AhR
Inhibitory Selectivity
AhR Products
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| 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. |
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| S2858 |
StemRegenin 1 (SR1)StemRegenin 1 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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| S8995New |
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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| S6560New |
PDM2PDM2 is a potent and selective aryl hydrocarbon receptor (AhR) antagonist. |
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| 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. |
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| S0154New |
CAY10465CAY 10465 is a selective and high-affinity agonist on aryl hydrocarbon receptor (AhR) with Ki of 0.2 nM. |
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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. |
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| S9092 |
NorisoboldineNorisoboldine, a natural aryl hydrocarbon receptor (AhR) agonist, attenuates ulcerative colitis (UC) and induces the generation of Treg cells. |
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| S5839 |
L-KynurenineL-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. |
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| S7510 |
UM729UM729 is an enhancer of aryl hydrocarbon receptor (AhR) antagonists. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| 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 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).
|
|
| S8995New |
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. |
||
| S6560New |
PDM2PDM2 is a potent and selective aryl hydrocarbon receptor (AhR) antagonist. |
| 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. |
|
| S0154New |
CAY10465CAY 10465 is a selective and high-affinity agonist on aryl hydrocarbon receptor (AhR) with Ki of 0.2 nM. |
||
| 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. |
||
| S9092 |
NorisoboldineNorisoboldine, a natural aryl hydrocarbon receptor (AhR) agonist, attenuates ulcerative colitis (UC) and induces the generation of Treg cells. |
||
| S5839 |
L-KynurenineL-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 |
|---|---|---|---|
| S7510 |
UM729UM729 is an enhancer of aryl hydrocarbon receptor (AhR) antagonists. |
