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-12028
    PD98059
    		Antagonist 99.96%
    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
  • HY-12684
    CH-223191
    		Antagonist 99.96%
    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.
    CH-223191
  • HY-104026
    L-Kynurenine
    		Agonist 99.93%
    L-Kynurenine is a metabolite of the amino acid L-tryptophan. L-Kynurenine is an aryl hydrocarbon receptor agonist.
    L-Kynurenine
  • HY-15484
    Pifithrin-α hydrobromide
    		Agonist 98.05%
    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
  • HY-12451
    FICZ
    		Agonist 99.42%
    FICZ is a potent aryl hydrocarbon receptor (AhR) agonist with a Kd of 70 pM.
    FICZ
  • HY-N6264R
    26-Deoxyactein (Standard)
    		Inhibitor
    26-Deoxyactein (Standard) is the analytical standard of 26-Deoxyactein. This product is intended for research and analytical applications. 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 (Standard)
  • HY-N4095R
    Brevifolincarboxylic acid (Standard)
    		Inhibitor
    Brevifolincarboxylic acid (Standard) is the analytical standard of Brevifolincarboxylic acid. This product is intended for research and analytical applications. Brevifolincarboxylic acid is extracted from Polygonum capitatum, has inhibitory effect on the aryl hydrocarbon receptor (AhR). Brevifolincarboxylic acid is an α-glucosidase inhibitor with an IC50 of 323.46 μM.
    Brevifolincarboxylic acid (Standard)
  • HY-B0311D
    Carbidopa hydrochloride
    		Modulator
    Carbidopa hydrochloride ((S)-(-)-Carbidopa hydrochloride) is a drug used to inhibit Parkinson's disease, which has the activity of inhibiting the peripheral metabolism of levodopa. Carbidopa hydrochloride can increase the proportion of peripheral levodopa penetrating the blood-brain barrier, thereby enhancing its effect on the central nervous system. Carbidopa hydrochloride has also been found to be an aryl hydrocarbon receptor (AhR) ligand with anticancer activity, which can inhibit the growth of pancreatic cancer cells and tumors. The selective AhR regulation properties of carbidopa hydrochloride provide potential prospects for its clinical application.
    Carbidopa hydrochloride
  • HY-15001
    Stemregenin 1
    		Antagonist 99.95%
    Stemregenin 1 is a potent aryl hydrocarbon receptor (AhR) antagonist with IC50 of 127 nM.
    Stemregenin 1
  • HY-109044
    Tapinarof
    		Agonist 99.95%
    Tapinarof (WBI-1001) is a natural aryl hydrocarbon receptor (AhR) agonist with an EC50 of 13 nM. Tapinarof resolves skin inflammation in mice.
    Tapinarof
  • HY-W028393
    Indole-3-pyruvic acid
    		Agonist 99.79%
    Indole-3-pyruvic acid, a keto analogue of tryptophan, is an orally active AHR agonist. Indole-3-pyruvic acid has antioxidant properties, and can be used in the research of inflammation, anxiety.
    Indole-3-pyruvic acid
  • 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.
    ITE
  • HY-N0170
    Indole-3-carbinol
    		Agonist 98.87%
    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
  • 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.
    BAY 2416964
  • HY-N0178
    Diosmin
    		Agonist 99.51%
    Diosmin is a flavonoid found in a variety of citrus fruits and also an agonist of the aryl hydrocarbon receptor (AhR).
    Diosmin
  • 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.
    Carbidopa
  • HY-W007355
    Skatole
    		Activator 99.97%
    Skatole (3-methylindole) is a heterocyclic compound naturally found in the feces of vertebrates and can be found in certain plants. Skatole can be produced by intestinal bacteria, inducing apoptosis of intestinal epithelial cells through activating aryl hydrocarbon receptors (AhR) and p38. Skatole has been used in specific products of the perfume industry or as a flavor additive in ice cream.
    Skatole
  • 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.
    GNF351
  • HY-125833
    Alpha-Naphthoflavone
    		Antagonist 98.54%
    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
  • HY-111449
    BAY-218
    		Antagonist 99.95%
    BAY-218 (AHR antagonist 1) is an aryl hydrocarbon receptor (AHR) antagonist. BAY-218 has AHR inhibitory activity with an IC50 of 39.9 nM in in U87 glioblastoma cells. BAY-218 can be used for the research of cancer or conditions with dysregulated immune responses.
    BAY-218
Cat. No. Product Name / Synonyms Application Reactivity