Aryl Hydrocarbon Receptor (AhR or AHR or ahr or ahR) is a protein that in humans is encoded by the AHR gene. The aryl hydrocarbon receptor is a ligand-activated transcription factor involved in the regulation of biological responses to planar aromatic (aryl) hydrocarbons, and regulates xenobiotic-metabolizing enzymes such as cytochrome P450s, most notably cyp 1A1. Aryl Hydrocarbon Receptor is a member of the family of basic helix-loop-helix transcription factors. AhR binds several exogenous ligands including natural plant flavonoids, polyphenolics and indoles, as well as synthetic polycyclic aromatic hydrocarbons and dioxin-like compounds. AhR is a cytosolic transcription factor that is normally inactive, binding to several co-chaperones. Upon ligand binding to chemicals such as 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD), the chaperones dissociate resulting in AhR translocating into the nucleus and dimerizing with ARNT (AhR nuclear translocator), leading to changes in gene transcription.


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Diosmin

Diosmin is a flavonoid found in a variety of citrus fruits and also an agonist of the aryl hydrocarbon receptor (AhR).

  • CAS Number: 520-27-4
  • MF: C28H32O15
  • MW: 608.545
  • Catalog: Aryl Hydrocarbon Receptor
  • Density: 1.7±0.1 g/cm3
  • Boiling Point: 926.8±65.0 °C at 760 mmHg
  • Melting Point: 277-278°C
  • Flash Point: 305.2±27.8 °C

Mivotilate

Mivotilate is a nontoxic, potent activator of the aryl hydrocarbon receptor (AhR), and acts as a hepatoprotective agent.

  • CAS Number: 130112-42-4
  • MF: C12H14N2O3S3
  • MW: 330.44600
  • Catalog: Aryl Hydrocarbon Receptor
  • Density: 1.467g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

AHR antagonist 5 free base

AHR antagonist 5 free base is a selective and orally active aryl hydrocarbon receptor (AHR) inhibitor. AHR antagonist 5 free base effectively blocks AHR from translocating from the cytoplasm to the nucleus. AHR antagonist 5 free base is highly selective for AHR over other receptors, transporters, and kinases[1].

  • CAS Number: 2247950-42-9
  • MF: C25H24FN7
  • MW: 441.50
  • Catalog: Aryl Hydrocarbon Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

10-Cl-BBQ

10-Cl-BBQ is a high affinity AhR ligand with immunosuppressive activity. 10-Cl-BBQ promotes cytosol to nuclear translocation of AhR and activates the AhR-regulated reporter gene at nanomolar concentrations[1][2].

  • CAS Number: 23982-76-5
  • MF: C18H9ClN2O
  • MW: 304.73
  • Catalog: Aryl Hydrocarbon Receptor
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 636.8±47.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 338.9±29.3 °C

D-kynurenine

D-kynurenine, a metabolite of D-tryptophan, can serve as the bioprecursor of kynurenic acid (KYNA) and 3-hydroxykynurenine. D-Kynurenine is an agonist for G protein-coupled receptor, GPR109B. D-Kynurenine is a substrate in a fluorometric assay of D-amino acid oxidase. D-kynurenine promotes epithelial-to-mesenchymal transition via activating aryl hydrocarbon receptor (AHR)[1][2][3][4].

  • CAS Number: 13441-51-5
  • MF: C10H12N2O3
  • MW: 208.214
  • Catalog: Aryl Hydrocarbon Receptor
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 466.6±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 236.0±28.7 °C

L-Kynurenine

L-Kynurenine is a metabolite of the amino acid L-tryptophan. L-Kynurenine is an aryl hydrocarbon receptor agonist.

  • CAS Number: 2922-83-0
  • MF: C10H12N2O3
  • MW: 208.214
  • Catalog: Aryl Hydrocarbon Receptor
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 466.6±45.0 °C at 760 mmHg
  • Melting Point: 302.49° C
  • Flash Point: 236.0±28.7 °C

CAY 10465

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).

  • CAS Number: 688348-33-6
  • MF: C15H9Cl2F3
  • MW: 317.133
  • Catalog: Aryl Hydrocarbon Receptor
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 361.2±42.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 201.8±21.3 °C

3,4,5-trihydroxy-6-methylphthalaldehyde

Flavipin is an aryl hydrocarbon receptor (Ahr) agonist that induces the expression of Ahr downstream genes in mouse CD4+ T cells and CD11b+ macrophages. Flavipin inhibits the stabilizing function of Arid5a on Il23a 3′UTR, a newly identified target mRNA[1]. Flavipin exhibits the DPPH free radical scavenging ability with IC50 value of 7.2 μM, and has potent α-glucosidase inhibition with IC50 value of 33.8 μM[2].

  • CAS Number: 483-53-4
  • MF: C9H8O5
  • MW: 196.15700
  • Catalog: Aryl Hydrocarbon Receptor
  • Density: 1.577g/cm3
  • Boiling Point: 353.7ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 181.9ºC

Indolokine A4

Indolokine A4, a catabolite of indole-3-pyruvate (I3P), is a potent AhR agonist[1].

  • CAS Number: 1809317-07-4
  • MF: C13H10N2O3S
  • MW: 274.30
  • Catalog: Aryl Hydrocarbon Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Indole-3-pyrubate

Indole-3-pyruvic acid, a keto analogue of tryptophan, is an orally active AHR agonist. Indole-3-pyruvic acid has antioxidant properties, and can be used in the research of inflammation, anxiety[1][2][3].

  • CAS Number: 392-12-1
  • MF: C11H9NO3
  • MW: 203.194
  • Catalog: Aryl Hydrocarbon Receptor
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 445.2±28.0 °C at 760 mmHg
  • Melting Point: 215 °C (dec.)(lit.)
  • Flash Point: 223.0±24.0 °C

1,4-Chrysenequinone

1,4-Chrysenequinone, a polycyclic aromatic quinone, acts as an activator of aryl hydrocarbon receptor (AhR).

  • CAS Number: 100900-16-1
  • MF: C18H10O2
  • MW: 258.271
  • Catalog: Aryl Hydrocarbon Receptor
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 499.5±45.0 °C at 760 mmHg
  • Melting Point: 210-212ºC(lit.)
  • Flash Point: 184.7±25.7 °C

-Trimethoxyflavone

6,2',4'-Trimethoxyflavone is a potent aryl hydrocarbon receptor (AHR) antagonist. 6,2',4'-Trimethoxyflavone represses AHR-mediated gene induction[1].

  • CAS Number: 720675-74-1
  • MF: C18H16O5
  • MW: 312.317
  • Catalog: Aryl Hydrocarbon Receptor
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 495.2±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 220.3±28.8 °C

FICZ

FICZ is a potent aryl hydrocarbon receptor (AhR) agonist with a Kd of 70 pM.

  • CAS Number: 172922-91-7
  • MF: C19H12N2O
  • MW: 284.31
  • Catalog: Aryl Hydrocarbon Receptor
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 463.8±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 191.1±34.1 °C

StemRegenin 1 (SR1)

StemRegenin 1 is a potent aryl hydrocarbon receptor (AhR) antagonist with IC50 of 127 nM.

  • CAS Number: 1227633-49-9
  • MF: C24H23N5OS
  • MW: 429.537
  • Catalog: Aryl Hydrocarbon Receptor
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 622.9±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 330.5±34.3 °C

7H-Benzimidazo[2,1-a]benzo[de]isoquinolin-7-one

AHR agonist 3 is an aryl hydrocarbon receptor (AhR) agonist, that can induces cell cycle arrest or apoptosis via activation of tumor-suppressive transcriptional programs. AHR agonist 3 inhibits triple-negative breast cancer (TNBC) stem cell growth via AhR while exhibits minimal cytotoxicity against normal human primary cells and can be used for cancer research[1].

  • CAS Number: 23749-58-8
  • MF: C18H10N2O
  • MW: 270.28
  • Catalog: Apoptosis
  • Density: 1.4g/cm3
  • Boiling Point: 613.6ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 324.9ºC

AhR modulator-1

AhR modulator-1 (compound 6-MCDF) is a selective and orally active aryl hydrocarbon receptor (AhR) modulator. AhR modulator-1 inhibits metastasis, in part, by inhibiting prostatic VEGF production prior to tumor formation. AhR modulator-1 also possess anti-estrogenic properties in rat uterus[1].

  • CAS Number: 115039-00-4
  • MF: C13H7Cl3O
  • MW: 285.55
  • Catalog: Aryl Hydrocarbon Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

3-Hydroxykynurenamine

3-Hydroxykynurenamine, also known as 3-Hydroxy-L-kynurenamine or 3-HKA, is a biogenic amine produced via an alternative pathway of tryptophan metabolism. In vitro, 3-HKA has an anti-inflammatory profile by inhibiting the IFN-γ mediated STAT1/NF-κΒ pathway in both mouse and human dendritic cells (DCs) with a consequent decrease in the release of pro-inflammatory chemokines and cytokines, most notably TNF, IL-6, and IL12p70. 3-HKA has protective effects in an experimental mouse model of psoriasis by decreasing skin thickness, erythema, scaling and fissuring, reducing TNF, IL-1β, IFN-γ, and IL-17 production, and inhibiting generation of effector CD8+ T cells. Similarly, in a mouse model of nephrotoxic nephritis, besides reducing inflammatory cytokines, 3-HKA improves proteinuria and serum urea nitrogen, overall ameliorating immune-mediated glomerulonephritis and renal dysfunction.

  • CAS Number: 99362-47-7
  • MF: C9H12N2O
  • MW: 180.21
  • Catalog: Aryl Hydrocarbon Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

GNF351

GNF351 is a full aryl hydrocarbon receptor (AHR) antagonist. GNF351 competes with a photoaffinity AHR ligand for binding to the AHR with an IC50 of 62 nM. GNF351 is minimal toxicity in mouse or human keratinocytes[1].

  • CAS Number: 1227634-69-6
  • MF: C24H25N7
  • MW: 411.50
  • Catalog: Aryl Hydrocarbon Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

5F 203

5F-203 (NSC-703786) is a cytotoxic molecule that forms DNA adducts and cell cycle arrest. 5F-203 induces aryl hydrocarbon receptor (AhR) signaling and elevates expression of CYP1A1. 5F-203 also increases the levels of reactive oxygen species as well as activates JNK, ERK, and p38[1][2][3].

  • CAS Number: 260443-89-8
  • MF: C14H11FN2S
  • MW: 258.31400
  • Catalog: Aryl Hydrocarbon Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

BAY 2416964

AHR antagonist 3 is a 2-heteroaryl-3-oxo-2,3-dihydropyridazine-4-carboxamide compound and an aryl hydrocarbon receptor (AHR) antagonist extracted from patent WO2018146010A1, example 192, has an IC50 of 341 nM. AHR antagonist 3 has anti-cancer effects[1].

  • CAS Number: 2242464-44-2
  • MF: C18H18ClN5O3
  • MW: 387.82
  • Catalog: Aryl Hydrocarbon Receptor
  • Density: 1.42±0.1 g/cm3(Predicted)
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Brevifolincarboxylic acid

Brevifolincarboxylic acid is extracted from Polygonum capitatum[1], has inhibitory effect on the aryl hydrocarbon receptor (AhR)[2]. Brevifolincarboxylic acid is an α-glucosidase inhibitor with an IC50 of 323.46 μM[3].

  • CAS Number: 18490-95-4
  • MF: C13H8O8
  • MW: 292.198
  • Catalog: Aryl Hydrocarbon Receptor
  • Density: 2.0±0.1 g/cm3
  • Boiling Point: 758.5±60.0 °C at 760 mmHg
  • Melting Point: 250 °C
  • Flash Point: 296.2±26.4 °C

3',4'-dimethoxyflavone

3',4'-Dimethoxyflavone is a lipophilic flavone, can be isolated from the leaves of Primula veris. 3',4'-Dimethoxyflavone can reduce the synthesis and accumulation of PARP and protect cortical neurones against cell death induced by Parthanatos. 3',4'-Dimethoxyflavone is also an aryl hydrocarbon receptor antagonist in human breast cancer cells. 3',4'-Dimethoxyflavone can promote the proliferation of human hematopoietic stem cells. 3',4'-Dimethoxyflavone has various biological activities, including antioxidant, anti-cancer, anti-inflammatory, anti-atherogenic, hypolipidaemic, and neuroprotective or neurotrophic effects[1][2][3][4].

  • CAS Number: 4143-62-8
  • MF: C17H14O4
  • MW: 282.29100
  • Catalog: PARP
  • Density: 1.242g/cm3
  • Boiling Point: 428.5ºC at 760 mmHg
  • Melting Point: 154-155°C
  • Flash Point: 190.6ºC

3-Methylindole

Skatole is produced by intestinal bacteria, regulates intestinal epithelial cellular functions through activating aryl hydrocarbon receptors and p38[1].

  • CAS Number: 83-34-1
  • MF: C9H9N
  • MW: 131.17
  • Catalog: Dopamine Receptor
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 265.1±9.0 °C at 760 mmHg
  • Melting Point: 92-97 °C(lit.)
  • Flash Point: 112.5±11.3 °C

AHR antagonist 5

AHR antagonist 5, a potent and orally active aryl hydrocarbon receptor (AHR) antagonist extracted from patent WO2018195397, example 39, has an IC50 of < 0.5 µΜ. AHR antagonist 5 significantly inhibits tumor growth combined with checkpoint inhibitor anti-PD-1[1].

  • CAS Number: 2247953-39-3
  • MF: C25H27Cl3FN7
  • MW: 550.89
  • Catalog: Aryl Hydrocarbon Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Indolokine A5

Indolokine A5, a catabolite of L-cysteine, is a potent AhR agonist[1].

  • CAS Number: 951207-88-8
  • MF: C13H8N2O3S
  • MW: 272.28
  • Catalog: Aryl Hydrocarbon Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Dibenz[a,i]pyrene

Dibenzo(a,i)pyrene is a 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) receptor ligand[1].

  • CAS Number: 189-55-9
  • MF: C24H14
  • MW: 302.37
  • Catalog: Aryl Hydrocarbon Receptor
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 552.3±17.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 282.0±15.1 °C

CHD-5

CHD-5 is a potent AhR (aryl hydrocarbon receptor) antagonist[1].

  • CAS Number: 289494-16-2
  • MF: C19H17N3O2
  • MW: 319.357
  • Catalog: Aryl Hydrocarbon Receptor
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 426.9±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 212.0±28.7 °C

Benzyl butyl phthalate-d4

Benzyl butyl phthalate-d4 is the deuterium labeled Benzyl butyl phthalate[1]. Benzyl butyl phthalate, a member of phthalic acid esters (PAEs), can trigger the migration and invasion of hemangioma (HA) cells via upregulation of Zeb1. Benzyl butyl phthalate activates aryl hydrocarbon receptor (AhR) in breast cancer cells to stimulate SPHK1/S1P/S1PR3 signaling and enhances formation of metastasis-initiating breast cancer stem cells (BCSCs)[2][3][4].

  • CAS Number: 93951-88-3
  • MF: C19H16D4O4
  • MW: 316.38400
  • Catalog: Aryl Hydrocarbon Receptor
  • Density: 1.114 g/mL at 25ºC
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: 113ºC

Carbidopa monohydrate

Carbidopa ((S)-(-)-Carbidopa) monohydrate, a peripheral decarboxylase inhibitor, can be used for the research of Parkinson's disease. Carbidopa monohydrate is a selective aryl hydrocarbon receptor (AhR) modulator. Carbidopa monohydrate inhibits pancreatic cancer cell and tumor growth[1][2].

  • CAS Number: 38821-49-7
  • MF: C10H16N2O5
  • MW: 244.244
  • Catalog: Aryl Hydrocarbon Receptor
  • Density: 1.42 g/cm3
  • Boiling Point: 528.7ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 273.5ºC

L -Kynurenine sulfate salt

L-Kynurenine sulfate, an aryl hydrocarbon receptor (AHR) agonist that activates AHR-directed, naive T cell polarization to the anti-inflammatory Treg phenotype[1].

  • CAS Number: 16055-80-4
  • MF: C10H14N2O7S
  • MW: 306.29200
  • Catalog: Aryl Hydrocarbon Receptor
  • Density: N/A
  • Boiling Point: 466.6ºC at 760 mmHg
  • Melting Point: 196 °C
  • Flash Point: 236ºC