2. Signalwege
  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.

Art. -Nr. Produktname Wirkung Reinheit Chemical Structure
  • 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-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-104026S5
    L-Kynurenine-13C10 sulfate hydrate
    		99.9%
    L-Kynurenine-13C10 sulfate hydrate is the C13 labeled L-Kynurenine sulfate hydrate. L-Kynurenine is an aryl hydrocarbon receptor agonist.
    L-Kynurenine-<sup>13</sup>C<sub>10</sub> sulfate hydrate
  • HY-W012278
    Benz[a]anthracene
    		Ligand 99.90%
    Benz[a]anthracene (Tetraphene) (Compound 92) is a ligand for the aryl hydrocarbon receptor (AhR) with a pIC50 of 7.319. Benz[a]anthracene is a polycyclic aromatic hydrocarbon (PAH) that can be detected in spruce needles near aluminum smelters.
    Benz[a]anthracene
  • HY-124404
    12(R)-HETE
    		Activator 99.90%
    12(R)-HETE is a CYP-dependent arachidonic acid metabolite that acts as a proinflammatory lipid mediator. 12 (R)-HETE widely exists in various tissues including the eye, skin and liver. In the cornea, 12(R)-HETE is metabolized via pathways such as β-oxidation into the precursor of 12(R)-HETrE. Without direct receptor binding, 12(R)-HETE indirectly activates AHR-mediated target gene transcription, while inhibiting the enzymatic activity of Na+,K+-ATPase and the intracellular calcium elevation induced by TP agonists. 12(R)-HETE also possesses multiple physiological effects such as chemotaxis, proangiogenesis, vasodilation, natriuresis, diuresis and intraocular pressure reduction, and can be widely used in studies related to psoriasis, inflammatory skin diseases and ocular inflammation.
    12(R)-HETE
  • 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.
    Skatole-d<sub>8</sub>
  • HY-111441
    1,4-Chrysenequinone
    		Activator 99.97%
    1,4-Chrysenequinone, a polycyclic aromatic quinone, acts as an activator of aryl hydrocarbon receptor (AhR).
    1,4-Chrysenequinone
  • HY-W764758
    3-OH-Kynurenamine dihydroiodide
    		Activator 99.56%
    3-OH-Kynurenamine dihydroiodide is the dihydroiodide form of 3-OH-Kynurenamine (HY-156908). 3-OH-Kynurenamine dihydroiodide is an activator for aryl hydrocarbon receptor (AhR), and thus regulates the immune response. 3-OH-Kynurenamine dihydroiodide upregulates the expressions of Ido1 and Tgfb1, ameliorates the skin inflammation in psoriasis mouse model and kidney damage in nephrotoxic lupus mouse model.
    3-OH-Kynurenamine dihydroiodide
  • HY-W014075S
    1-Hydroxypyrene-d9
    		Agonist 99.95%
    1-Hydroxypyrene-d9 is the deuterium labeled 1-Hydroxypyrene (HY-W014075). 1-Hydroxypyrene, a biomarker of exposure to polycyclic aromatic hydrocarbons (PAHs), is analyzed in urine samples. 1-Hydroxypyrene is the major biomarker of exposure to pyrenes. 1-Hydroxypyrene is the orally active agonist for aryl hydrocarbon receptor (AhR) and can lead to renal fibrosis.
    1-Hydroxypyrene-d<sub>9</sub>
  • HY-135831
    AHR antagonist 2
    		Antagonist 99.30%
    AHR antagonist 2 (Example 1) is a potent aryl hydrocarbon receptor (AHR) antagonist with IC50s of 885 pM and 2.03 nM for human and mouse AHR. AHR antagonist 2 can be used for the studies of cancers and imbalance of the immune response.
    AHR antagonist 2
  • HY-B0311AS
    Carbidopa-d3 monohydrate
    		Modulator 98.53%
    Carbidopa-d3 (monohydrate) is the deuterium labeled Carbidopa monohydrate. 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-d<sub>3</sub> monohydrate
  • HY-W007355R
    Skatole (Standard)
    		Activator
    Skatole (Standard) is the analytical standard of Skatole. This product is intended for research and analytical applications. 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 (Standard)
  • HY-12028R
    PD98059 (Standard)
    		Antagonist
    PD98059 (Standard) is the analytical standard of PD98059. This product is intended for research and analytical applications. 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 (Standard)
  • HY-109131
    Foscarbidopa
    		Inhibitor
    Foscarbidopa (ABBV-951; Carbidopa 4′-monophosphate) is an inhibitory prodrug targeting peripheral aromatic L-amino acid decarboxylase. Foscarbidopa is hydrolyzed into Carbidopa (HY-B0311) by phosphatases in vivo to suppress peripheral metabolism of levodopa and elevate brain delivery of levodopa. Foscarbidopa can be used for the research of Parkinson’s disease and advanced Parkinson’s disease.
    Foscarbidopa
  • HY-147128
    PY109
    		Agonist 99.15%
    PY109 is an orally active and highly selective aryl hydrocarbon receptor (AHR) agonist. PY109's EC50 values in human-derived HepG2 and mouse Hepa-1c1c7 cells are 1.2 nM and 1.4 nM respectively. PY109 significantly upregulates the expression of CYP1A1 and IL-22, and inhibits the expression of IL-17A. PY109 significantly improves colitis in mice. PY109 can be used for research on colitis.
    PY109
  • HY-16031B
    AFP464 dihydrochloride
    		Agonist 99.45%
    AFP464 (NSC710464) dihydrochloride is a prodrug of Aminoflavone (HY-132974) and an agonist of the aryl hydrocarbon receptor (AhR). AFP464 dihydrochloride downregulates the expression of α6-integrin (α6-integrin), inhibits breast tumor growth, reduces the population of tumor-initiating cells, disrupts mammosphere structure, induces the formation of mucin lake clusters, triggers DNA damage, and exerts antiproliferative activity. AFP464 dihydrochloride is rapidly converted to Aminoflavone by nonspecific esterases in plasma and cell culture media. AFP464 dihydrochloride is applicable to research related to breast cancer.
    AFP464 dihydrochloride
  • HY-103222
    DiMNF
    		Modulator 98.46%
    DiMNF (3',4'-Dimethoxy-αNF) is a selective aryl hydrocarbon receptor (AHR) modulator. DiMNF is a competitive AHR ligand (IC50 = 21 nM) with apparent antagonistic activity. DiMNF can be used as an anti-inflammatory agent.
    DiMNF
  • HY-N0170R
    Indole-3-carbinol (Standard)
    		Agonist
    Indole-3-carbinol (Standard) is the analytical standard of Indole-3-carbinol. This product is intended for research and analytical applications. 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 (Standard)
  • HY-N0178R
    Diosmin (Standard)
    		Agonist
    Diosmin (Standard) is the analytical standard of Diosmin. This product is intended for research and analytical applications. Diosmin is a flavonoid found in a variety of citrus fruits and also an agonist of the aryl hydrocarbon receptor (AhR).
    Diosmin (Standard)
  • HY-114740R
    β-Naphthoflavone (Standard)
    		Agonist
    β-Naphthoflavone (Standard) is the analytical standard of β-Naphthoflavone. This product is intended for research and analytical applications. 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 study aristolochic acid (AAI) induced renal injury.
    β-Naphthoflavone (Standard)
Art. -Nr. Produktname / Synonyms Application Reactivity