AhR

Nimodipine (BAY-e 9736), a 1, 4-dihydropyridine calcium channel blocker, acts primarily on vascular smooth muscle cells.

WAY-605471 is a AHR antagonist with IC50 of 0.5 - 1 μM.

Phortress (NSC-710305) is a potent AhR ligand with strong binding affinity, which subsequently triggers the transcription of CYP1A1 and induces antitumor activity.

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

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

CH-223191 is a potent and specific antagonist for aryl hydrocarbon receptor (AhR).

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

CAY10464 (AHR antagonist 7) is a potent AHR antagonist with potential antitumor activity that inhibits CYP1A1 mRNA expression and may be used to study cancer and metabolic diseases.

PDM11 (1-[2-(4-Chloro-phenyl)-vinyl]-3,5-diMeth) is an antagonist of aryl hydrocarbon receptor (AhR)

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

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).

ITE is a potent endogenous agonist of aryl hydrocarbon receptor (AhR) (Ki : 3 nM), has immunosuppressive activity.

D-Kynurenine (ZINC901103) is a metabolite of D-tryptophan and an agonist of GPR109B. D-Kynurenine activates AhR and promotes the conversion of the epithelium to mesenchyme. D-Kynurenine serves as a substrate in the fluorescence analysis of D-amino acid oxidase.

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

BAY-218 (AHR antagonist 1) is an aryl hydrocarbon receptor (AHR) antagonist , has an IC50 of 39.9 nM in human cell line.

Brevifolincarboxylic acid is a natural product isolated from Polygonum capitatum, it has inhibitory effect on the aryl hydrocarbon receptor (AhR). Brevifolincarboxylic acid is an α-glucosidase inhibitor with an IC50 of 323.46 μM.

(-)-Perillaldehyde shows antibacterial activity.

Skatole (3-Methyl-1H-indole) is produced by intestinal bacteria. Skatole regulates intestinal epithelial cellular functions through activating aryl hydrocarbon receptors and p38.

L-Kynurenine ((S)-Kynurenine) is a key intermediate in the breakdown pathway of tryptophan. L-Kynurenine is a substrate of kynureninase, KMO, and KAT associated with the suppression of antitumor immune responses. It has been shown to inhibit allogeneic T-cell proliferation and to increase malignant U87 glioma cell invasion into a collagen matrix.

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

Leflunomide (HWA486) is an immunomodulatory agent used in the therapy of rheumatoid arthritis and psoriatic arthritis.

Potassium 1H-indol-3-yl sulfate (Potassium 3-indoxyl sulfate) is an agonist for the human Aryl Hydrocarbon Receptor (AhR). The Aryl Hydrocarbon Receptor (AhR) has recently emerged as a pathophysiological regulator of immune-inflammatory conditions and potassium 1H-indol-3-yl sulfate has been shown to be a ligand for AhR. Potassium 1H-indol-3-yl sulfate is also a metabolite of tryptophan derived from dietary protein. Tryptophan is metabolized by intestinal bacteria into indole, which is absorbed into the blood and then further metabolized to indoxyl sulfate in the liver, which is normally excreted in urine. In chronic kidney disease patients where renal function is compromised, potassium 1H-indol-3-yl sulfate can accumulate in serum as a uremic toxin, inducing oxidative stress and accelerating progression of the disease. Potassium 1H-indol-3-yl sulfate at 250 μM can induce the activation of NF-Κb, promoting the expression of both TGF-β1 and Smad3 expression in proximal tubular cells of rats, which is associated with profibrotic activity.

Mexiletine hydrochloride (KOE-1173 hydrochloride) is a voltage-gated sodium channel blocker and a Class IB antiarrhythmic drug. Mexiletine hydrochloride exerts antiarrhythmic effects by inhibiting sodium current in myocardial cells, thereby reducing the rise rate of cardiac action potential (phase 0) and reducing the automaticity of Purkinje fibers.