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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.

  • AHR antagonist 5 free base
    T397622247950-42-9In house
    AHR antagonist 5 free base is an orally active antagonist of AHR with IC50s of ~35-150 nM in human and rodent cell lines.
    • $155
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    TargetMol | Inhibitor Hot
  • Diosmin
    T0878520-27-4
    Diosmin (Venosmine) is a bioflavonoid that strengthens vascular walls.
    • $45
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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.
    • $29
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  • Benzyl butyl phthalate
    T064085-68-7
    Benzyl butyl phthalate (1,2-benzenedicarboxylic acid) is used as a plasticizer for PVC.
    • $40
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    TargetMol | Citations Cited
  • 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.
    • $49
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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.
    • $35
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    TargetMol | Citations Cited
  • StemRegenin 1
    T18311227633-49-9
    StemRegenin 1 (SR1) is an aryl hydrocarbon receptor (AhR) inhibitor.
    • $32
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    TargetMol | Citations Cited
  • Tapinarof
    T464479338-84-4
    Tapinarof (Benvitimod) is targeted as a topical cream treatment for psoriasis, a chronic autoimmune skin disease.
    • $34
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    TargetMol | Citations Cited
  • 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.
    • $34
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    TargetMol | Citations Cited
  • CH-223191
    T2448301326-22-7
    CH-223191 is a potent and specific antagonist for aryl hydrocarbon receptor (AhR).
    • $56
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    TargetMol | Citations Cited
  • Pifithrin-α hydrobromide
    T270763208-82-2
    Pifithrin-α hydrobromide (Pifithrin-α hydrobromide) is a p53 inhibitor, inhibiting p53-dependent transactivation of p53-responsive genes.
    • $33
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    TargetMol | Citations Cited
  • YL-109
    T196036341-25-0
    YL-109, a novel anticancer agent, can inhibit breast Y cell growth and invasiveness in vitro and in vivo.
    • $30
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    TargetMol | Inhibitor Sale
  • Carbidopa monohydrate
    T214838821-49-7
    Carbidopa monohydrate (S(-)-Carbidopa) is an inhibitor of DOPA decarboxylase, preventing the conversion of levodopa to dopamine.
    • $38
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  • BAY 2416964
    T102702242464-44-2
    BAY 2416964 is a potent and orally active aryl hydrocarbon receptor (AHR) antagonist(example 192, IC50: 341 nM). It has the potential for cancer treatment.
    • $48
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  • VAF347
    T13276574759-62-9
    VAF347 is a cell-permeable and highly affinity agonist of the aryl hydrocarbon receptor (AhR) with anti-inflammatory effects.
    • $34
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  • SGA360
    T8980680611-86-3
    SGA360 is a selective aryl hydrocarbon (Ah) receptor modulator. It exhibits anti-inflammatory properties.
    • $39
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  • MeBIO
    T21966667463-95-8
    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.
    • $33
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  • ITE
    T7202448906-42-1
    ITE is a potent endogenous agonist of aryl hydrocarbon receptor (AhR) (Ki : 3 nM), has immunosuppressive activity.
    • $34
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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.
    • $77
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  • CAY 10465
    T4607688348-33-6
    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).
    • $30
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  • BAY-218
    T56222162982-11-6
    BAY-218 (AHR antagonist 1) is an aryl hydrocarbon receptor (AHR) antagonist , has an IC50 of 39.9 nM in human cell line.
    • $34
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  • AHR agonist 4
    T79436
    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].
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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).
    • $37
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  • PDM2
    T4608688348-25-6
    PDM 2 is a potent and selective aryl hydrocarbon receptor (AhR) antagonist.
    • $42
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  • L-Kynurenine
    T49282922-83-0
    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.
    • $30
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  • Skatole
    T528183-34-1
    Skatole (3-Methyl-1H-indole) is produced by intestinal bacteria. Skatole regulates intestinal epithelial cellular functions through activating aryl hydrocarbon receptors and p38.
    • $29
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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).
    • $47
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