AhR

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.

GNF351 is a full aryl hydrocarbon receptor (AHR) antagonist.

StemRegenin 1 (SR1) is a cell-permeable purine derivative that acts as an antagonist of aryl hydrocarbon receptor and promotes the self-renewal of hematopoietic stem cells (HSCs).

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.

CH-223191 is a ligand-selective antagonist of the Ah (Dioxin) receptor.

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.

PDM2 is a selective, high-affinity aryl hydrocarbon receptor (AhR) antagonist with an Ki of 1.2±0.4 nM.

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).

AHR antagonist 1 is an aryl hydrocarbon receptor (AHR) antagonist extracted from patent WO2017202816A1, example 23, has an IC50 of 39.9 nM in human cell line.

1,4-Chrysenequinone, a polycyclic aromatic quinone, acts as an activator of aryl hydrocarbon receptor (AhR).

Mivotilate is a nontoxic, potent activator of the aryl hydrocarbon receptor (AhR), and acts as a hepatoprotective agent.

FICZ is a potent aryl hydrocarbon receptor (AhR) agonist with a Kd of 70 pM.

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.

SGA360 is a selective modulator of aryl hydrocarbon (Ah) receptor that exhibits anti-inflammatory properties.

NSC-703786 (5F-203) is a cytotoxic molecule that forms DNA adducts leading to cell death. NSC-703786 induces aryl hydrocarbon receptor signaling, and elevates expression of CYP1A1. Treatment of cells with NSC-703786 also leads to elevation of reactive oxygen species and activation of p38, JNK and ERK.

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.

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.

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.

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 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.

3'-Methoxy-4'-nitroflavone is a specific antagonist of the aryl hydrocarbon receptor (AhR). This compound inhibits the metabolism of the endogenous ligand FICZ by blocking CYP1, thereby increasing FICZ accumulation. It effectively reverses the anti-apoptotic effects of TCDD and attenuates the activation of Akt and Erk1/2 kinases, as well as TGFα expression induced by TCDD. 3'-Methoxy-4'-nitroflavone is valuable for research into breast tumor promotion, rheumatoid arthritis, multiple sclerosis, and inflammatory bowel disease.

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.

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.

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.

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.

IK-175 is a selective aryl hydrocarbon receptor (AHR) inhibitor that prevents the translocation of AHR from the cytoplasm to the nucleus. This compound exhibits high specificity for AHR, distinguishing itself from other receptors, transporters, and kinases. IK-175 is primarily used in research applications focused on studying AHR-related pathways and their implications in various diseases, including cancer and immune responses.

6,2',4'-Trimethoxyflavone is a potent antagonist of the aryl hydrocarbon receptor (AHR). This compound effectively represses AHR-mediated gene induction, making it a valuable tool for studying AHR-related signaling pathways. Its biological activity supports research in fields such as toxicology, cancer biology, and environmental health.

KYN-101 is a selective AHR inhibitor that is potent and orally active. This compound effectively reduces CYP1A1 mRNA expression, contributing to its role in mediating anti-cancer activity. Researchers can utilize KYN-101 to investigate the therapeutic potential in cancer biology and the modulation of AHR-related signaling pathways.

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.

CAY10464 is a selective aryl hydrocarbon receptor (AhR) antagonist with a high affinity, exhibiting a Ki value of 1.4 nM. This compound effectively inhibits AhR signaling, making it valuable for research applications related to toxicology, environmental studies, and the modulation of immune responses. CAY10464 serves as a crucial tool for investigating the role of AhR in various biological processes and disease mechanisms.

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.

CB7993113 is a potent antagonist of the aryl hydrocarbon receptor (AHR), exhibiting an IC50 value of 0.33 μM. This compound effectively binds to the AHR protein and prevents its nuclear translocation, thereby inhibiting the biological effects mediated by this receptor. CB7993113 demonstrates significant inhibitory activity, reducing polycyclic aromatic hydrocarbon (PAH)- and TCDD-induced reporter activity by 75% and 90%, respectively, making it a valuable tool for research into AHR-related signaling pathways and toxicological studies.

10-Cl-BBQ is a high-affinity ligand for the aryl hydrocarbon receptor (AhR), exhibiting significant immunosuppressive activity. This compound facilitates the translocation of AhR from the cytosol to the nucleus and effectively activates AhR-regulated reporter genes at nanomolar concentrations. Its properties make 10-Cl-BBQ a valuable tool for research in immunology and toxicology, particularly in studies focusing on AhR signaling pathways.

AHR Antagonist 2 is a potent aryl hydrocarbon receptor (AHR) antagonist, displaying IC50 values of 885 pM for human AHR and 2.03 nM for mouse AHR. This compound is valuable for investigations into cancer biology and the modulation of immune responses, making it an important tool for research in immunology and oncology.

Benz[a]anthracene is an aromatic hydrocarbon receptor (AhR) ligand, displaying a pIC50 value of 7.319. As a polycyclic aromatic hydrocarbon (PAH), it is important for studies investigating AhR-mediated biological processes and environmental toxicity. This compound is also relevant in assessing pollution impacts, particularly in samples from areas influenced by industrial activities such as aluminum smelting.

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.

3-OH-Kynurenamine (dihydroiodide) is an aryl hydrocarbon receptor (AhR) activator that modulates the immune response. It enhances the expression levels of indoleamine 2,3-dioxygenase 1 (Ido1) and transforming growth factor-beta 1 (Tgfb1). Research indicates that it can alleviate skin inflammation in psoriasis mouse models and mitigate kidney damage in nephrotoxic lupus mouse models, making it a valuable tool in studying immune-related conditions.

DiMNF (3',4'-Dimethoxy-αNF) is a selective modulator of the aryl hydrocarbon receptor (AHR). Acting as a competitive ligand with an IC50 of 21 nM, it exhibits antagonistic properties that can be harnessed in anti-inflammatory research. DiMNF is valuable for investigating the role of AHR in various biological processes and potential therapeutic applications.

N-Methylscatole is an aryl hydrocarbon receptor (AhR) agonist known for its ability to activate this important transcription factor. It exhibits weak agonistic activity and no significant antagonistic properties. This compound can be utilized in research involving AhR-mediated pathways and the study of environmental chemicals affecting biological systems.

AHR Antagonist 5 is a potent aryl hydrocarbon receptor (AHR) antagonist with an IC50 of less than 0.5 μM. This compound effectively inhibits tumor growth, particularly when used in conjunction with the checkpoint inhibitor anti-PD-1. It serves as a valuable tool for research in cancer biology and the development of combination therapies targeting the immune response.

CHD-5 is a potent antagonist of the aryl hydrocarbon receptor (AhR). This compound effectively inhibits AhR-mediated signaling pathways, which are involved in various biological processes including cellular proliferation and immune responses. CHD-5 is valuable for researchers investigating the role of AhR in cancer biology, immunology, and toxicology.

Corannulene is an agonist of the aryl hydrocarbon receptor (AhR), known for its ability to modulate cellular signaling pathways. This compound exhibits reduced cytotoxicity compared to Benzo[a]pyrene in hepatoma cells, making it a valuable tool in cancer research. Corannulene's unique properties may facilitate the exploration of AhR-related mechanisms in tumor biology and therapeutic interventions.

AHR-IN-1 is a selective aryl hydrocarbon receptor (AHR) inhibitor, exhibiting an IC50 of less than 0.5 μM. This compound is useful for investigating the role of AHR in various biological processes, including immune response modulation and xenobiotic metabolism. AHR-IN-1 serves as a valuable tool for researchers studying the mechanisms by which AHR influences cellular signaling and gene expression.

AHR Antagonist 4 is a potent aryl hydrocarbon receptor (AHR) antagonist with a 2-heteroaryl-3-oxo-2,3-dihydropyridazine-4-carboxamide structure, exhibiting an IC50 of 82.2 nM. This compound demonstrates significant anti-cancer properties, making it a valuable tool for research on cancer biology and therapeutic applications targeting AHR pathways. Its ability to modulate AHR signaling may offer insights into mechanisms driving tumor progression and potential treatment strategies.

AhR Agonist 8 is a potent agonist of the Aryl Hydrocarbon Receptor (AhR) with an EC50 value of 0.154 nM. This compound serves as a valuable tool for investigating the biological processes linked to psoriasis and atopic dermatitis. Its high affinity and specificity make AhR Agonist 8 suitable for research applications targeting immune modulation and skin-related disorders.