S1177 |
PD98059
|
PD98059 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. |
-
Nat Commun, 2024, 15(1):987
-
Adv Sci (Weinh), 2024, 11(4):e2304987
-
Cell Commun Signal, 2024, 22(1):473
|
|
S2929 |
Pifithrin-α (PFTα) HBr
|
Pifithrin-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). |
-
Cell Death Differ, 2024, 31(8):999-1012
-
Int J Biol Sci, 2024, 20(6):2008-2026
-
Cell Mol Life Sci, 2024, 81(1):101
|
|
S7711 |
CH-223191
|
CH-223191 is a potent and specific aryl hydrocarbon receptor (AhR) antagonist with IC50 of 30 nM.
|
-
Cancer Commun (Lond), 2024, 10.1002/cac2.12545
-
Cancer Commun (Lond), 2024, 44(6):670-694
-
Theranostics, 2024, 14(7):2719-2735
|
|
S2858 |
SR1 (StemRegenin 1)
|
SR1 (StemRegenin 1) is an aryl hydrocarbon receptor (AhR) inhibitor with IC50 of 127 nM in a cell-free assay. |
-
Nat Biotechnol, 2024, 10.1038/s41587-024-02360-7
-
Biochem Pharmacol, 2024, 223:116172
-
iScience, 2024, 27(5):109682
|
|
S1247 |
Leflunomide
|
Leflunomide 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. |
-
Nat Commun, 2024, 15(1):8708
-
bioRxiv, 2024, 2024.07.02.601567
-
EMBO J, 2023, e110620.
|
|
S9682 |
FICZ
|
FICZ (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. |
-
Cell Death Dis, 2023, 14(1):18
-
Front Microbiol, 2022, 13:934786
-
J Agric Food Chem, 2020, 10.1021/acs.jafc.0c06319
|
|
S8842 |
BAY-218
|
BAY-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. |
-
Cancer Commun (Lond), 2024, 10.1002/cac2.12545
-
Cancer Commun (Lond), 2024, 44(6):670-694
-
Commun Biol, 2024, 7(1):442
|
|
S9700 |
Tapinarof
|
Tapinarof (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. |
-
Mol Cancer Res, 2024, 10.1158/1541-7786.MCR-24-0151
-
J Med Chem, 2022, 2
-
Mol Cancer Ther, 2022, molcanther.0841.2021
|
|
S8995 |
BAY 2416964
|
BAY 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. |
-
bioRxiv, 2024, 2023.11.04.565649
-
Cell Death Dis, 2023, 14(1):18
|
|
S6926 |
GNF351
|
GNF351 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. |
-
Front Pharmacol, 2021, 12:655281
|
|
S5839 |
L-Kynurenine
|
L-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. |
-
Theranostics, 2021, 11(19):9623-9651
|
|
S2292 |
Diosmin
|
Diosmin 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. |
-
Int J Mol Sci, 2020, 21(14):5025
-
Mol Biol Rep, 2020, 47(3):2217-2230
|
|
S6560 |
PDM2
|
PDM2 is a potent and selective aryl hydrocarbon receptor (AhR) antagonist. |
-
Cancer Cell Int, 2021, 21(1):538
|
|
S0154 |
CAY10465
|
CAY 10465 is a selective and high-affinity agonist on aryl hydrocarbon receptor (AhR) with Ki of 0.2 nM. |
|
|
S0155 |
PDM-11
|
PDM-11 is a derivative of resveratrol that exhibits stronger antagonist affinity for arylhydrocarbon receptors (AhR) than resveratrol, without any affinity for the estrogen receptor. |
|
|
E5768New |
Indolelactic acid
|
Indolelactic acid (Indole-3-lactic acid), a metabolite of tryptophan (Trp), plays a role in immune cell differentiation and cytokine production by activating aryl hydrocarbon receptors (AhR). This regulation supports immune responses and aids in anti-inflammatory and anti-allergic activities. It also plays an important role in the balance of Th17/Treg cells by reprogramming CD4+ Th cells into CD4+CD8+ Treg cells and inhibiting the polarization of Th17 cells. |
|
|
S9092 |
Norisoboldine
|
Norisoboldine (Laurelliptine), a natural aryl hydrocarbon receptor (AhR) agonist, attenuates ulcerative colitis (UC) and induces the generation of Treg cells. |
-
iScience, 2024, 27(5):109682
-
bioRxiv, 2024, 2023.11.04.565649
|
|
S3205 |
Perillaldehyde
|
Perillaldehyde (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. |
|
|
E0143 |
ITE
|
ITE (2-(1′H-indole-3′-carbonyl)-thiazole-4-carboxylic acid methyl ester) is a potent endogenous agonist of aryl hydrocarbon receptor (AhR) that directly binds to AHR with a Ki of 3 nM. |
|
|
S2929 |
Pifithrin-α (PFTα) HBr
|
Pifithrin-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). |
-
Cell Death Differ, 2024, 31(8):999-1012
-
Int J Biol Sci, 2024, 20(6):2008-2026
-
Cell Mol Life Sci, 2024, 81(1):101
|
|
S1247 |
Leflunomide
|
Leflunomide 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. |
-
Nat Commun, 2024, 15(1):8708
-
bioRxiv, 2024, 2024.07.02.601567
-
EMBO J, 2023, e110620.
|
|
S9682 |
FICZ
|
FICZ (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. |
-
Cell Death Dis, 2023, 14(1):18
-
Front Microbiol, 2022, 13:934786
-
J Agric Food Chem, 2020, 10.1021/acs.jafc.0c06319
|
|
S9700 |
Tapinarof
|
Tapinarof (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. |
-
Mol Cancer Res, 2024, 10.1158/1541-7786.MCR-24-0151
-
J Med Chem, 2022, 2
-
Mol Cancer Ther, 2022, molcanther.0841.2021
|
|
S5839 |
L-Kynurenine
|
L-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. |
-
Theranostics, 2021, 11(19):9623-9651
|
|
S2292 |
Diosmin
|
Diosmin 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. |
-
Int J Mol Sci, 2020, 21(14):5025
-
Mol Biol Rep, 2020, 47(3):2217-2230
|
|
S0154 |
CAY10465
|
CAY 10465 is a selective and high-affinity agonist on aryl hydrocarbon receptor (AhR) with Ki of 0.2 nM. |
|
|
S9092 |
Norisoboldine
|
Norisoboldine (Laurelliptine), a natural aryl hydrocarbon receptor (AhR) agonist, attenuates ulcerative colitis (UC) and induces the generation of Treg cells. |
-
iScience, 2024, 27(5):109682
-
bioRxiv, 2024, 2023.11.04.565649
|
|
E0143 |
ITE
|
ITE (2-(1′H-indole-3′-carbonyl)-thiazole-4-carboxylic acid methyl ester) is a potent endogenous agonist of aryl hydrocarbon receptor (AhR) that directly binds to AHR with a Ki of 3 nM. |
|
|
S1177 |
PD98059
|
PD98059 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. |
- Nat Commun, 2024, 15(1):987
- Adv Sci (Weinh), 2024, 11(4):e2304987
- Cell Commun Signal, 2024, 22(1):473
|
|
S7711 |
CH-223191
|
CH-223191 is a potent and specific aryl hydrocarbon receptor (AhR) antagonist with IC50 of 30 nM.
|
- Cancer Commun (Lond), 2024, 10.1002/cac2.12545
- Cancer Commun (Lond), 2024, 44(6):670-694
- Theranostics, 2024, 14(7):2719-2735
|
|
S2858 |
SR1 (StemRegenin 1)
|
SR1 (StemRegenin 1) is an aryl hydrocarbon receptor (AhR) inhibitor with IC50 of 127 nM in a cell-free assay. |
- Nat Biotechnol, 2024, 10.1038/s41587-024-02360-7
- Biochem Pharmacol, 2024, 223:116172
- iScience, 2024, 27(5):109682
|
|
S8995 |
BAY 2416964
|
BAY 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. |
- bioRxiv, 2024, 2023.11.04.565649
- Cell Death Dis, 2023, 14(1):18
|
|
S6926 |
GNF351
|
GNF351 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. |
- Front Pharmacol, 2021, 12:655281
|
|
S6560 |
PDM2
|
PDM2 is a potent and selective aryl hydrocarbon receptor (AhR) antagonist. |
- Cancer Cell Int, 2021, 21(1):538
|
|
S0155 |
PDM-11
|
PDM-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) HBr
|
Pifithrin-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). |
- Cell Death Differ, 2024, 31(8):999-1012
- Int J Biol Sci, 2024, 20(6):2008-2026
- Cell Mol Life Sci, 2024, 81(1):101
|
|
S1247 |
Leflunomide
|
Leflunomide 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. |
- Nat Commun, 2024, 15(1):8708
- bioRxiv, 2024, 2024.07.02.601567
- EMBO J, 2023, e110620.
|
|
S9682 |
FICZ
|
FICZ (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. |
- Cell Death Dis, 2023, 14(1):18
- Front Microbiol, 2022, 13:934786
- J Agric Food Chem, 2020, 10.1021/acs.jafc.0c06319
|
|
S9700 |
Tapinarof
|
Tapinarof (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. |
- Mol Cancer Res, 2024, 10.1158/1541-7786.MCR-24-0151
- J Med Chem, 2022, 2
- Mol Cancer Ther, 2022, molcanther.0841.2021
|
|
S5839 |
L-Kynurenine
|
L-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. |
- Theranostics, 2021, 11(19):9623-9651
|
|
S2292 |
Diosmin
|
Diosmin 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. |
- Int J Mol Sci, 2020, 21(14):5025
- Mol Biol Rep, 2020, 47(3):2217-2230
|
|
S0154 |
CAY10465
|
CAY 10465 is a selective and high-affinity agonist on aryl hydrocarbon receptor (AhR) with Ki of 0.2 nM. |
|
|
S9092 |
Norisoboldine
|
Norisoboldine (Laurelliptine), a natural aryl hydrocarbon receptor (AhR) agonist, attenuates ulcerative colitis (UC) and induces the generation of Treg cells. |
- iScience, 2024, 27(5):109682
- bioRxiv, 2024, 2023.11.04.565649
|
|
E0143 |
ITE
|
ITE (2-(1′H-indole-3′-carbonyl)-thiazole-4-carboxylic acid methyl ester) is a potent endogenous agonist of aryl hydrocarbon receptor (AhR) that directly binds to AHR with a Ki of 3 nM. |
|
|