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

Aryl Hydrocarbon Receptor

Aryl Hydrocarbon Receptor (AhR or AHR or ahr or ahR) is a protein that in humans is encoded by the AHR gene. The aryl hydrocarbon receptor is a ligand-activated transcription factor involved in the regulation of biological responses to planar aromatic (aryl) hydrocarbons, and regulates xenobiotic-metabolizing enzymes such as cytochrome P450s, most notably cyp 1A1.

Aryl Hydrocarbon Receptor is a member of the family of basic helix-loop-helix transcription factors. AhR binds several exogenous ligands including natural plant flavonoids, polyphenolics and indoles, as well as synthetic polycyclic aromatic hydrocarbons and dioxin-like compounds. AhR is a cytosolic transcription factor that is normally inactive, binding to several co-chaperones. Upon ligand binding to chemicals such as 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD), the chaperones dissociate resulting in AhR translocating into the nucleus and dimerizing with ARNT (AhR nuclear translocator), leading to changes in gene transcription.

Aryl Hydrocarbon Receptor Related Products (25):

Cat. No. Product Name Effect Purity
  • HY-12028
    PD98059 Antagonist 99.84%
    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 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 98.16%
    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-15001
    StemRegenin 1 Antagonist 99.50%
    StemRegenin 1 is a potent aryl hydrocarbon receptor (AhR) antagonist with IC50 of 127 nM.
  • HY-12451
    FICZ Agonist 99.42%
    FICZ is a potent aryl hydrocarbon receptor (AhR) agonist with a Kd of 70 pM.
  • HY-117102
    ANI-7 Activator 99.25%
    ANI-7 is an activator of aryl hydrocarbon receptor (AhR) pathway. ANI-7 inhibits the growth of multiple cancer cells, and potently and selectively inhibits the growth of MCF-7 breast cancer cells with a GI50 of 0.56 μM. ANI-7 induces CYP1-metabolizing mono-oxygenases by activating AhR pathway, and also induces DNA damage, checkpoint Kinase 2 (Chk2) activation, S-phase cell cycle arrest, and cell death in sensitive breast cancer cell lines.
  • HY-135829
    AHR antagonist 3 Antagonist
    AHR antagonist 3 is a 2-heteroaryl-3-oxo-2,3-dihydropyridazine-4-carboxamide compound and an aryl hydrocarbon receptor (AHR) antagonist extracted from patent WO2018146010A1, example 192, has an IC50 of 341 nM. AHR antagonist 3 has anti-cancer effects.
  • HY-135831
    AHR antagonist 2 Antagonist
    AHR antagonist 2 is a potent aryl hydrocarbon receptor (AHR) antagonist, extracted from patent WO2019101641A1, compound example 1, with IC50s of 0.885 and 2.03 nM for human and mouse AhR.
  • HY-104026
    L-Kynurenine Agonist 99.40%
    L-Kynurenine is a metabolite of the amino acid L-tryptophan. L-Kynurenine is an aryl hydrocarbon receptor agonist.
  • HY-19317
    ITE Agonist 99.27%
    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-109044
    Tapinarof Agonist 99.74%
    Tapinarof (Benvitimod; WBI 1001; GSK2894512) is a natural aryl hydrocarbon receptor (AhR) agonist with an EC50 of 13 nM.
  • 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-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-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 98.88%
    PDM2 is a selective, high-affinity aryl hydrocarbon receptor (AhR) antagonist with an Ki of 1.2±0.4 nM.
  • 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-112627
    CAY 10465 Agonist 98.48%
    CAY 10465 is a selective and high-affinity AhR agonist, with a Ki of 0.2 nM, and shows no effect on estrogen receptor (Ki >100000 nM).
  • 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-100242
    Mivotilate Activator >98.0%
    Mivotilate is a nontoxic, potent activator of the aryl hydrocarbon receptor (AhR), and acts as a hepatoprotective agent.
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