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

Aryl Hydrocarbon Receptor

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-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-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-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
  • HY-D0932
    Sudan IV
    		Agonist ≥98.0%
    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
  • 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-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-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-N4095
    Brevifolincarboxylic acid
    		Inhibitor 99.90%
    Brevifolincarboxylic acid is a phenolic compound. Brevifolincarboxylic acid can be isolated from Duchesnea chrysantha. Brevifolincarboxylic acid inhibits α-glucosidase with an IC50 value of 323.46 μM. Brevifolincarboxylic acid has an inhibitory effect on the aryl hydrocarbon receptor (AhR). Brevifolincarbacid scavenges ROS. Brevifolincarbacid restores the glucose uptake activity of myotubes. Brevifolincarboxylic acid has antitumor activity against lung and gastric cancer. Brevifolincarbacid can be used in the study of diabetes and inflammatory diseases.
    Brevifolincarboxylic acid
  • 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-W014701
    1,4-Dihydroxy-2-naphthoic acid
    		Activator 99.60%
    1,4-Dihydroxy-2-naphthoic acid is an aryl hydrocarbon receptor (AhR) agonist. 1,4-Dihydroxy-2-naphthoic acid is also a bacterially derived metabolite and has anti-inflammatory activity.
    1,4-Dihydroxy-2-naphthoic acid
  • 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-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-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-W012248
    KG-655
    		99.87%
    KG-655 is a small molecule compound that binds to the β-folded surface and internal cavity of ARNT PAS-B and interferes with its binding to the transcriptional coactivator TACC3. KG-655 can promote the homodimerization of ARNT PAS-B and has the potential to regulate multiple ARNT-mediated signaling pathways.
    KG-655
  • HY-124404
    12(R)-HETE
    		Activator 99.90%
    12(R)-HETE is a metabolite of Arachidonic acid, AA (HY-109590) and can be found in skin from psoriatic lesions. 12(R)-HETE induces lymphocytes chemotaxis, stimulates calcium mobilization and chemotaxis in neutrophils via the BLT1 receptor, activates the aryl hydrocarbon receptor, and inhibits Na+/K+ ATPase activity in the corneal epithelium.
    12(R)-HETE
  • 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-118780
    CHD-5
    		Antagonist ≥98.0%
    CHD-5 is a potent AhR (aryl hydrocarbon receptor) antagonist.
    CHD-5
  • HY-N10123
    Indolokine A5
    		Agonist ≥98.0%
    Indolokine A5, a catabolite of L-cysteine, is a potent AhR agonist.
    Indolokine A5
  • 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-118474
    GW 610
    		Activator 99.78%
    GW 610 (NSC 721648), an antitumor agent, is a potent AhR ligand with a Ki of 6.8 nM. GW 610 induces CYP1A1 expression in MCF-7 cells. GW 610 shows potent and selective anticancer activity against lung, colon, and breast cancer cell lines.
    GW 610
Cat. No. Product Name / Synonyms Application Reactivity