AhR

抑制剂选择性比较

AhR产品

所有产品(17) AhR抑制剂(2) AhR拮抗剂(7) AhR激动剂(8)

目录号	产品描述	文献引用	实验数据
S3205^New	Perillaldehyde Perillaldehyde (Perilladehyde, Perillal, PAE, PA) 是紫苏 Perilla frutescens（一种传统的抗氧化剂）的主要成分，可抑制BaP诱导的 AHR 的活化和 ROS 的产生，抑制 BaP/AHR 介导的 CCL2 chemokine 的释放，并激活 NRF2/HO1 抗氧化剂途径。
S8842	BAY-218 BAY-218是一种有效的、选择性AhR小分子抑制剂，抑制AhR核转运、DRE荧光酶报告基因的表达以及AhR调控的靶基因表达。
S1177	PD98059 PD98059 是一种非ATP竞争性的MEK抑制剂，无细胞试验中IC50为2 μM，特异性抑制MEK-1介导的MAPK激活；不直接抑制ERK1或ERK2。PD98059 是一种aryl hydrocarbon receptor (AHR)的配体并起到拮抗剂的功能。	J Cell Physiol, 2021, 236(2):1375-1390 Sci Adv, 2020, 22;6(21):eaaz5913 Cell Rep, 2020, 7;30(1):215-228 e5	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) 是一种aryl hydrocarbon receptor (AhR)抑制剂，无细胞试验中IC50为127 nM。	Proc Natl Acad Sci U S A, 2020, 21;117(16):8845-8849 J Cell Mol Med, 2020, 10.1111/jcmm.15626 Cancer Immunol Immunother, 2020, 27	(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-223191 CH-223191是一种有效的特定aryl hydrocarbon receptor (AhR)拮抗剂，IC50为30 nM。	Cell Res, 2020, 1-10 Am J Respir Crit Care Med, 2020, 10.1164/rccm.202009-3385LE Genome Med, 2020, 12(1):85	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).
S6926^New	GNF351 GNF351 是一种 aryl hydrocarbon receptor (AHR) 的有效拮抗剂。GNF351 可直接与AHR配体结合袋相互作用，并与特征明确的光亲和性AHR配体竞争结合AHR，对应的IC50值为62 nM。
S8995^New	BAY 2416964 BAY 2416964 (compound 192) 是一种有效的、口服活性的 aryl hydrocarbon receptor (AhR) 的拮抗剂，对应的IC50值为341 nM。BAY 2416964 具有治疗实体瘤的潜力。
S0155^New	PDM-11 PDM-11 是一种白藜芦醇resveratrol的衍生物，与白藜芦醇相比，对 arylhydrocarbon receptors (AhR) 的拮抗剂亲和力更强，而对雌激素受体estrogen receptor没有亲和力。
S6560	PDM2 PDM2是一种有效的、选择性aryl hydrocarbon receptor (AhR)拮抗剂。
S2929	Pifithrin-α (PFTα) HBr Pifithrin-α (PFTα)是一种p53抑制剂，抑制p53依赖性的p53应答基因转录。Pifithrin-α也是一种有效的 aryl hydrocarbon receptor (AhR) 的兴奋剂。	Am J Respir Crit Care Med, 2020, 10.1164/rccm.202004-1274OC Neuro Oncol, 2020, noaa207 Br J Pharmacol, 2020, 10.1111/bph.15350	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 Leflunomide (HWA486) 是一种属于DMARD的免疫抑制剂，可抑制嘧啶的合成和 protein tyrosine kinase 的活性。Leflunomide 的活性代谢产物为A77 1726(RS-61980)，可抑制 dihydroorotate dehydrogenase (DHODH)。Leflunomide 还是 AhR 的激动剂。	Gastroenterology, 2019, 10.1053/j Sci Rep, 2019, 9(1):3462 Toxicol Lett, 2018, 282:154-165	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.
S9700^New	Tapinarof Tapinarof (GSK2894512, Benvitimod, WBI 1001, DHPS, DMVT 505) 是一种 aryl hydrocarbon receptor (AhR) 的天然激动剂，可诱导永生化角质形成细胞(HaCaT)中AhR的核易位，EC50值为0.16 nM。Tapinarof 可以以剂量依赖的方式诱导CD4+ T细胞的凋亡，其IC50值为5.2 μM。
S9682^New	FICZ FICZ (6-Formylindolo[3,2-b]carbazole) 是一种 aryl hydrocarbon receptor (AhR) 的有效激动剂，可被AHR调节的细胞色素P4501酶有效地代谢。	J Agric Food Chem, 2020, 10.1021/acs.jafc.0c06319
S0154^New	CAY10465 CAY 10465 是一种对 aryl hydrocarbon receptor (AhR) 具有选择性的、高亲和力的激动剂，其Ki值为0.2 nM。
S2292	Diosmin Diosmin 是一种 aryl hydrocarbon receptor (AhR) 的激动剂。Diosmin 是一种半合成Phlebotropic药物，也是一种在各种柑橘类水果中发现的类黄酮。	Mol Biol Rep, 2020, 47(3):2217-2230 Int J Mol Sci, 2020, 21(14):5025
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)是一种 aryl hydrocarbon receptor (AhR) 激动剂。 L-Kynurenine是氨基酸L-色氨酸的代谢产物和色氨酸代谢途径的中心化合物，可用于生产烟酸（niacin）。

目录号

产品描述

文献引用

实验数据

S3205^New

Perillaldehyde

Perillaldehyde (Perilladehyde, Perillal, PAE, PA) 是紫苏 Perilla frutescens（一种传统的抗氧化剂）的主要成分，可抑制BaP诱导的 AHR 的活化和 ROS 的产生，抑制 BaP/AHR 介导的 CCL2 chemokine 的释放，并激活 NRF2/HO1 抗氧化剂途径。

S8842

BAY-218

BAY-218是一种有效的、选择性AhR小分子抑制剂，抑制AhR核转运、DRE荧光酶报告基因的表达以及AhR调控的靶基因表达。

目录号	产品描述	文献引用	实验数据
S1177	PD98059 PD98059 是一种非ATP竞争性的MEK抑制剂，无细胞试验中IC50为2 μM，特异性抑制MEK-1介导的MAPK激活；不直接抑制ERK1或ERK2。PD98059 是一种aryl hydrocarbon receptor (AHR)的配体并起到拮抗剂的功能。	J Cell Physiol, 2021, 236(2):1375-1390 Sci Adv, 2020, 22;6(21):eaaz5913 Cell Rep, 2020, 7;30(1):215-228 e5	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) 是一种aryl hydrocarbon receptor (AhR)抑制剂，无细胞试验中IC50为127 nM。	Proc Natl Acad Sci U S A, 2020, 21;117(16):8845-8849 J Cell Mol Med, 2020, 10.1111/jcmm.15626 Cancer Immunol Immunother, 2020, 27	(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-223191 CH-223191是一种有效的特定aryl hydrocarbon receptor (AhR)拮抗剂，IC50为30 nM。	Cell Res, 2020, 1-10 Am J Respir Crit Care Med, 2020, 10.1164/rccm.202009-3385LE Genome Med, 2020, 12(1):85	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).
S6926^New	GNF351 GNF351 是一种 aryl hydrocarbon receptor (AHR) 的有效拮抗剂。GNF351 可直接与AHR配体结合袋相互作用，并与特征明确的光亲和性AHR配体竞争结合AHR，对应的IC50值为62 nM。
S8995^New	BAY 2416964 BAY 2416964 (compound 192) 是一种有效的、口服活性的 aryl hydrocarbon receptor (AhR) 的拮抗剂，对应的IC50值为341 nM。BAY 2416964 具有治疗实体瘤的潜力。
S0155^New	PDM-11 PDM-11 是一种白藜芦醇resveratrol的衍生物，与白藜芦醇相比，对 arylhydrocarbon receptors (AhR) 的拮抗剂亲和力更强，而对雌激素受体estrogen receptor没有亲和力。
S6560	PDM2 PDM2是一种有效的、选择性aryl hydrocarbon receptor (AhR)拮抗剂。

目录号	产品描述	文献引用	实验数据
S2929	Pifithrin-α (PFTα) HBr Pifithrin-α (PFTα)是一种p53抑制剂，抑制p53依赖性的p53应答基因转录。Pifithrin-α也是一种有效的 aryl hydrocarbon receptor (AhR) 的兴奋剂。	Am J Respir Crit Care Med, 2020, 10.1164/rccm.202004-1274OC Neuro Oncol, 2020, noaa207 Br J Pharmacol, 2020, 10.1111/bph.15350	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 Leflunomide (HWA486) 是一种属于DMARD的免疫抑制剂，可抑制嘧啶的合成和 protein tyrosine kinase 的活性。Leflunomide 的活性代谢产物为A77 1726(RS-61980)，可抑制 dihydroorotate dehydrogenase (DHODH)。Leflunomide 还是 AhR 的激动剂。	Gastroenterology, 2019, 10.1053/j Sci Rep, 2019, 9(1):3462 Toxicol Lett, 2018, 282:154-165	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.
S9700^New	Tapinarof Tapinarof (GSK2894512, Benvitimod, WBI 1001, DHPS, DMVT 505) 是一种 aryl hydrocarbon receptor (AhR) 的天然激动剂，可诱导永生化角质形成细胞(HaCaT)中AhR的核易位，EC50值为0.16 nM。Tapinarof 可以以剂量依赖的方式诱导CD4+ T细胞的凋亡，其IC50值为5.2 μM。
S9682^New	FICZ FICZ (6-Formylindolo[3,2-b]carbazole) 是一种 aryl hydrocarbon receptor (AhR) 的有效激动剂，可被AHR调节的细胞色素P4501酶有效地代谢。	J Agric Food Chem, 2020, 10.1021/acs.jafc.0c06319
S0154^New	CAY10465 CAY 10465 是一种对 aryl hydrocarbon receptor (AhR) 具有选择性的、高亲和力的激动剂，其Ki值为0.2 nM。
S2292	Diosmin Diosmin 是一种 aryl hydrocarbon receptor (AhR) 的激动剂。Diosmin 是一种半合成Phlebotropic药物，也是一种在各种柑橘类水果中发现的类黄酮。	Mol Biol Rep, 2020, 47(3):2217-2230 Int J Mol Sci, 2020, 21(14):5025
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)是一种 aryl hydrocarbon receptor (AhR) 激动剂。 L-Kynurenine是氨基酸L-色氨酸的代谢产物和色氨酸代谢途径的中心化合物，可用于生产烟酸（niacin）。

研究领域

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AhR

抑制剂选择性比较

AhR产品

Perillaldehyde

BAY-218

PD98059

StemRegenin 1 (SR1)

CH-223191

GNF351

BAY 2416964

PDM-11

PDM2

Pifithrin-α (PFTα) HBr

Leflunomide

Tapinarof

FICZ

CAY10465

Diosmin

Norisoboldine

L-Kynurenine

Perillaldehyde

BAY-218

PD98059

StemRegenin 1 (SR1)

CH-223191

GNF351

BAY 2416964

PDM-11

PDM2

Pifithrin-α (PFTα) HBr

Leflunomide

Tapinarof

FICZ

CAY10465

Diosmin

Norisoboldine

L-Kynurenine