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.

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.

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

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.

VAF347 is a cell-permeable and highly affinity agonist of the aryl hydrocarbon receptor (AhR) with anti-inflammatory effects.

GNF351 is a full antagonist of the aryl hydrocarbon receptor (AHR)with the capacity to inhibit both DRE-dependent and -independent activity. GNF351 is minimal toxicity in mouse or human keratinocytes. GNF351 competes with a photoaffinity AHR ligand for binding to the AHR (IC50: 62 nM).

StemRegenin 1 (SR1) is an aryl hydrocarbon receptor (AhR) inhibitor.

YL-109, a novel anticancer agent, can inhibit breast Y cell growth and invasiveness in vitro and in vivo.

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

PDM 2 is a potent and selective aryl hydrocarbon receptor (AhR) antagonist.

Tapinarof (Benvitimod) is targeted as a topical cream treatment for psoriasis, a chronic autoimmune skin disease.

L-Kynurenine ((S)-Kynurenine) is an endogenous agonist of the tryptophan metabolite and the aromatic hydrocarbon receptor (AHR). L-Kynurenine can inhibit the proliferation of allogeneic T cells and increase the invasion of malignant U87 glioma cells into the collagen matrix.