2. Immunology/Inflammation
  3. Aryl Hydrocarbon Receptor

Aryl Hydrocarbon Receptor

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.

Aryl Hydrocarbon Receptor Related Products (54):

Cat. No. Product Name Effect Purity
  • HY-12684
    CH-223191 Antagonist 99.60%
    CH-223191 is a potent and specific antagonist of aryl hydrocarbon receptor (AhR). CH-223191 inhibits TCDD-mediated nuclear translocation and DNA binding of AhR, and inhibits TCDD-induced luciferase activity with an IC50 of 0.03 μM[1].
  • HY-12028
    PD98059 Antagonist 99.94%
    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[1][2][3].
  • HY-104026
    L-Kynurenine Agonist 99.85%
    L-Kynurenine is a metabolite of the amino acid L-tryptophan. L-Kynurenine is an aryl hydrocarbon receptor agonist.
  • HY-15484
    Pifithrin-α hydrobromide Agonist
    Pifithrin-α hydrobromide is a p53 inhibitor which blocks its transcriptional activity and prevents cells from apoptosis. Pifithrin-α hydrobromide is also an aryl hydrocarbon receptor (AhR) agonist.
  • HY-12451
    FICZ Agonist
    FICZ is a potent aryl hydrocarbon receptor (AhR) agonist with a Kd of 70 pM.
  • HY-W011338S
    Benzyl butyl phthalate-d4
    Benzyl butyl phthalate-d4 is the deuterium labeled Benzyl butyl phthalate[1]. 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)[2][3][4].
  • HY-104026BS
    L-Kynurenine-13C10 sulfate
    L-Kynurenine-13C10 (sulfate) is the 13C labeled L-Kynurenine sulfate[1]. L-Kynurenine sulfate, an aryl hydrocarbon receptor (AHR)?agonist that activates AHR-directed, naive T cell polarization to the anti-inflammatory Treg phenotype[2].
  • HY-112629
    PDM2 Antagonist 98.85%
    PDM2 is a selective, high-affinity aryl hydrocarbon receptor (AhR) antagonist with an Ki of 1.2±0.4 nM.
  • HY-117102
    ANI-7 Activator 99.25%
    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[1][2][3].
  • HY-102023
    GNF351 Antagonist 99.90%
    GNF351 is a full aryl hydrocarbon receptor (AHR) antagonist. GNF351 competes with a photoaffinity AHR ligand for binding to the AHR with an IC50 of 62 nM. GNF351 is minimal toxicity in mouse or human keratinocytes[1].
  • HY-N0170
    Indole-3-carbinol Agonist
    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).
  • HY-118780
    CHD-5 Antagonist
    CHD-5 is a potent AhR (aryl hydrocarbon receptor) antagonist[1].
  • HY-124421
    5F-203 Inducer
    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[1][2][3].
  • 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)[1].
  • 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[1].
  • HY-N6264
    26-Deoxyactein Inhibitor
    26-Deoxyactein is a constituent isolated from Cimicifuga racemosa, prevents TCDD-induced osteoblasts damage. 26-Deoxyactein inhibits increased AhR, CYP1A1 and ERK levels[1].
  • HY-15001
    StemRegenin 1 Antagonist
    StemRegenin 1 is a potent aryl hydrocarbon receptor (AhR) antagonist with IC50 of 127 nM.
  • HY-135829
    BAY 2416964 Antagonist 99.59%
    BAY 2416964 is a potent and orally active aryl hydrocarbon receptor (AHR) antagonist extracted from patent WO2018146010A1, example 192, has an IC50 of 341 nM. BAY 2416964 has the potential for solid tumors treatment[1].
  • HY-18619
    YL-109 Modulator 98.74%
    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[1].
  • HY-N8572
    3',4'-Dimethoxyflavone Antagonist 98.76%
    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[1][2][3][4].