aryl hydrocarbon receptor

CH-223191 is a specific and effective aromatic hydrocarbon receptor (AhR) antagonist, and its IC50 value for inhibiting luciferase activity induced by TCDD is 0.03 μM. CH-223191 can be used in tumor immunotherapy, cytotoxicity research, stem cell research, inflammation research and neuroprotection.

PD98059 is an MEK inhibitor that inhibits MEK1 and MEK2 (IC50=2/50 μM) and is non-ATP-competitive. PD98059 is also antagonistic as a ligand for AHR. PD98059 inhibits autophagy.

Pifithrin-α hydrobromide (Pifithrin-α hydrobromide) is a p53 inhibitor, inhibiting p53-dependent transactivation of p53-responsive genes.

BAY-218 is an aryl hydrocarbon receptor (AHR) antagonist with IC50 of 39.9 nM in the human glioblastoma U87 cell line. BAY-218 inhibition of AhR stimulates pro-inflammatory monocyte and T cell responses in vitro and drives anti-tumor immune responses, leading to reduced tumor growth in vivo.

AHR antagonist 2 is an antagonist of the aryl hydrocarbon receptor. The IC50s for human AHR and mouse AHR are 0.885 and 2.03 nM, respectively.

AHR antagonist 4 is a potent aryl hydrocarbon receptor (AHR) antagonist(example 293; IC50: 82.2 nM).It has anti-cancer effects.

ANI-7 is an activator of the aryl hydrocarbon receptor (AhR) pathway, inhibiting the growth of various cancer cells and selectively inhibiting the growth of MCF-7 breast cancer cells (GI50: 0.56 μM).

DiMNF (3',4'-Dimethoxy-αNF) is a selective and potent modulator of the aryl hydrocarbon receptor (AHR) and an AHR ligand with anti-inflammatory activity that inhibits cytokine-mediated induction of complement factor genes.

AHR antagonist 5 free base is an orally active AHR antagonist with IC50 of approximately 35-150 nM in human and rodent cell lines, and exhibits anticancer activity.

KYN-101 is an orally active and selective aryl hydrocarbon receptor (AHR) inhibitor with anticancer activity. KYN-101 decreases CYP1A1 mRNA expression and can be used in the study of breast cancer and acute myeloid leukemia. KYN-101 is an orally active and selective aryl hydrocarbon receptor (AHR) inhibitor with anticancer activity.

AHR Inhibitor I-103 is an aryl hydrocarbon receptor (AHR) inhibitor with anticancer activity used in the study of breast cancer and acute myeloid leukemia.

3-Hydroxykynurenamine, also known as 3-Hydroxy-L-kynurenamine or 3-HKA, is a biogenic amine produced via an alternative pathway of tryptophan metabolism. In vitro, 3-HKA has an anti-inflammatory profile by inhibiting the IFN-γ mediated STAT1/NF-κΒ pathway in both mouse and human dendritic cells (DCs) with a consequent decrease in the release of pro-inflammatory chemokines and cytokines, most notably TNF, IL-6, and IL12p70. 3-HKA has protective effects in an experimental mouse model of psoriasis by decreasing skin thickness, erythema, scaling and fissuring, reducing TNF, IL-1β, IFN-γ, and IL-17 production, and inhibiting generation of effector CD8+ T cells. Similarly, in a mouse model of nephrotoxic nephritis, besides reducing inflammatory cytokines, 3-HKA improves proteinuria and serum urea nitrogen, overall ameliorating immune-mediated glomerulonephritis and renal dysfunction.This compound is unstable in powder form and other related salt forms are recommended.

Benzyl butyl phthalate (1,2-benzenedicarboxylic acid) is used as a plasticizer for PVC.

Diosmin (Venosmine) is a bioflavonoid that strengthens vascular walls.

Prochloraz (Prelude) is a broad-spectrum contact imidazole fungicide. Prochloraz inhibits human placental microsomal aromatase in vitro (IC50 = 40 nM). Prochloraz also acts as an estrogen receptor (IC50s = 25 μM) and androgen receptor (IC50 = 4 μM) antagonist, and activates aryl hydrocarbon receptors (EC50 = 1 μM).

Carbidopa monohydrate (S(-)-Carbidopa) is an inhibitor of DOPA decarboxylase, preventing the conversion of levodopa to dopamine.

Indole-3-carbinol (I3C), a naturally occurring, orally available cleavage product of the glucosinolate glucobrassicanin, inhibits NF-κB and IκBα kinase activation.

Carbidopa (Lodosyn) is an aromatic-L-amino-acid decarboxylase inhibitor (IC50: 29±2 μM). It is used in PARKINSON DISEASE to reduce peripheral adverse effects of LEVODOPA.

5,6-Benzoflavone (β-Naphthoflavone) is an exogenous ligand for the aryl hydrocarbon receptor, which disrupts zinc homeostasis in human hepatocellular carcinoma HepG2 cells. 5,6-Benzoflavone (β-Naphthoflavone) possesses anti-inflammatory and antioxidant activities, inhibits LPS-induced inflammation through the AKT/Nrf-2/HO-1-NF-kappaB signaling axis, inhibits TNF-α-induced ICAM-1 and VCAM-1 expression, which can be used to study neurodegenerative diseases.

2-Mercaptobenzothiazole (Captax) is an organosulfur compound. 2-Mercaptobenzothiazole is used in rubber vulcanization.

1,4-Chrysenequinone (Chrysene-1,4-dione) is an activator of aryl hydrocarbon receptor (AhR).

BAY 2416964 is a small molecule inhibitor that selectively targets aromatic receptor (AhR) with an IC50 of 341 nM and is commonly used in cancer immunotherapy research.

AHR antagonist 5 is a potent and orally active aryl hydrocarbon receptor (AHR) antagonist(example 39; IC50 < 0.5 μΜ). It significantly inhibits tumor growth combined with checkpoint inhibitor anti-PD-1.

AhR modulator-1 is a selective and orally active aryl hydrocarbon receptor (AhR) modulator. It inhibits metastasis, in part, by inhibiting prostatic VEGF production prior to tumor formation. It also possesses anti-estrogenic properties in rat uterus.