1. Signaling Pathways
  2. Immunology/Inflammation
  3. Aryl Hydrocarbon Receptor

Aryl Hydrocarbon Receptor

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.

Aryl Hydrocarbon Receptor Related Products (32):

Cat. No. Product Name Effect Purity
  • HY-12028
    PD98059 Antagonist 99.94%
    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 autophagy.
  • HY-15484
    Pifithrin-α hydrobromide Agonist
    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.
  • HY-12684
    CH-223191 Antagonist 99.60%
    CH-223191 is a potent and specific antagonist of aryl hydrocarbon receptor (AhR). CH-223191 inhibits TCDD-mediated nuclear translocation and DNA binding of AhR, and inhibits TCDD-induced luciferase activity with an IC50 of 0.03 μM.
  • HY-12451
    FICZ Agonist
    FICZ is a potent aryl hydrocarbon receptor (AhR) agonist with a Kd of 70 pM.
  • HY-104026
    L-Kynurenine Agonist 99.85%
    L-Kynurenine is a metabolite of the amino acid L-tryptophan. L-Kynurenine is an aryl hydrocarbon receptor agonist.
  • 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.
  • HY-15001
    StemRegenin 1 Antagonist
    StemRegenin 1 is a potent aryl hydrocarbon receptor (AhR) antagonist with IC50 of 127 nM.
  • HY-109044
    Tapinarof Agonist 99.74%
    Tapinarof (WBI-1001) is a natural aryl hydrocarbon receptor (AhR) agonist with an EC50 of 13 nM. Tapinarof resolves skin inflammation in mice.
  • HY-19317
    ITE Agonist ≥98.0%
    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.
  • HY-102023
    GNF351 Antagonist 99.90%
    GNF351 is a full aryl hydrocarbon receptor (AHR) antagonist. GNF351 competes with a photoaffinity AHR ligand for binding to the AHR with an IC50 of 62 nM. GNF351 is minimal toxicity in mouse or human keratinocytes.
  • HY-N0170
    Indole-3-carbinol Agonist ≥98.0%
    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).
  • HY-N0178
    Diosmin Agonist ≥98.0%
    Diosmin is a flavonoid found in a variety of citrus fruits and also an agonist of the aryl hydrocarbon receptor (AhR).
  • HY-112629
    PDM2 Antagonist 98.85%
    PDM2 is a selective, high-affinity aryl hydrocarbon receptor (AhR) antagonist with an Ki of 1.2±0.4 nM.
  • HY-B0311
    Carbidopa Modulator ≥98.0%
    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.
  • HY-111449
    AHR antagonist 1 Antagonist 99.07%
    AHR antagonist 1 is an aryl hydrocarbon receptor (AHR) antagonist extracted from patent WO2017202816A1, example 23, has an IC50 of 39.9 nM in human cell line.
  • HY-W007355
    Skatole Activator ≥98.0%
    Skatole is produced by intestinal bacteria, regulates intestinal epithelial cellular functions through activating aryl hydrocarbon receptors and p38.
  • HY-18619
    YL-109 Modulator 98.74%
    YL-109 is an antitumor agent that can induce carboxyl terminus of Hsp70-interacting protein (CHIP) expression through aryl hydrocarbon receptor (AhR) signaling. YL-109 has ability to inhibit breast cancer cell growth and invasiveness.
  • HY-N0279
    Cardamonin Activator 98.54%
    Cardamonin (Cardamomin), a natural flavone isolated from Alpinia katsumadai Hayata, acts as an aryl hydrocarbon receptor (AhR) activator. Cardamonin alleviates inflammatory bowel disease by the inhibition of NLRP3 inflammasome activation via an AhR/Nrf2/NQO1 pathway.
  • HY-135829
    BAY 2416964 Antagonist 99.59%
    BAY 2416964 is a potent and orally active aryl hydrocarbon receptor (AHR) antagonist extracted from patent WO2018146010A1, example 192, has an IC50 of 341 nM. BAY 2416964 has the potential for solid tumors treatment.
  • HY-135750
    VAF347 Agonist 99.85%
    VAF347 is a cell permeable and highly affinity aryl hydrocarbon receptor (AhR) agonist and induces AhR signaling. VAF347 inhibits the development of CD14+CD11b+ monocytes from granulo-monocytic (GM stage) precursors. VAF347 has anti-inflammatory effects.
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