AhR
Inhibitory Selectivity
AhR Products
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S3205New |
PerillaldehydePerillaldehyde (Perilladehyde, Perillal, PAE, PA), the main component of Perilla frutescens (a traditional medicinal antioxidant herb), inhibits BaP-induced AHR activation and ROS production, inhibits BaP/AHR-mediated release of the CCL2 chemokine, and activats the NRF2/HO1 antioxidant pathway. |
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| S8842 |
BAY-218BAY-218 is a potent and selective small-molecule AhR inhibitor, inhibiting AhR nuclear translocation, dioxin response element (DRE)-luciferase reporter expression and AhR-regulated target gene expression induced by both exogenous and endogenous AhR ligands. |
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| S1177 |
PD98059PD98059 is a non-ATP competitive MEK inhibitor with IC50 of 2 μM in a cell-free assay, specifically inhibits MEK-1-mediated activation of MAPK; does not directly inhibit ERK1 or ERK2. PD98059 is a ligand for the aryl hydrocarbon receptor (AHR) and functions as an AHR antagonist. |
Activation of a TLR2eERK1/2 pathway in MDDC. (C) MDDC were either untreated or treated with C. pneumoniae alone or in the presence of the ERK1/2 inhibitor PD98059 for 48 h. IL-12p70 and IL-10 release in culture media was assessed by ELISA. (D) MDDC were treated as in panel C for 48 h and then cocultured with purified allogeneic CD3t T cells. On day 12, supernatants were collected, and secreted cytokines were measured by ELISA. |
|
| S2858 |
StemRegenin 1 (SR1)StemRegenin 1 (SR1) is an aryl hydrocarbon receptor (AhR) inhibitor with IC50 of 127 nM in a cell-free assay. |
(A,B): Number of total cells and percentage CD41a+ and CD42b+ cells from day 6 + 7 cultures induced by the various cytokine cocktails. Data are mean ± SD; n = 5. *, p<.05; **, p<.01; ***, p<.001
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| S7711 |
CH-223191CH-223191 is a potent and specific aryl hydrocarbon receptor (AhR) antagonist with IC50 of 30 nM. |
Western blots for LLC cells treated for 24 h with PM2 5 or 10 μM chrysene (diluted in DMSO to make a stock solution of 10 mM) with or without 1 μM AhR inhibitor (CH-223191, diluted in DMSO to make a stock solution of 1 mM).
|
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| S6926New |
GNF351GNF351 is a potent antagonist of aryl hydrocarbon receptor (AHR). GNF351 interacts directly with the AHR ligand binding pocket and competes with a well-characterized photoaffinity AHR ligand for binding to the AHR with IC50 of 62 nM. |
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| S8995 |
BAY 2416964BAY 2416964 (compound 192) is a potent and orally active antagonist of aryl hydrocarbon receptor (AhR) with IC50 of 341 nM. BAY 2416964 has the potential in the treatment of solid tumors. |
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| S6560 |
PDM2PDM2 is a potent and selective aryl hydrocarbon receptor (AhR) antagonist. |
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| S0155 |
PDM-11PDM-11 is a derivative of resveratrol that exhibits stronger antagonist affinity for arylhydrocarbon receptors (AhR) than resveratrol, without any affinity for the estrogen receptor. |
||
| S2929 |
Pifithrin-α (PFTα) HBrPifithrin-α is an inhibitor of p53, inhibiting p53-dependent transactivation of p53-responsive genes. Pifithrin-α is also a potent agonist of the aryl hydrocarbon receptor (AhR). |
A, HAECs were per-incubated with PFTα (3 μmol/L) for 60 min followed by transfected with siB-myb or siNC in the presence of PFTα (3 μmol/L) for 7 d. The expression levels of B-myb, p-p53, p53 and p21 proteins were analysed by western blotting. GAPDH was used as a loading control. A typical group of blots is shown from one of three independent experiments. |
|
| S1247 |
Leflunomide (HWA486)Leflunomide (HWA486, RS-34821, SU101, Arava) is a pyrimidine synthesis and protein tyrosine kinase inhibitor belonging to the DMARD, used as an immunosuppressant agent. The active metabolite of Leflunomide is A77 1726, which inhibits dihydroorotate dehydrogenase (DHODH). Leflunomide is also an agonist of the AhR. |
Peritoneal macrophages were pretreated for 1 h with the leflunomide (100 umol/L), followed by treatment with 10 ug/ml rTsP53 for 6 h. Western blot analysis of P-STAT6 and STAT6 expression was performed. Corresponding staining for b-actin was carried out to control for equal loading. *P < 0.05 versus control group, #P < 0.05 versus rTsP53 group. |
|
| S9700New |
TapinarofTapinarof (GSK2894512, Benvitimod, WBI 1001, DHPS, DMVT 505) is a natural agonist of aryl hydrocarbon receptor (AhR) and induces nuclear translocation of AhR in immortalized keratinocytes (HaCaT) with EC50 of 0.16 nM. Tapinarof induces cellular apoptosis in CD4+ T cells in a dosedependent manner with IC50 of 5.2 μM. |
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| S9682New |
FICZFICZ (6-Formylindolo[3,2-b]carbazole) is a potent agonist of aryl hydrocarbon receptor (AhR) that is efficiently metabolized by AHR-regulated cytochrome P4501 enzymes. |
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| S2292 |
DiosminDiosmin is an agonist of the aryl hydrocarbon receptor (AhR). Diosmin is a semisynthetic phlebotropic agent and a flavonoid found in a variety of citrus fruits. |
||
| S0154 |
CAY10465CAY 10465 is a selective and high-affinity agonist on aryl hydrocarbon receptor (AhR) with Ki of 0.2 nM. |
||
| S9092 |
NorisoboldineNorisoboldine (Laurelliptine), a natural aryl hydrocarbon receptor (AhR) agonist, attenuates ulcerative colitis (UC) and induces the generation of Treg cells. |
||
| S5839 |
L-KynurenineL-Kynurenine ((S)-Kynurenine) is a aryl hydrocarbon receptor agonist. L-Kynurenine is a metabolite of the amino acid L-tryptophan used in the production of niacin and a central compound of the tryptophan metabolism pathway. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S3205New |
PerillaldehydePerillaldehyde (Perilladehyde, Perillal, PAE, PA), the main component of Perilla frutescens (a traditional medicinal antioxidant herb), inhibits BaP-induced AHR activation and ROS production, inhibits BaP/AHR-mediated release of the CCL2 chemokine, and activats the NRF2/HO1 antioxidant pathway. |
||
| S8842 |
BAY-218BAY-218 is a potent and selective small-molecule AhR inhibitor, inhibiting AhR nuclear translocation, dioxin response element (DRE)-luciferase reporter expression and AhR-regulated target gene expression induced by both exogenous and endogenous AhR ligands. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S1177 |
PD98059PD98059 is a non-ATP competitive MEK inhibitor with IC50 of 2 μM in a cell-free assay, specifically inhibits MEK-1-mediated activation of MAPK; does not directly inhibit ERK1 or ERK2. PD98059 is a ligand for the aryl hydrocarbon receptor (AHR) and functions as an AHR antagonist. |
Activation of a TLR2eERK1/2 pathway in MDDC. (C) MDDC were either untreated or treated with C. pneumoniae alone or in the presence of the ERK1/2 inhibitor PD98059 for 48 h. IL-12p70 and IL-10 release in culture media was assessed by ELISA. (D) MDDC were treated as in panel C for 48 h and then cocultured with purified allogeneic CD3t T cells. On day 12, supernatants were collected, and secreted cytokines were measured by ELISA. |
|
| S2858 |
StemRegenin 1 (SR1)StemRegenin 1 (SR1) is an aryl hydrocarbon receptor (AhR) inhibitor with IC50 of 127 nM in a cell-free assay. |
(A,B): Number of total cells and percentage CD41a+ and CD42b+ cells from day 6 + 7 cultures induced by the various cytokine cocktails. Data are mean ± SD; n = 5. *, p<.05; **, p<.01; ***, p<.001
|
|
| S7711 |
CH-223191CH-223191 is a potent and specific aryl hydrocarbon receptor (AhR) antagonist with IC50 of 30 nM. |
Western blots for LLC cells treated for 24 h with PM2 5 or 10 μM chrysene (diluted in DMSO to make a stock solution of 10 mM) with or without 1 μM AhR inhibitor (CH-223191, diluted in DMSO to make a stock solution of 1 mM).
|
|
| S6926New |
GNF351GNF351 is a potent antagonist of aryl hydrocarbon receptor (AHR). GNF351 interacts directly with the AHR ligand binding pocket and competes with a well-characterized photoaffinity AHR ligand for binding to the AHR with IC50 of 62 nM. |
||
| S8995 |
BAY 2416964BAY 2416964 (compound 192) is a potent and orally active antagonist of aryl hydrocarbon receptor (AhR) with IC50 of 341 nM. BAY 2416964 has the potential in the treatment of solid tumors. |
||
| S6560 |
PDM2PDM2 is a potent and selective aryl hydrocarbon receptor (AhR) antagonist. |
||
| S0155 |
PDM-11PDM-11 is a derivative of resveratrol that exhibits stronger antagonist affinity for arylhydrocarbon receptors (AhR) than resveratrol, without any affinity for the estrogen receptor. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S2929 |
Pifithrin-α (PFTα) HBrPifithrin-α is an inhibitor of p53, inhibiting p53-dependent transactivation of p53-responsive genes. Pifithrin-α is also a potent agonist of the aryl hydrocarbon receptor (AhR). |
A, HAECs were per-incubated with PFTα (3 μmol/L) for 60 min followed by transfected with siB-myb or siNC in the presence of PFTα (3 μmol/L) for 7 d. The expression levels of B-myb, p-p53, p53 and p21 proteins were analysed by western blotting. GAPDH was used as a loading control. A typical group of blots is shown from one of three independent experiments. |
|
| S1247 |
Leflunomide (HWA486)Leflunomide (HWA486, RS-34821, SU101, Arava) is a pyrimidine synthesis and protein tyrosine kinase inhibitor belonging to the DMARD, used as an immunosuppressant agent. The active metabolite of Leflunomide is A77 1726, which inhibits dihydroorotate dehydrogenase (DHODH). Leflunomide is also an agonist of the AhR. |
Peritoneal macrophages were pretreated for 1 h with the leflunomide (100 umol/L), followed by treatment with 10 ug/ml rTsP53 for 6 h. Western blot analysis of P-STAT6 and STAT6 expression was performed. Corresponding staining for b-actin was carried out to control for equal loading. *P < 0.05 versus control group, #P < 0.05 versus rTsP53 group. |
|
| S9700New |
TapinarofTapinarof (GSK2894512, Benvitimod, WBI 1001, DHPS, DMVT 505) is a natural agonist of aryl hydrocarbon receptor (AhR) and induces nuclear translocation of AhR in immortalized keratinocytes (HaCaT) with EC50 of 0.16 nM. Tapinarof induces cellular apoptosis in CD4+ T cells in a dosedependent manner with IC50 of 5.2 μM. |
||
| S9682New |
FICZFICZ (6-Formylindolo[3,2-b]carbazole) is a potent agonist of aryl hydrocarbon receptor (AhR) that is efficiently metabolized by AHR-regulated cytochrome P4501 enzymes. |
||
| S2292 |
DiosminDiosmin is an agonist of the aryl hydrocarbon receptor (AhR). Diosmin is a semisynthetic phlebotropic agent and a flavonoid found in a variety of citrus fruits. |
||
| S0154 |
CAY10465CAY 10465 is a selective and high-affinity agonist on aryl hydrocarbon receptor (AhR) with Ki of 0.2 nM. |
||
| S9092 |
NorisoboldineNorisoboldine (Laurelliptine), a natural aryl hydrocarbon receptor (AhR) agonist, attenuates ulcerative colitis (UC) and induces the generation of Treg cells. |
||
| S5839 |
L-KynurenineL-Kynurenine ((S)-Kynurenine) is a aryl hydrocarbon receptor agonist. L-Kynurenine is a metabolite of the amino acid L-tryptophan used in the production of niacin and a central compound of the tryptophan metabolism pathway. |
