Aryl Hydrocarbon Receptor Agonist

CAY 10465 is a selective and high-affinity AhR agonist, with a K_i of 0.2 nM, and shows no effect on estrogen receptor (K_i >100000 nM).

PY109 is an orally active and highly selective aryl hydrocarbon receptor (AHR) agonist. PY109's EC₅₀ values in human-derived HepG2 and mouse Hepa-1c1c7 cells are 1.2 nM and 1.4 nM respectively. PY109 significantly upregulates the expression of CYP1A1 and IL-22, and inhibits the expression of IL-17A. PY109 significantly improves colitis in mice. PY109 can be used for research on colitis.

1-Hydroxypyrene-d₉ is the deuterium labeled 1-Hydroxypyrene (HY-W014075). 1-Hydroxypyrene, a biomarker of exposure to polycyclic aromatic hydrocarbons (PAHs), is analyzed in urine samples. 1-Hydroxypyrene is the major biomarker of exposure to pyrenes. 1-Hydroxypyrene is the orally active agonist for aryl hydrocarbon receptor (AhR) and can lead to renal fibrosis.

Diosmin (Standard) is the analytical standard of Diosmin. This product is intended for research and analytical applications. Diosmin is a flavonoid found in a variety of citrus fruits and also an agonist of the aryl hydrocarbon receptor (AhR).

AFP464 (NSC710464) dihydrochloride is a prodrug of Aminoflavone (HY-132974) and an agonist of the aryl hydrocarbon receptor (AhR). AFP464 dihydrochloride downregulates the expression of α6-integrin (α6-integrin), inhibits breast tumor growth, reduces the population of tumor-initiating cells, disrupts mammosphere structure, induces the formation of mucin lake clusters, triggers DNA damage, and exerts antiproliferative activity. AFP464 dihydrochloride is rapidly converted to Aminoflavone by nonspecific esterases in plasma and cell culture media. AFP464 dihydrochloride is applicable to research related to breast cancer.

Indole-3-carbinol (Standard) is the analytical standard of Indole-3-carbinol. This product is intended for research and analytical applications. 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).

β-Naphthoflavone (Standard) is the analytical standard of β-Naphthoflavone. This product is intended for research and analytical applications. β-Naphthoflavone is an exogenous aryl hydrocarbon receptor (AHR) ligand. β-Naphthoflavone can activate AHR to participate in various biological processes, including cell growth, differentiation, apoptosis, and metabolism. β-Naphthoflavone has antioxidant activity and can exert its antioxidant function by regulating the activity of antioxidant enzymes. β-Naphthoflavone is also a non-carcinogenic CYP1A inducer and can be used to study aristolochic acid (AAI) induced renal injury.

D-Kynurenine (Standard) is the analytical standard of D-Kynurenine. This product is intended for research and analytical applications. D-kynurenine, a metabolite of D-tryptophan, can serve as the bioprecursor of kynurenic acid (KYNA) and 3-hydroxykynurenine. D-Kynurenine is an agonist for G protein-coupled receptor, GPR109B. D-Kynurenine is a substrate in a fluorometric assay of D-amino acid oxidase. D-kynurenine promotes epithelial-to-mesenchymal transition via activating aryl hydrocarbon receptor (AHR).

AFP464 (NSC710464) free base is a prodrug of Aminoflavone (HY-132974) and an agonist of the aryl hydrocarbon receptor (AhR). AFP464 free base downregulates the expression of α6-integrin (α6-integrin), inhibits breast tumor growth, reduces the population of tumor-initiating cells, disrupts mammosphere structure, induces the formation of mucin lake clusters, triggers DNA damage, and exerts antiproliferative activity. AFP464 free base is rapidly converted to Aminoflavone by nonspecific esterases in plasma and cell culture media. AFP464 free base is applicable to research related to breast cancer.

Indolokine A5, a catabolite of L-cysteine, is a potent AhR agonist.

L-Kynurenine-¹³C10 (sulfate hemihydrate) is the ¹³C labeled L-Kynurenine sulfate. L-Kynurenine sulfate hemihydrate, an aryl hydrocarbon receptor (AHR) agonist that activates AHR-directed, naive T cell polarization to the anti-inflammatory Treg phenotype.

Corannulene is an agonist of aryl hydrocarbon receptor (AhR). Corannulene causes less cytotoxic responses than Benzo[a]pyrene (HY-107377) in hepatoma cells. Corannulene is promising for research of cancers.

N-Methylscatole (compound 70130) is a weak aryl hydrocarbon receptor (AhR) agonist exhibiting no significant antagonistic activity.

Sudan IV (Standard) (Solvent Red 24 (Standard)) is the analytical standard of Sudan IV (HY-D0932). This product is intended for research and analytical applications. Sudan IV is an agonist of the aryl hydrocarbon receptor (AhR) that activates downstream signaling pathways and induces CYP1A1 expression. Sudan IV promotes CYP1A1 gene transcription by activating AhR-ARNT heterodimers and binding to exogenous response elements (XREs) on DNA, thereby enhancing drug metabolizing enzyme activity. Sudan IV can be used to study the toxicity mechanisms of industrial dyes and the effects of interactions with serum proteins (such as bovine serum albumin (BSA)) on their distribution in vivo. Sudan IV is a fat-soluble diazo dye that can be used to stain lipids, triglycerides, and lipoproteins on frozen sections.

ZSTK3744 is an aryl hydrocarbon receptor (AhR) agonist. ZSTK3744 directly binds to AhR, upregulates the expression of AhR target genes including CYP1A1, CYP1B1 and TIPARP, and mediates cell growth inhibitory activity in triple-negative breast cancer cells. ZSTK3744 induces apoptosis in triple-negative breast cancer cells. ZSTK3744 exhibits anti-tumor activity and can be used in the research of chemoresistant triple-negative breast cancer.

ZSTK3744 free base is an aryl hydrocarbon receptor (AhR) agonist. ZSTK3744 free base directly binds to AhR, upregulates the expression of AhR target genes including CYP1A1, CYP1B1 and TIPARP, and mediates cell growth inhibitory activity in triple-negative breast cancer cells. ZSTK3744 free base induces apoptosis in triple-negative breast cancer cells. ZSTK3744 free base exhibits anti-tumor activity and can be used in the research of chemoresistant triple-negative breast cancer.

AHR agonist 10 is a potent AHR agonist (EC₅₀ = 2.01 nM). AHR agonist 10 can elevate the transcript levels of key AHR downstream pathway target genes, including CYP1A1 and CYP1B1. AHR agonist 10 can downregulate the expression levels of CD36, IL-18 and shows low cytotoxicity (>40 μM) to normal cells. AHR agonist 10 can suppress the expression of CCL5, CCL20, IL-6, IL-8, S100A9, TLR4, TNF-α, and TNFR1, demonstrating that AHR agonist 10 effectively modulate inflammatory responses through AHR dependent signaling pathways. AHR agonist 10 can be used for psoriasis research.

10 (11)-Cl-BBQ is a high-affinity aryl hydrocarbon receptor (AhR) agonist. 10 (11)-Cl-BBQ is a mixture of 10-Cl-BBQ and 11-Cl-BBQ, among which 11-Cl-BBQ exhibits higher AhR activation potency than 10-Cl-BBQ. Low-dose/short-term AhR activation by 10 (11)-Cl-BBQ promotes IL-17 production, while high-dose/sustained activation induces regulatory T cells and suppresses immune responses. 10 (11)-Cl-BBQ can be used in immunomodulation research.

AhR agonist 5 is an AHR agonist (EC₅₀ = 6 nM). From patent WO2024061187A1, compound 5.

AhR agonist 8 (compound 9) is a potent Aryl Hydrocarbon Receptor (AhR) agonist with an EC₅₀ of 0.154 nM. AhR agonist 8 can be used in the study of psoriasis and atopic dermatitis.