Aryl Hydrocarbon Receptor Ligand

Tryptamine is a selective, blood-brain-penetrating 5-HT4 receptor agonist (EC50=1-3 mM) and an endogenous ligand of the aryl hydrocarbon receptor (AHR) (Kd=10-50 nM). Tryptamine promotes intestinal anion secretion and fluid transport by activating G protein-coupled receptors (GPCRs) and accelerates gastrointestinal motility. Tryptamine regulates Th17/Treg balance to inhibit neuroinflammation, competitively binds to 5-HT receptors to regulate central nervous system activity, and participates in temperature regulation and spinal reflex regulation as a neuromodulator. Tryptamine can be used to study intestinal motility disorders such as functional constipation, and has shown significant efficacy in multiple sclerosis models.

Dibenzo (a,i) pyrene is a polycyclic aromatic hydrocarbon and also a carcinogenic ligand of the TCDD (Ah) receptor. Dibenzo (a,i) pyrene binds to the TCDD (Ah) receptor in rat liver. Dibenzo (a,i) pyrene induces DNA adduct formation and upregulates the protein levels of p53 and p21^WAF1 in diploid lung fibroblasts. Dibenzo (a,i) pyrene alters the cell cycle distribution of diploid lung fibroblasts, increasing the proportion of cells in the S phase, decreasing the proportions of cells in the G0/G1 and G2/M phases, and causing S phase delay/arrest. Dibenzo (a,i) pyrene is applicable for cancer research.

β-NF-JQ1 is a BRD2/3/4 PROTAC degrader. β-NF-JQ1 recruits the AhR E3 ligase complex to BRD2, BRD3 and BRD4, induces AhR-BRD interaction, and mediates AhR-dependent degradation through the proximity effect between the target protein and AhR. β-NF-JQ1 acts as an antiproliferative and cytotoxic agent that induces anticancer activity associated with BRD protein knockdown. β-NF-JQ1 can be used for research on breast cancer and neuroblastoma.

Benz[a]anthracene (Tetraphene) is a polycyclic aromatic hydrocarbon pollutant and also a ligand of aryl hydrocarbon receptor 2 (AHR2), with a pIC₅₀ of 7.319. Benz[a]anthracene can be detected in spruce needles near aluminum smelters. Exposure to Benz[a]anthracene during zebrafish embryonic stage activates the AHR-CYP1A signaling pathway and induces AHR2 expression, leading to social behavioral deficits that persist into adulthood, accompanied by impaired neuro-immune interaction, while anxiety levels remain unaffected. Benz[a]anthracene can be used in studies related to PAH environmental toxicology, developmental neurotoxicity and biodegradation.

Benz[a]anthracene-d12 (Tetraphene-d12) is the deuterated-labeled Benz[a]anthracene (HY-W012278). Benz[a]anthracene (Tetraphene) is a polycyclic aromatic hydrocarbon pollutant and also a ligand of aryl hydrocarbon receptor 2 (AHR2), with a pIC₅₀ of 7.319. Benz[a]anthracene can be detected in spruce needles near aluminum smelters. Exposure to Benz[a]anthracene during zebrafish embryonic stage activates the AHR-CYP1A signaling pathway and induces AHR2 expression, leading to social behavioral deficits that persist into adulthood, accompanied by impaired neuro-immune interaction, while anxiety levels remain unaffected. Benz[a]anthracene can be used in studies related to PAH environmental toxicology, developmental neurotoxicity and biodegradation.

X15695 is selective and orally active estrogen receptor (ERα) degrader. X15695 is an aryl hydrocarbon receptor (AHR) ligand. X15695 enables AHR to form a complex with the ERα, promoting its proteasomal degradation. X15695 inhibits the breast cancer cells proliferation, promotes cell cycle block and induces apoptosis. X15695 can be used for the study of breast cancer.

2,3-Dichlorodibenzofuran (Compound 29; R: 2,3-Cl₂) is an aryl hydrocarbon receptor (Ah receptor) ligand, with a pEC₅₀ value of 5.326.

2,3,8-Trichlorodibenzofuran is a cytosolic aryl hydrocarbon (Ah) receptor ligand with a pEC₅₀ of 6.000.

1,2,3,7,8,9-Hexachlorodibenzofuran is a polychlorinated dibenzofuran homologue. 1,2,3,7,8,9-Hexachlorodibenzofuran can interact with AhR. 1,2,3,7,8, 9-hexachlorodibenzofuran is highly toxic, teratogenic, carcinogenic and mutagenic.