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-124421
    5F-203
    		Inducer 99.04%
    5F-203 (NSC-703786) is a cytotoxic molecule that forms DNA adducts and cell cycle arrest. 5F-203 induces aryl hydrocarbon receptor (AhR) signaling and elevates expression of CYP1A1. 5F-203 also increases the levels of reactive oxygen species as well as activates JNK, ERK, and p38.
    5F-203
  • HY-112628
    CAY10464
    		Antagonist 99.77%
    CAY10464 (AHR antagonist 7; compound 4j) is a selective and high-affinity aryl hydrocarbon receptor (AhR) antagonist with a Ki of 1.4 nM.
    CAY10464
  • HY-118438
    10-Cl-BBQ
    		Agonist 99.48%
    10-Cl-BBQ is a high affinity AhR ligand with immunosuppressive activity. 10-Cl-BBQ promotes cytosol to nuclear translocation of AhR and activates the AhR-regulated reporter gene at nanomolar concentrations.
    10-Cl-BBQ
  • HY-117102
    ANI-7
    		Activator 98.13%
    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.
    ANI-7
  • HY-111441
    1,4-Chrysenequinone
    		Activator 98.42%
    1,4-Chrysenequinone, a polycyclic aromatic quinone, acts as an activator of aryl hydrocarbon receptor (AhR).
    1,4-Chrysenequinone
  • HY-W017113
    2-Mercaptobenzothiazole
    		Activator 99.85%
    2-Mercaptobenzothiazole is an activator of the aryl hydrocarbon receptor (AhR), inhibiting thyroid hormone synthesis and dopamine beta-hydroxylase activity. 2-Mercaptobenzothiazole promotes bladder cancer cell invasion by altering the conformation of the AhR ligand binding domain (LBD), activating AhR transcription, and upregulating the mRNA and protein expression of target genes CYP1A1 and CYP1B1. 2-Mercaptobenzothiazole inhibits thyroid peroxidase (TPO) with an IC50 value of 11.5 μM, induces histological changes such as follicular cell hypertrophy in Xenopus laevis tadpoles, delaying metamorphosis. 2-Mercaptobenzothiazole increases chromosomal aberrations and sister chromatid exchanges (SCEs) in Chinese hamster ovary (CHO) cells, and enhances carcinogenicity in F344/N rats. 2-Mercaptobenzothiazole inhibits norepinephrine synthesis in mice and completely blocks the conversion of exogenous dopamine to norepinephrine in rat cardiomyocytes.
    2-Mercaptobenzothiazole
  • HY-118780
    CHD-5
    		Antagonist ≥98.0%
    CHD-5 is a potent AhR (aryl hydrocarbon receptor) antagonist.
    CHD-5
  • HY-N6264
    26-Deoxyactein
    		Inhibitor 99.76%
    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
  • HY-100242
    Mivotilate
    		Activator 99.58%
    Mivotilate is a nontoxic, potent activator of the aryl hydrocarbon receptor (AhR), and acts as a hepatoprotective agent.
    Mivotilate
  • HY-N10123
    Indolokine A5
    		Agonist ≥98.0%
    Indolokine A5, a catabolite of L-cysteine, is a potent AhR agonist.
    Indolokine A5
  • HY-B0311A
    Carbidopa monohydrate
    		Modulator ≥98.0%
    Carbidopa ((S)-(-)-Carbidopa) monohydrate, a peripheral decarboxylase inhibitor, can be used for the research of Parkinson's disease. Carbidopa monohydrate is a selective aryl hydrocarbon receptor (AhR) modulator. Carbidopa monohydrate inhibits pancreatic cancer cell and tumor growth.
    Carbidopa monohydrate
  • HY-77278
    25-Hydroxytachysterol3
    		Agonist 98.89%
    25-Hydroxytachysterol3 is the metabolite of Vitamin D3 (HY-15398). 25-Hydroxytachysterol3 inhibits the proliferation of epidermal keratinocytes and dermal fibroblasts, stimulates the expression of differentiation- and antioxidant-related genes in keratinocytes. 25-Hydroxytachysterol3 activates vitamin D receptor (VDR) and aryl hydrocarbon receptor (AhR), liver X receptor α/β (LXR α/β) and peroxisome proliferator-activated receptor γ (PPARγ), stimulates the expression of CYP24A1.
    25-Hydroxytachysterol3
  • HY-15001G
    Stemregenin 1 (GMP)
    		Antagonist
    Stemregenin 1 (GMP) (SR1 (GMP)) is Stemregenin 1 Y-15001) in GMP grade. GMP-grade small molecules can be used as auxiliary reagents in cell therapy. Stemregenin 1 is a potent aryl hydrocarbon receptor (AhR) antagonist with IC50 of 127 nM.
    Stemregenin 1 (GMP)
  • HY-W007355S1
    Skatole-d8
    		Activator 98.50%
    Skatole-d8 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>8</sub>
  • HY-104026CS
    L-Kynurenine-13C10 sulfate hemihydrate
    		Agonist 99.90%
    L-Kynurenine-13C10 (sulfate hemihydrate) is the 13C labeled L-Kynurenine sulfate. L-Kynurenine sulfate hemihydrate, an aryl hydrocarbon receptor (AHR) agonist that activates AHR-directed, naive T cell polarization to the anti-inflammatory Treg phenotype.
    L-Kynurenine-<sup>13</sup>C<sub>10</sub> sulfate hemihydrate
  • HY-111450
    CB7993113
    		Antagonist ≥98.0%
    CB7993113 is a potent AHR antagonist, with an IC50 of 0.33 μM. CB7993113 directly binds AHR protein and blocks AHR nuclear translocation. CB7993113 inhibits polycyclic aromatic hydrocarbon (PAH)- and TCDD-induced reporter activity by 75% and 90% respectively.
    CB7993113
  • HY-136220A
    AHR antagonist 5 hemimaleate
    		Antagonist
    AHR antagonist 5 hemimaleate, a potent and orally active aryl hydrocarbon receptor (AHR) antagonist, has an IC50 of < 0.5 µΜ. AHR antagonist 5 hemimaleate significantly inhibits tumor growth combined with checkpoint inhibitor anti-PD-1 (WO2018195397, example 39).
    AHR antagonist 5 hemimaleate
  • 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-161649
    hCYP1B1-IN-2
    		Inhibitor
    hCYP1B1-IN-2 (compound 3n) is a potent human cytochrome P450 1B1 enzyme hCYP1B1 inhibitor. hCYP1B1-IN-2 shows the extremely potent anti-hCYP1B1 activity (IC50=0.040 nM) and blocks AhR transcription activity. hCYP1B1-IN-2 potently inhibits hCYP1B1 via a mix inhibition manner, showing a Ki value of 21.71 pM.
    hCYP1B1-IN-2
  • 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
Cat. No. Product Name / Synonyms Application Reactivity