AhR

抑制剂选择性比较

AhR产品

所有产品(18) AhR抑制剂(2) AhR拮抗剂(7) AhR激动剂(9)

目录号	产品描述	文献引用	实验数据
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。	Acta Biochim Biophys Sin (Shanghai), 2021, gmab017
S3205	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。
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。	Cells, 2022, 11(1)134 Microbiol Spectr, 2022, e0188121 Cancer Immunol Immunother, 2022, 10.1007/s00262-021-03126-9	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。	Stem Cell Res, 2021, 53:102287 Mol Cancer Ther, 2021, molcanther.0029.2021 Acta Biochim Biophys Sin (Shanghai), 2021, gmab122	(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。	EMBO Mol Med, 2021, e13466 J Immunol, 2021, 207(6):1672-1682 Mol Hum Reprod, 2021, 27(3)gaab003	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).
S8995	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。
S6560	PDM2 PDM2是一种有效的、选择性aryl hydrocarbon receptor (AhR)拮抗剂。
S6926	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。	Front Pharmacol, 2021, 12:655281
S0155	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。
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。	Br J Pharmacol, 2021, 10.1111/bph.15385 Development, 2021, dev.188276 Biochim Biophys Acta Mol Cell Res, 2021, 1869(2):119174	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)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。	Cell Death Dis, 2021, 12(9):821 Front Immunol, 2021, 12:685984 Cell Transplant, 2021, 30:9636897211054503	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.
E0143^New	ITE ITE (2-(1′H-indole-3′-carbonyl)-thiazole-4-carboxylic acid methyl ester)是一种有效的芳烃受体 (AhR) 内源性激动剂，可直接与 AHR 结合，Ki 为 3 nM。
S9700	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。
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
S0154	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。
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）。	Theranostics, 2021, 11(19):9623-9651
S9682	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

目录号	产品描述	文献引用	实验数据
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。	Acta Biochim Biophys Sin (Shanghai),2021, gmab017
S3205	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。

目录号

产品描述

文献引用

实验数据

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。

Acta Biochim Biophys Sin (Shanghai),2021, gmab017

S3205

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。

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。	Cells, 2022, 11(1)134 Microbiol Spectr, 2022, e0188121 Cancer Immunol Immunother, 2022, 10.1007/s00262-021-03126-9	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。	Stem Cell Res, 2021, 53:102287 Mol Cancer Ther, 2021, molcanther.0029.2021 Acta Biochim Biophys Sin (Shanghai), 2021, gmab122	(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。	EMBO Mol Med, 2021, e13466 J Immunol, 2021, 207(6):1672-1682 Mol Hum Reprod, 2021, 27(3)gaab003	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).
S8995	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。
S6560	PDM2 PDM2是一种有效的、选择性aryl hydrocarbon receptor (AhR)拮抗剂。
S6926	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。	Front Pharmacol, 2021, 12:655281
S0155	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。

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。	Br J Pharmacol, 2021, 10.1111/bph.15385 Development, 2021, dev.188276 Biochim Biophys Acta Mol Cell Res, 2021, 1869(2):119174	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)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。	Cell Death Dis, 2021, 12(9):821 Front Immunol, 2021, 12:685984 Cell Transplant, 2021, 30:9636897211054503	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.
E0143^New	ITE ITE (2-(1′H-indole-3′-carbonyl)-thiazole-4-carboxylic acid methyl ester)是一种有效的芳烃受体 (AhR) 内源性激动剂，可直接与 AHR 结合，Ki 为 3 nM。
S9700	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。
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
S0154	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。
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）。	Theranostics, 2021, 11(19):9623-9651
S9682	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

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