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Aryl hydrocarbon receptor (AhR) ligands act on a ligand-activated transcription factor of the bHLH-PAS family. Cloning of the receptor complementary DNA in 1992 showed that AhR combines a basic helix-loop-helix (bHLH) domain with a Per-Arnt-Sim (PAS) domain. The tryptophan metabolite kynurenine was later described as an endogenous agonist produced by tryptophan 2,3-dioxygenase. Antagonists of AhR were shown to support the expansion of human hematopoietic stem cells in culture, which made StemRegenin 1 a common tool in that work. CH-223191, ITE, tapinarof and L-Kynurenine complete a set that covers both receptor activation and blockade in reporter and gene expression assays.
ITE is a potent endogenous agonist of aryl hydrocarbon receptor (AhR), binding directly to AHR, with a Ki of 3 nM. ITE also has immunosuppressive activity.
Synonyms: (+)-N-Norisoboldine; (+)-Laurelliptine; (S)-(+)-Laurelliptine
Norisoboldine, an alkaloid compound isolated from Radix Linderae, inhibits synovial angiogenesis in adjuvant-induced arthritis rats by moderating Notch1 pathway-related endothelial tip cell phenotype.
Synonyms: Benvitimod; WBI 1001; GSK2894512
Tapinarof (Benvitimod; WBI 1001; GSK2894512) is a natural aryl hydrocarbon receptor (AhR) agonist with an EC50 of 13 nM.
L-Kynurenine is a metabolite of the amino acid L-tryptophan. L-Kynurenine is an aryl hydrocarbon receptor agonist.
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).
Synonyms: Chrysene-1,4-dione
1,4-Chrysenequinone, a polycyclic aromatic quinone, acts as an activator of aryl hydrocarbon receptor (AhR).
Synonyms: YH439
Mivotilate is a nontoxic, potent activator of the aryl hydrocarbon receptor (AhR), and acts as a hepatoprotective agent.
Synonyms: 6-Formylindolo[3,2-b]carbazole
FICZ is a potent aryl hydrocarbon receptor (AhR) agonist with a Kd of 70 pM.
SGA360 is a selective modulator of aryl hydrocarbon (Ah) receptor that exhibits anti-inflammatory properties.
Indole-3-pyruvic acid is an orally active agonist of the aryl hydrocarbon receptor (AHR). This compound exhibits antioxidant properties and is valuable for research into inflammation and anxiety-related pathways. Its role as an AHR modulator makes it a significant tool for studying the physiological effects of this receptor in various biological contexts.
Synonyms: NSC-686288
Aminoflavone is an activator of the aryl hydrocarbon receptor (AhR) with significant anti-tumor properties. It modulates the expression of ITGA6/SOX2 through the AhR-miR-125b-2-3p axis, effectively targeting breast cancer stem cells. This compound promotes the generation of reactive oxygen species (ROS) and elevates oxidative DNA damage, as indicated by increased levels of 8-oxodG and DNA-protein cross-links. Additionally, Aminoflavone induces S-phase cell cycle arrest, activates caspase pathways, and triggers apoptosis, while inhibiting HIF-1α expression independent of the AhR pathway. It serves as a valuable reagent for research into breast cancer mechanisms and therapies.
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Synonyms: 5,6-Benzoflavone; beta-NF
β-Naphthoflavone is a potent aryl hydrocarbon receptor (AHR) agonist that modulates various biological processes, including cell proliferation, differentiation, apoptosis, and metabolism. This compound exhibits antioxidant activity, primarily by enhancing the function of antioxidant enzymes. As a non-carcinogenic CYP1A inducer, β-Naphthoflavone is valuable for investigating the mechanisms underlying aristolochic acid-induced renal injury and other related research applications.
1,4-Dihydroxy-2-naphthoic acid is an agonist of the aryl hydrocarbon receptor (AhR). This compound exhibits significant anti-inflammatory activity and serves as a bacterially derived metabolite, making it of interest in studies related to immune modulation and inflammation. Its role in signaling pathways linked to AhR provides valuable insights for research in toxicology, pharmacology, and environmental health.
AHR Agonist 3 is a potent agonist of the aryl hydrocarbon receptor (AhR) that induces cell cycle arrest and apoptosis by activating tumor-suppressive transcriptional programs. It effectively inhibits the growth of stem cells in triple-negative breast cancer (TNBC) while demonstrating low cytotoxicity towards normal human primary cells. This compound is a valuable tool for cancer research, particularly in studies focused on TNBC and the mechanisms underlying AhR-mediated signaling pathways.
AHR Agonist 10 is a potent agonist of the aryl hydrocarbon receptor (AHR), exhibiting an EC50 of 2.01 nM. This compound significantly upregulates the expression of AHR downstream target genes, such as CYP1A1 and CYP1B1, while downregulating pro-inflammatory markers including CD36, IL-18, CCL5, CCL20, IL-6, and TNF-α. AHR Agonist 10 demonstrates low cytotoxicity (above 40 μM) in normal cells, making it suitable for use in psoriasis research and studies investigating AHR-dependent modulation of inflammatory responses.
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AhR Modulator-1 (6-MCDF) is a selective and orally active modulator of the aryl hydrocarbon receptor (AhR). This compound demonstrates significant inhibition of metastasis by reducing vascular endothelial growth factor (VEGF) production in prostatic tissues prior to tumor formation. Additionally, AhR Modulator-1 exhibits anti-estrogenic effects in the rat uterus, making it a valuable tool for investigating the roles of AhR in cancer biology and endocrine regulation.
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PY109 is a highly selective aryl hydrocarbon receptor (AHR) agonist that exhibits oral bioactivity. It demonstrates potent efficacy with EC50 values of 1.2 nM in human HepG2 cells and 1.4 nM in mouse Hepa-1c1c7 cells. PY109 significantly enhances the expression of CYP1A1 and interleukin-22 (IL-22), while inhibiting interleukin-17A (IL-17A) expression. This compound has been shown to effectively improve colitis in murine models, making it a valuable tool for research focused on inflammatory bowel diseases.
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ANI-7 is an aryl hydrocarbon receptor (AhR) activator that exhibits significant cytotoxicity against various cancer cell lines. It selectively inhibits the growth of MCF-7 breast cancer cells with a GI50 of 0.56 μM. ANI-7 activates the AhR pathway, leading to the induction of CYP1-metabolizing mono-oxygenases, DNA damage, kinase activation, and S-phase cell cycle arrest, ultimately resulting in cell death in sensitive breast cancer cell lines.
MeBIO is a potent aryl hydrocarbon receptor (AhR) agonist, exhibiting an IC50 of 44 μM for GSK-3 and 55 μM for CDK1/cyclin B interactions. This compound is primarily utilized in research to explore the role of AhR signaling in various biological processes, such as immune response regulation and cellular differentiation. Researchers can employ MeBIO to investigate its effects in toxicology studies and the development of therapeutic strategies targeting AhR pathways.
Synonyms: (+)-Laurelliptine hydrochloride
Norisoboldine hydrochloride is an orally active agonist of the aryl hydrocarbon receptor (AhR). This natural isoquinoline alkaloid, predominantly found in Radix Linderae, demonstrates significant biological activity relevant to inflammatory disorders. It is particularly valuable for research related to rheumatoid arthritis and ulcerative colitis.
ZSTK3744 is an aryl hydrocarbon receptor (AhR) agonist that binds directly to AhR, leading to the upregulation of key target genes such as CYP1A1, CYP1B1, and TIPARP. This compound demonstrates notable cell growth inhibitory effects and induces apoptosis specifically in triple-negative breast cancer cells. Its anti-tumor properties make ZSTK3744 a valuable tool for investigating mechanisms underlying chemoresistance in triple-negative breast cancer.
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VAF347 is a highly selective aryl hydrocarbon receptor (AhR) agonist that effectively activates AhR signaling pathways. It has been shown to inhibit the differentiation of CD14+CD11b+ monocytes from granulo-monocytic precursors, demonstrating significant anti-inflammatory activity. VAF347 is utilized in research related to immune modulation and the study of inflammatory responses.
AhR Agonist 2 is a highly potent agonist of the aryl hydrocarbon receptor (AhR), exhibiting an EC50 of 0.03 nM. This compound facilitates the nuclear translocation of AhR, leading to the activation of downstream gene transcription and enhancement of skin barrier repair mechanisms. AhR Agonist 2 is valuable for research applications focused on skin conditions, particularly psoriasis.
2-Mercaptobenzothiazole is an activator of the aryl hydrocarbon receptor (AhR), functioning as an inhibitor of thyroid hormone synthesis and dopamine beta-hydroxylase activity. This compound promotes the invasion of bladder cancer cells by activating AhR transcription and upregulating the expression of CYP1A1 and CYP1B1, implicated in carcinogenesis. Additionally, 2-Mercaptobenzothiazole exhibits inhibition of thyroid peroxidase activity with an IC50 of 11.5 μM and induces significant histological changes in Xenopus laevis, including delayed metamorphosis. It also increases chromosomal aberrations in Chinese hamster ovary cells and inhibits norepinephrine synthesis in murine models, demonstrating its relevance in carcinogenic studies and neurobiological research.
Indolokine A5 is a potent AhR (Aryl hydrocarbon receptor) agonist that plays a significant role in various biological processes. This compound is of particular interest in research applications involving immunology, toxicology, and cancer biology, where AhR activation may influence cellular responses and signaling pathways. Its ability to modulate AhR activity makes Indolokine A5 a valuable tool for studying the effects of environmental contaminants and endogenous ligands on cellular function.
