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Home >> Signaling Pathways >> Immunology/Inflammation >> Aryl Hydrocarbon Receptor

Aryl Hydrocarbon Receptor

Aryl Hydrocarbon Receptor (AhR or AHR or ahr or ahR) is a protein that in humans is encoded by the AHR gene. The aryl hydrocarbon receptor is a ligand-activated transcription factor involved in the regulation of biological responses to planar aromatic (aryl) hydrocarbons, and regulates xenobiotic-metabolizing enzymes such as cytochrome P450s, most notably cyp 1A1.

Aryl Hydrocarbon Receptor is a member of the family of basic helix-loop-helix transcription factors. AhR binds several exogenous ligands including natural plant flavonoids, polyphenolics and indoles, as well as synthetic polycyclic aromatic hydrocarbons and dioxin-like compounds. AhR is a cytosolic transcription factor that is normally inactive, binding to several co-chaperones. Upon ligand binding to chemicals such as 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD), the chaperones dissociate resulting in AhR translocating into the nucleus and dimerizing with ARNT (AhR nuclear translocator), leading to changes in gene transcription.

Targets for  Aryl Hydrocarbon Receptor

Products for  Aryl Hydrocarbon Receptor

  1. Cat.No. Product Name Information
  2. GC33314 1,4-Chrysenequinone (Chrysene-1,4-dione) 1,4-Chrysenequinone (Chrysene-1,4-dione), a polycyclic aromatic quinone, acts as an activator of aryl hydrocarbon receptor (AhR). 1,4-Chrysenequinone (Chrysene-1,4-dione) Chemical Structure
  3. GC50422 10-Cl-BBQ Potent aryl hydrocarbon receptor (AhR) agonist; orally bioavailable 10-Cl-BBQ Chemical Structure
  4. GC74164 25-Hydroxytachysterol3

    25-droxytacsterol3 is the metabolite of Vitamin D3.

     25-Hydroxytachysterol3 Chemical Structure
  5. GC68631 AhR agonist 2

    AhR agonist 2 (Compound 12a) is an effective aryl hydrocarbon receptor (AhR) agonist with an EC50 of 0.03 nM. AhR agonist 2 induces rapid nuclear enrichment of AhR, triggers downstream gene transcription, and promotes skin barrier repair. AhR agonist 2 has the potential to be studied for psoriasis treatment.

     AhR agonist 2 Chemical Structure
  6. GC35271 AHR antagonist 1

    AHR antagonist 1

     AHR antagonist 1 (AHR antagonist 1) is an aryl hydrocarbon receptor (AHR) antagonist. AHR antagonist 1 Chemical Structure
  7. GC39669 AHR antagonist 2 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 Chemical Structure
  8. GC64275 AHR antagonist 5 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 ?Μ. AHR antagonist 5 significantly inhibits tumor growth combined with checkpoint inhibitor anti-PD-1. AHR antagonist 5 Chemical Structure
  9. GC64208 AHR antagonist 5 free base 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 Chemical Structure
  10. GC39284 ANI-7 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 Chemical Structure
  11. GC60636 Benzyl butyl phthalate 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 Chemical Structure
  12. GC35553 Brevifolincarboxylic acid

    Brevifolin Carboxylic Acid

     Brevifolincarboxylic acid is extracted from Polygonum capitatum, has inhibitory effect on the aryl hydrocarbon receptor (AhR). Brevifolincarboxylic acid Chemical Structure
  13. GC47037 Carbidopa (hydrate) Carbidopa ((S)-(-)-Carbidopa) monohydrate, a peripheral decarboxylase inhibitor, can be used for the research of Parkinson's disease. Carbidopa (hydrate) Chemical Structure
  14. GC38059 Cardamonin A chalconoid with anti-inflammatory and anti-tumor activity Cardamonin Chemical Structure
  15. GC18824 CAY10465 The aryl hydrocarbon receptor (AhR) is a ligand-dependent intracellular transcription factor whose ligands include some of the most infamous xenobiotics, including dioxin, benzo[a]pyrene, and numerous polyaromatics from soot and coal tar. CAY10465 Chemical Structure
  16. GC72826 CB7993113 CB7993113 is a potent AHR antagonist, with an IC50 of 0.33 μM. CB7993113 Chemical Structure
  17. GC16220 CH 223191 CH 223191 is an effective and specific antagonist of the aryl hydrocarbon receptor (AhR), capable of inhibiting TCDD-mediated AhR nuclear translocation and DNA binding, and suppresses TCDD-induced luciferase activity, with an IC50 of 0.03 μM. CH 223191 Chemical Structure
  18. GC67892 CHD-5 CHD-5 Chemical Structure
  19. GC45705 D-Kynurenine An antagonist of GPR109B D-Kynurenine Chemical Structure
  20. GC72948 Dibenzo(a,i)pyrene Dibenzo(a,i)pyrene is a 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) receptor ligand. Dibenzo(a,i)pyrene Chemical Structure
  21. GN10706 Diosimin

    3’,5,7-Trihydroxy-4’-methoxyflavone 7-rutinoside

     Diosimin Chemical Structure
  22. GC36043 FICZ

    FICZ

     FICZ (Formyl-indolo [3,2-b] carbazole), as an endogenous ligand for the aryl hydrocarbon receptor (AhR), can exert pleiotropic effects including protection against inflammation, fibrosis, and oxidative stress. FICZ Chemical Structure
  23. GC34597 GNF351 GNF351 is a full aryl hydrocarbon receptor (AHR) antagonist. GNF351 Chemical Structure
  24. GC16368 Indole-3-carbinol

    3-hydroxymethyl Indole, I3C, Indinol, 1H-Indole-3-methanol, 3-Indolylmethanol, NSC 525801

     anticarcinogenic drug Indole-3-carbinol Chemical Structure
  25. GC12628 ITE AHR agonist ITE Chemical Structure
  26. GC69347 KYN-101

    KYN-101 is an effective, selective, and orally active AHR inhibitor. KYN-101 reduces CYP1A1 mRNA expression. KYN-101 has anti-cancer activity.

     KYN-101 Chemical Structure
  27. GC12040 L-Kynurenine

    3-anthraniloyl-Alanine, L-KYN

     L-Kynurenine is a metabolite of L-tryptophan and an aryl hydrocarbon receptor (AhR) agonist. L-Kynurenine Chemical Structure
  28. GC70236 L-Kynurenine-13C10 sulfate hemihydrate L-Kynurenine-13C10 (sulfate hemihydrate) is the 13C labeled L-Kynurenine sulfate. L-Kynurenine-13C10 sulfate hemihydrate Chemical Structure
  29. GC64898 L-Kynurenine-d4-1 L-Kynurenine-d4-1 Chemical Structure
  30. GC30297 Mivotilate (YH439)

    YH439

     Mivotilate (YH439) is a nontoxic, potent activator of the aryl hydrocarbon receptor (AhR), and acts as a hepatoprotective agent. Mivotilate (YH439) Chemical Structure
  31. GC11817 PDM 2 potent and selective aryl hydrocarbon receptor (AhR) antagonist PDM 2 Chemical Structure
  32. GC10538 Pifithrin-α (PFTα)

    PFTα

     Pifithrin-α(PFT-α) is a p53 inhibitor.Pifithrin-α widely used in neuroscience to block neuronal apoptotic cell death.Pifithrin-α is also a potent stimulant of aryl hydrocarbon receptor (AhR). Pifithrin-α (PFTα) Chemical Structure
  33. GC44686 Prochloraz

    BTS-40542

     Prochloraz is an imidazole antifungal that inhibits ergosterol biosynthesis via inhibition of the cytochrome P450-dependent 14α-demethylation of lanosterol, which results in disruption of the fungal cell membrane and cell death. Prochloraz Chemical Structure
  34. GC30646 Skatole(3-Methylindole)

    3-Methyl-1H-indole

     Skatole(3-Methylindole) is produced by intestinal bacteria, regulates intestinal epithelial cellular functions through activating aryl hydrocarbon receptors and p38. Skatole(3-Methylindole) Chemical Structure
  35. GC69908 Skatole-d3

    3-Methylindole-d3; 3-Methyl-1H-indole-d3

    Skatole-d3 is the deuterated form of Skatole. Skatole is a substance produced by intestinal bacteria that activates aryl hydrocarbon receptors and regulates intestinal epithelial cell function through p38 activation.

     Skatole-d3 Chemical Structure
  36. GC17043 StemRegenin 1 (SR1)

    SR1

     Antagonizes hematopoietic stem cell differentiation StemRegenin 1 (SR1) Chemical Structure
  37. GC31732 Tapinarof (WBI 1001) Tapinarof (WBI 1001) (WBI-1001) is a natural aryl hydrocarbon receptor (AhR) agonist with an EC50 of 13 nM. Tapinarof (WBI 1001) Chemical Structure

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