AhR

阻害剤の選択性比較

カタログ番号 製品カタログ 溶解度(25°C)
DMSO アルコール
S8842 BAY-218 <1 mg/mL 80 mg/mL 20 mg/mL
S1177 PD98059 <1 mg/mL 14 mg/mL <1 mg/mL
S2858 StemRegenin 1 (SR1) <1 mg/mL 86 mg/mL <1 mg/mL
S7711 CH-223191 <1 mg/mL 66 mg/mL 4 mg/mL
S8995 BAY 2416964 <1 mg/mL 78 mg/mL 1.5 mg/mL
S6560 PDM2 <1 mg/mL 57 mg/mL 14 mg/mL
S6926 GNF351 <1 mg/mL 30 mg/mL <1 mg/mL
S0155 PDM-11 <1 mg/mL 55 mg/mL 20 mg/mL
S2929 Pifithrin-α (PFTα) HBr <1 mg/mL 67 mg/mL <1 mg/mL
S1247 Leflunomide (HWA486) <1 mg/mL 54 mg/mL ''54 mg/mL
E0143 ITE <1 mg/mL 57 mg/mL 2 mg/mL
S9700 Tapinarof <1 mg/mL 51 mg/mL 51 mg/mL
S2292 Diosmin <1 mg/mL 6 mg/mL <1 mg/mL
S0154 CAY10465 <1 mg/mL 63 mg/mL 40 mg/mL
S9092 Norisoboldine -1 mg/mL 62 mg/mL -1 mg/mL
S5839 L-Kynurenine 3 mg/mL 42 mg/mL '<1 mg/mL
S9682 FICZ <1 mg/mL 57 mg/mL <1 mg/mL

AhR製品

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
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.

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.

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.

S2858

StemRegenin 1 (SR1)

StemRegenin 1 (SR1) is an aryl hydrocarbon receptor (AhR) inhibitor with IC50 of 127 nM in a cell-free assay.

S7711

CH-223191

CH-223191 is a potent and specific aryl hydrocarbon receptor (AhR) antagonist with IC50 of 30 nM.

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.

S6560

PDM2

PDM2 is a potent and selective aryl hydrocarbon receptor (AhR) antagonist.

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.

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).

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.

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.

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.

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.

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.

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.

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.

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
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.

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.

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
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.

2022, 541:215749

2022, e12795

2022, 13:817596

S2858

StemRegenin 1 (SR1)

StemRegenin 1 (SR1) is an aryl hydrocarbon receptor (AhR) inhibitor with IC50 of 127 nM in a cell-free assay.

2022, 604(7906):534-540

2022, 177:106132

2022, 12(1):6005

S7711

CH-223191

CH-223191 is a potent and specific aryl hydrocarbon receptor (AhR) antagonist with IC50 of 30 nM.

2022, 158:106989

2022, 30:101272

2021, e13466

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.

S6560

PDM2

PDM2 is a potent and selective aryl hydrocarbon receptor (AhR) antagonist.

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.

2021, 12:655281

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.

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
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).

2022, S1525-0016(22)00317-3

2022, 41(1):130

2022, S2352-345X(22)00063-7

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.

2022, 13(2):154

2021, 12(9):821

2021, 12:685984

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.

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.

2022, molcanther.0841.2021

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.

2020, 47(3):2217-2230

2020, 21(14):5025

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.

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.

2021, 11(19):9623-9651

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.

2020, 10.1021/acs.jafc.0c06319

Tags: AhR inhibitor|AhR agonist|AhR activator|AhR inducer|AhR antagonist|AhR signaling pathway|AhR assay kit