AhR

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

Tapinarof (Benvitimod; WBI 1001; GSK2894512) is a natural aryl hydrocarbon receptor (AhR) agonist with an EC50 of 13 nM.

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.

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.

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.

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.

Benzyl butyl phthalate is an aryl hydrocarbon receptor (AhR) activator that plays a significant role in cellular signaling. It has been shown to promote the migration and invasion of hemangioma (HA) cells through the upregulation of Zeb1. In breast cancer cells, Benzyl butyl phthalate activates the SPHK1/S1P/S1PR3 pathway, contributing to the formation of metastasis-initiating breast cancer stem cells (BCSCs). This compound is instrumental for research in cancer biology and cellular signaling.

AFP464 is a prodrug of Aminoflavone and an agonist of the aryl hydrocarbon receptor (AhR). It exhibits significant biological activity by downregulating α6-integrin expression, inhibiting breast tumor growth, and reducing the population of tumor-initiating cells. Additionally, AFP464 disrupts mammosphere structure, induces mucin lake cluster formation, triggers DNA damage, and demonstrates antiproliferative effects. This compound is suitable for research applications focused on breast cancer.

Dibenz[a,h]anthracene (DBA) acts as a potent agonist of the aryl hydrocarbon receptor (AhR) and is classified as a polycyclic aromatic hydrocarbon. It is known for its significant carcinogenic properties, inducing dose-dependent increases in DNA adduct formation and mutation frequency in lacZ assays. Additionally, DBA has been shown to upregulate the St3gal5 gene. This reagent is applicable in cancer research, particularly in studies examining mechanisms of carcinogenesis and the role of AhR signaling in tumor development.