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Immunology/Inflammation

Aryl Hydrocarbon Receptor

Immunology/Inflammation related

NOD-like Receptor (NLR)

Prostaglandin Receptor

Reactive Oxygen Species

Thrombopoietin Receptor

Aryl Hydrocarbon Receptor

The aryl hydrocarbon receptor (also known as AhR, AHR, ahr, ahR, or dioxin receptor) is a protein that in humans is encoded by the AHR gene. The aryl hydrocarbon receptor is a transcription factor that regulates gene expression. It was originally thought to function primarily as a sensor of xenobiotic chemicals and also as the regulator of enzymes such as cytochrome P450s that metabolize these chemicals. The most notable of these xenobiotic chemicals are aromatic (aryl) hydrocarbons from which the receptor derives its name. More recently, it has been discovered that AhR is activated (or deactivated) by a number of endogenous indole derivatives such as kynurenine. In addition to regulating metabolism enzymes, the AhR has roles in regulating immunity, stem cell maintenance, and cellular differentiation.

Filter HomeSignaling PathwaysImmunology/InflammationAryl Hydrocarbon Receptor

CH-223191

T2448301326-22-7

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.

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BAY-218

T56222162982-11-6

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.

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L-Kynurenine

T49282922-83-0

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.

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FICZ

TQ0257172922-91-7

FICZ (6-Formylindolo[3,2-b]carbazole) is a potent aryl agonist for the hydrocarbon receptor (AhR, Kd: 70 pM).

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Tapinarof

T464479338-84-4

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

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Pifithrin-α hydrobromide

T270763208-82-2

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

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PD98059

T2623167869-21-8

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.

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StemRegenin 1

T18311227633-49-9

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

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ITE

T7202448906-42-1

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

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26-Deoxyactein

TN1222264624-38-6

23-epi-26-Deoxyactein (27-Deoxyactein) has anti-inflammatory activity, it inhibits nitric oxide production by reducing iNOS expression without affecting activity of the enzyme. It also has anti-cancer activity, it can inhibit growth of the MCF7 human breast cancer cells and induce cell cycle arrest at G1.

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Indole-3-pyruvic acid

T4939392-12-1

Indole-3-pyruvic acid (3-(3-Indolyl)-2-oxopropanoic acid) is a compound involved in the biosynthesis of Indole-3-acetic acid, a plant hormone which plays important roles in regulating growth and responses to environmental changes.

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Brevifolincarboxylic acid

TN145118490-95-4

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.

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Diosmin

T0878520-27-4

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

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AHR antagonist 2

T102692338747-54-7In house

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.

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Carbidopa

T679528860-95-9

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.

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GNF351

T154101227634-69-6

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).

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BAY 2416964

T102702242464-44-2

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.

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Prochloraz

T2062567747-09-5

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).

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AHR antagonist 5 free base

T397622247950-42-9In house

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.

$155

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Indole-3-carbinol

T2947700-06-1

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

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L-Kynurenine-d4

TMID-00712672568-86-2

L-Kynurenine-d4 is a deuterated compound of L-Kynurenine. L-Kynurenine has a CAS number of 2922-83-0. L-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.

$265

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alpha-Naphthoflavone

T2O2744604-59-1

alpha-Naphthoflavone (7,8-benzoflavone), a synthetic flavonoid, is a potent inhibitor of aromatase with an I50 value of 0.5 μM.

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WAY-605471

T9822378223-81-5

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

$117

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KYN-101

T720562247950-73-6In house

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.

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