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

Aryl Hydrocarbon Receptor

AhR

Aryl Hydrocarbon Receptor

Related Products

PDF 0.68 MB

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-114740
    β-Naphthoflavone
    		Agonist 99.95%
    β-Naphthoflavone is an exogenous aryl hydrocarbon receptor (AHR) ligand. β-Naphthoflavone can activate AHR to participate in various biological processes, including cell growth, differentiation, apoptosis, and metabolism. β-Naphthoflavone has antioxidant activity and can exert its antioxidant function by regulating the activity of antioxidant enzymes. β-Naphthoflavone is also a non-carcinogenic CYP1A inducer and can be used to treat aristolochic acid (AAI) induced renal injury.
    β-Naphthoflavone
  • HY-135750
    VAF347
    		Agonist 99.90%
    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.
    VAF347
  • HY-112629
    PDM2
    		Antagonist 98.76%
    PDM2 is a selective, high-affinity aryl hydrocarbon receptor (AhR) antagonist with an Ki of 1.2±0.4 nM.
    PDM2
  • HY-134217
    KYN-101
    		Inhibitor 98.17%
    KYN-101 is a potent, selective and orally active AHR inhibitor. KYN-101 decreases the CYP1A1 mRNA expression. KYN-101 shows anti-cancer activity.
    KYN-101
  • HY-103220
    6,2',4'-Trimethoxyflavone
    		Antagonist 98.09%
    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
  • HY-W014502
    D-Kynurenine
    		Agonist 99.67%
    D-kynurenine, a metabolite of D-tryptophan, can serve as the bioprecursor of kynurenic acid (KYNA) and 3-hydroxykynurenine. D-Kynurenine is an agonist for G protein-coupled receptor, GPR109B. D-Kynurenine is a substrate in a fluorometric assay of D-amino acid oxidase. D-kynurenine promotes epithelial-to-mesenchymal transition via activating aryl hydrocarbon receptor (AHR).
    D-Kynurenine
  • HY-W011338
    Benzyl butyl phthalate
    		Activator
    Benzyl butyl phthalate, a member of phthalic acid esters (PAEs), can trigger the migration and invasion of hemangioma (HA) cells via upregulation of Zeb1. Benzyl butyl phthalate activates aryl hydrocarbon receptor (AhR) in breast cancer cells to stimulate SPHK1/S1P/S1PR3 signaling and enhances formation of metastasis-initiating breast cancer stem cells (BCSCs).
    Benzyl butyl phthalate
  • HY-104026S
    L-Kynurenine-d4
    		Agonist 99.25%
    L-Kynurenine-d4 is the deuterium labeled L-Kynurenine. L-Kynurenine is a metabolite of the amino acid L-tryptophan. L-Kynurenine is an aryl hydrocarbon receptor agonist[1][2].
    L-Kynurenine-d<sub>4</sub>
  • HY-144339
    AhR agonist 2
    		99.53%
    AhR agonist 2 (Compound 12a) is a potent agonist of aryl hydrocarbon receptor (AhR) with an EC50 of 0.03 nM. AhR agonist 2 induces rapid nuclear enrichment of AhR, triggers the transcription of downstream genes and promote skin barrier repair. AhR agonist 2 has the potential for the research of psoriasis.
    AhR agonist 2
  • HY-18619
    YL-109
    		Modulator 99.26%
    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.
    YL-109
  • HY-B0845
    Prochloraz
    		Activator 99.77%
    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
  • HY-112627
    CAY 10465
    		Agonist 98.30%
    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).
    CAY 10465
  • HY-103221
    MeBIO
    		Agonist ≥98.0%
    MeBIO is a potent AhR (aryl hydrocarbon receptor) agonist, with IC50 of 44 μM (GSK-3) and 55 μM (CDK1/cyclin B), respectively.
    MeBIO
  • HY-135831
    AHR antagonist 2
    		Antagonist 99.91%
    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.
    AHR antagonist 2
  • HY-141609
    AHR antagonist 5 free base
    		Inhibitor 99.56%
    AHR antagonist 5 free base is a selective and orally active aryl hydrocarbon receptor (AHR) inhibitor. AHR antagonist 5 free base effectively blocks AHR from translocating from the cytoplasm to the nucleus. AHR antagonist 5 free base is highly selective for AHR over other receptors, transporters, and kinases.
    AHR antagonist 5 free base
  • HY-N8572
    3',4'-Dimethoxyflavone
    		Antagonist 98.55%
    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
  • HY-N4095
    Brevifolincarboxylic acid
    		Inhibitor 99.90%
    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
  • HY-W007355S
    Skatole-d3
    		Activator ≥98.0%
    Skatole-d3 is the deuterium labeled Skatole. Skatole is produced by intestinal bacteria, regulates intestinal epithelial cellular functions through activating aryl hydrocarbon receptors and p38[1].
    Skatole-d<sub>3</sub>
  • HY-136220
    AHR antagonist 5
    		Antagonist 98.05%
    AHR antagonist 5, a potent and orally active aryl hydrocarbon receptor (AHR) antagonist extracted from patent WO2018195397, example 39, has an IC50 of < 0.5 µΜ. AHR antagonist 5 significantly inhibits tumor growth combined with checkpoint inhibitor anti-PD-1.
    AHR antagonist 5
  • HY-124211
    Dibenzo(a,i)pyrene
    		≥98.0%
    Dibenzo(a,i)pyrene is a 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) receptor ligand.
    Dibenzo(a,i)pyrene
Cat. No. Product Name / Synonyms Application Reactivity