AhR

Bindarit (AF2838)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.

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

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

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.

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), a key regulator of immune-inflammatory conditions. A metabolite of tryptophan derived from dietary protein, it is produced by intestinal bacteria and metabolized in the liver. In chronic kidney disease patients with impaired renal function, it accumulates in serum as a uremic toxin, inducing oxidative stress and accelerating disease progression. At 250 μM, it activates NF-Κb, promoting TGF-β1 and Smad3 expression in rat proximal tubular cells, which is associated with profibrotic activity.

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

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

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

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

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.

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

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).

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.

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).

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

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

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

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 Inhibitor I-103 is an aryl hydrocarbon receptor (AHR) inhibitor with anticancer activity 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. 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.

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

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.