standard)
    		Inducer
    5F-203 (Standard) is the analytical standard of 5F-203. This product is intended for research and analytical applications. 5F-203 (NSC-703786) is a cytotoxic molecule that forms DNA adducts and cell cycle arrest. 5F-203 induces aryl hydrocarbon receptor (AhR) signaling and elevates expression of CYP1A1. 5F-203 also increases the levels of reactive oxygen species as well as activates JNK, ERK, and p38.
    5F-203 (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-B0973R
    Dibenzothiophene (Standard)
    Dibenzothiophene (Standard) is the analytical standard of Dibenzothiophene (HY-B0973). This product is intended for research and analytical applications. Dibenzothiophene is an orally active and a noncompetitive CYP1A inhibitor. Dibenzothiophene inhibits CYP1A-mediated EROD activity with 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 (Standard)
  • HY-N1939R
    Icariside I (Standard)
    Icariside I (Standard) is the analytical standard of Icariside I (HY-N1939). This product is intended for research and analytical applications. Icariside I (GH01) is an orally active metabolite of icalin. Icariside I improves estrogen deficiency-induced osteoporosis by simultaneously regulating osteoblast and osteoclast differentiation. Icariside I promotes ATP (HY-B2176) or Nigericin (HY-127019)-induced mtROS production and NLRP3 inflammasome activation and causes idiosyncratic hepatotoxicity. Icariside I does not alter the activation of NLRC4 and AIM2 inflammasomes. Icariside I inhibits breast cancer proliferation, apoptosis, invasion, and metastasis by targeting the IL-6/STAT3 pathway. Icariside I is a kynurenine-AhR pathway inhibitor that alleviates cancer by blocking tumor immune escape.
    Icariside I (Standard)
  • HY-109044S
    Tapinarof-d5
    		Agonist
    Tapinarof-d5 (WBI-1001-d5) is deuterium labeled Tapinarof. Tapinarof (WBI-1001) is a natural aryl hydrocarbon receptor (AhR) agonist with an EC50 of 13 nM. Tapinarof resolves skin inflammation in mice.
    Tapinarof-d<sub>5</sub>
  • HY-15600B
    UPF-648 sodium salt
    UPF-648 sodium salt is an effective inhibitor of kynurenine 3-monooxygenase (KMO), achieving approximately 81% inhibition at a concentration of 1uM, with no inhibitory effect on kynurenine aminotransferase (KAT).
    UPF-648 sodium salt
  • HY-104026BS
    L-Kynurenine-13C10 sulfate
    		Agonist
    L-Kynurenine-13C10 (sulfate) is the 13C labeled L-Kynurenine sulfate. 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-<sup>13</sup>C<sub>10</sub> sulfate
  • 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-15001R
    Stemregenin 1 (Standard)
    		Antagonist
    Stemregenin 1 (Standard) is the analytical standard of Stemregenin 1. This product is intended for research and analytical applications. Stemregenin 1 is a potent aryl hydrocarbon receptor (AhR) antagonist with IC50 of 127 nM.
    Stemregenin 1 (Standard)
  • HY-19317R
    ITE (Standard)
    		Agonist
    ITE (Standard) is the analytical standard of ITE. This product is intended for research and analytical applications. ITE is a potent endogenous agonist of aryl hydrocarbon receptor (AhR), binding directly to AHR, with a Ki of 3 nM. ITE also has immunosuppressive activity.
    ITE (Standard)
  • HY-15484R
    Pifithrin-α hydrobromide (Standard)
    		Agonist
    Pifithrin-α (hydrobromide) (Standard) is the analytical standard of Pifithrin-α (hydrobromide). This product is intended for research and analytical applications. Pifithrin-α hydrobromide is a p53 inhibitor which blocks its transcriptional activity and prevents cells from apoptosis. Pifithrin-α hydrobromide is also an aryl hydrocarbon receptor (AhR) agonist.
    Pifithrin-α hydrobromide (Standard)
  • 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-N8572R
    3',4'-Dimethoxyflavone (Standard)
    		Antagonist
    3',4'-Dimethoxyflavone is a lipophilic flavone, can be isolated from the leaves of Primula veris. 3',4'-Dimethoxyflavone can reduce the synthesis and accumulation of PARP and protect cortical neurones against cell death induced by Parthanatos. 3',4'-Dimethoxyflavone is also an aryl hydrocarbon receptor antagonist in human breast cancer cells. 3',4'-Dimethoxyflavone can promote the proliferation of human hematopoietic stem cells. 3',4'-Dimethoxyflavone has various biological activities, including antioxidant, anti-cancer, anti-inflammatory, anti-atherogenic, hypolipidaemic, and neuroprotective or neurotrophic effects.
    3',4'-Dimethoxyflavone (Standard)
  • HY-N4069
    Lupinalbin A
    		Agonist
    Lupinalbin A (Boeravinone L) is a dipeptidyl peptidase 4 (DPP4) and α-glucosidase inhibitor with IC50 values ​​of 45.2 and 53.4 µM, respectively. Lupinalbin A exhibits antidiabetic activity.
    Lupinalbin A
  • HY-170514
    1,2,3,7,8,9-Hexachlorodibenzofuran
    		Ligand
    1,2,3,7,8,9-Hexachlorodibenzofuran is a polychlorinated dibenzofuran homologue. 1,2,3,7,8,9-Hexachlorodibenzofuran can interact with AhR. 1,2,3,7,8, 9-hexachlorodibenzofuran is highly toxic, teratogenic, carcinogenic and mutagenic.
    1,2,3,7,8,9-Hexachlorodibenzofuran
  • 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-D0932S
    Sudan IV-d6
    		Agonist
    Sudan IV-d6 (Solvent Red 24-d6) is the deuterium labeled Sudan IV(HY-D0932). 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-</sub>d<sub>6</sub>
Cat. No. Product Name / Synonyms Application Reactivity