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.

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

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.

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).

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

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

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

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

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.

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).

β-NF-JQ1 is a PROTAC that recruits aryl hydrocarbon receptor E3 (AhR E3) ligase to target proteins. Using β-NF as an AhR ligand, it targets bromodomain (BRD)-containing proteins and induces AhR and BRD protein interactions. β-NF-JQ1 exhibits potent anticancer activity associated with protein knockdown activity.

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

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.

Pifithrin-β hydrobromide (Cyclic PFT-α) is an inhibitor of p53; reversibly blocks p53-dependent transcriptional activation and apoptosis. Protects against neuronal death in models of stroke and neurodegenerative disorders. Active in vivo; protects mice from the side-effects of Y therapy associated with p53 induction. Supresses self-renewal of embryonic stem cells. Also aryl hydrocarbon receptor (AHR) agonist, causes upregulation of AHR target gene CYP1A1 (EC50 = 1.1 μM).

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

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

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.

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

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

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.

3',4'-Dimethoxyflavone is a standard flavonoid compound with numerous medicinal activities.

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

MeBIO is an agonist of aryl hydrocarbon receptor, with IC50 of 44 and 55 μM for GSK-3 and CDK1/CyclinB, respectively. MeBIO does not affect GSK-3β.

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

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).

Flavipin, an aryl hydrocarbon receptor (Ahr) agonist, activates Ahr downstream gene expression in mouse CD4+ T cells and CD11b+ macrophages. This compound disrupts the stabilizing effect of Arid5a on the newly identified target mRNA, Il23a 3′UTR. Additionally, Flavipin demonstrates significant antioxidant properties, evidenced by its DPPH free radical scavenging capability with an IC50 value of 7.2 μM, and exhibits potent α-glucosidase inhibitory activity with an IC50 value of 33.8 μM.

DiMNF is a selective aryl hydrocarbon receptor (AHR) modulator. It also suppresses the expression of CD55 and CD46 induced by IL-1β in an inflammatory tumor cell microenvironment.

1,2,3,6,7,8-Hexachlorodibenzo-p-dioxin, a polychlorinated dibenzodioxin (PCDD), acts as an agonist for the aryl hydrocarbon receptor (AhR; EC50s = 5.4 and 9.3 nM at 4 and 8 h, respectively, in a reporter assay). It has been observed to reduce antibody production against sheep red blood cells in mice at doses of 0.5 and 2 µg/kg. This compound has been detected in animal feed and in the vicinity of municipal waste incinerators.

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

L-Kynurenine sulfate, an aryl hydrocarbon receptor (AHR) agonist, activates AHR-driven polarization of naive T cells towards the anti-inflammatory [Treg] phenotype.

Norisoboldine hydrochloride, an orally active aryl hydrocarbon receptor (AhR) agonist and a prominent isoquinoline alkaloid found in Radix Linderae, is utilized for research purposes in the study of Rheumatoid Arthritis and Ulcerative Colitis [1] [2].

MNF, also known as 3,4-MNF, is an antagonist of the aryl hydrocarbon receptor (AhR). MNF reduces UVR-mediated immunosuppression and induces Tregs in murine contact hypersensitivity (CHS).

Compound 6, an AhR agonist, selectively activates the aryl hydrocarbon receptor (AhR) with an EC50 of 0.01 nM [1].

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

AHR agonist 4 (compound 24e), as an Aryl hydrocarbon receptor (AHR) agonist, modulates the immune equilibrium between Th17/22 and Treg cells. It is a lead compound under investigation for anti-psoriasis drugs and demonstrates efficacy in mitigating imiquimod (IMQ)-induced psoriasis-like skin lesions [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.

CHD-5 is a selective antagonist of the aryl hydrocarbon receptor (AhR).

10-Cl-BBQ is a ligand of aryl hydrocarbon receptor (AhR).

Mivotilate, a potent, non-toxic aryl hydrocarbon receptor (AhR) activator, functions as a hepatoprotective agent.

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

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).

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.

Indoxyl sulfate-d5 is intended for use as an internal standard for the quantification of indoxyl sulfate by GC- or LC-MS. Indoxyl sulfate is a uremic toxin and a metabolite of tryptophan. It is formed via sulfation of indole, an intermediate generated from tryptophan by intestinal bacteria, by the sulfotransferase (SULT) isoform 1A1 variant 2 (SULT1A1*2) in the liver. Indoxyl sulfate activates the aryl hydrocarbon receptor (AhR) in HepG2 40/6 hepatoma cells (EC50 = 12.1 nM in a reporter assay). It also inhibits the organic anion transporter (OAT) isoforms OAT1 and OAT3 (Kis = 34.2 and 74.4 µM, respectively for the rat transporters) in S2 proximal tubule cells. Indoxyl sulfate (0.2 and 1 mM) increases superoxide anion and nitric oxide levels in isolated human mononuclear blood cells. It increases serum creatinine and blood urea nitrogen (BUN) levels in the 5/6 nephrectomized rat model of chronic renal failure when administered at a dose of 50 mg/kg.

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 antagonist 5 hemimaleate is a potent antagonist (IC50 < 0.5 μM) of the orally active aryl hydrocarbon receptor (AHR). aHR antagonist 5 hemimaleate in combination with the detection site inhibitor anti-PD-1 exhibited inhibitory effects on tumor growth.

AFP464 (NSC710464) free base is an active HIF-1α inhibitor (IC50: 0.25 μM) and a potent aryl hydrocarbon receptor (AhR) activator.

Indoxyl sulfate is a metabolite of tryptophan, showing adverse effects on bones and the central nervous system, having been most frequently implicated as a contributor to renal disease progression and vascular disease