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-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-103221R
    MeBIO (Standard)
    		Agonist
    MeBIO (Standard) is the analytical standard of MeBIO (HY-103221). This product is intended for research and analytical applications. MeBIO is a potent AhR (aryl hydrocarbon receptor) agonist, with IC50 of 44 μM (GSK-3) and 55 μM (CDK1/cyclin B), respectively.
    MeBIO (Standard)
  • HY-103220R
    6,2',4'-Trimethoxyflavone (Standard)
    		Antagonist
    6,2',4'-Trimethoxyflavone (Standard) is the analytical standard of 6,2',4'-Trimethoxyflavone (HY-103220). This product is intended for research and analytical applications. 6,2',4'-Trimethoxyflavone is a potent aryl hydrocarbon receptor (AHR) antagonist. 6,2',4'-Trimethoxyflavone represses AHR-mediated gene induction.
    6,2',4'-Trimethoxyflavone (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-W714200
    Neburon
    		Activator
    Neburon is a phenylurea herbicide whose main mechanism of action is to inhibit photosynthetic electron transport, thereby disrupting algal growth. Neburon activates the Ahr and Notch1 signaling pathways, and induces oxidative stress and apoptosis. Long-term exposure causes significant male reproductive toxicity and cardiotoxicity in zebrafish.
    Neburon
  • 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-148637
    Picoberin
    		Agonist
    Picoberin is a low picomolar inhibitor of Hedgehog-induced osteoblast differentiation. Picoberin is a potent aryl hydrocarbon receptor (AhR) agonist. Picoberin inhibits Wnt3A-induced osteoblast differentiation of C3H10T1/2 cells. Picoberin can upregulate genes encoding phase I and II metabolic enzymes.
    Picoberin
  • 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-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>
  • HY-N16435
    Plumericin
    		Inhibitor
    Plumericin is an anti-inflammatory, antioxidant, and antibacterial agent. Plumericin reduces Apoptosis, promotes Nrf-2 and inhibits NF-κB and AhR activation, blocks STAT3 signaling. Plumericin inhibits Mycobacterium tuberculosis growth. Plumericin can be used for the research of chronic kidney disease, vascular diseases, inflammatory bowel diseases, peritonitis, and tuberculosis.
    Plumericin
  • HY-129247
    Versicolorin A
    		Activator
    Versicolorin A is a biosynthetic precursor of Aflatoxin B1 (HY-N6615). Versicolorin A induces phosphorylation of p53. Versicolorin A activates the aryl hydrocarbon receptor AhR and significantly induces the expression of CYP1A1. Versicolorin A exerts genotoxic and cytotoxic effects. Versicolorin A enhances the genotoxicity of aflatoxin B1 in cells by promoting CYP450-mediated bioactivation of aflatoxin B1. Versicolorin A can be used in research related to colorectal cancer and hepatocellular carcinoma.
    Versicolorin A
  • HY-128229
    AHR antagonist 6
    		Antagonist
    AHR antagonist 6 (Compound 44) is an aryl hydrocarbon receptor (AHR) antagonist used in cancer research.
    AHR antagonist 6
  • HY-N9924
    Glucoerucin
    Glucoerucin is an aryl hydrocarbon receptor antagonist and is the 4-methylthio-butyl glucosinolate found in the seeds of Eruca sativa Mill.
    Glucoerucin
  • HY-W007355S2
    Skatole-13C6
    Skatole-13C6 is the 13C-labeled Skatole (HY-W007355). 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-13C<sub>6</sub>
Cat. No. Product Name / Synonyms Application Reactivity