AhR

抑制剂选择性比较

AhR产品

所有产品 AhR抑制剂(1) AhR拮抗剂(5) AhR激动剂(5) AhR调节剂(1)

目录号	产品描述	文献引用	实验数据
S8842^New	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。	Sci Adv, 2020, 22;6(21):eaaz5913 Cell Rep, 2020, 7;30(1):215-228 e5 Cell Death Dis, 2020, 11(2):143	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 Cancer Immunol Immunother, 2020, 27 Int Immunopharmacol, 2020, 81:106266	(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。	Leuk Lymphoma, 2020, 6:1-11 Cell Biol Toxicol, 2019, 10.1007/s10565-019-09499-z Nat Commun, 2018, 9(1):4775	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^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。
S6560^New	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。	Cancers (Basel), 2020, 20;12(2) pii: E493 J Steroid Biochem Mol Biol, 2020, 198:105537 J Biol Chem, 2020, 27;295(13):4237-4251	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.
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
S9092	Norisoboldine Norisoboldine, a natural aryl hydrocarbon receptor (AhR) agonist, attenuates ulcerative colitis (UC) and induces the generation of Treg cells.
S5839	L-Kynurenine L-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）。
S7510	UM729 UM729 是一种aryl hydrocarbon receptor (AhR)拮抗剂的增强剂。	Front Oncol, 2020, 1;10:393 Haematologica, 2019, 10.3324/haematol.2018.212886 Blood Adv, 2019, 3(19):2825-2835

目录号

产品描述

文献引用

实验数据

S8842^New

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。	Sci Adv, 2020, 22;6(21):eaaz5913 Cell Rep, 2020, 7;30(1):215-228 e5 Cell Death Dis, 2020, 11(2):143	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 Cancer Immunol Immunother, 2020, 27 Int Immunopharmacol, 2020, 81:106266	(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。	Leuk Lymphoma, 2020, 6:1-11 Cell Biol Toxicol, 2019, 10.1007/s10565-019-09499-z Nat Commun, 2018, 9(1):4775	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^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。
S6560^New	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。	Cancers (Basel), 2020, 20;12(2) pii: E493 J Steroid Biochem Mol Biol, 2020, 198:105537 J Biol Chem, 2020, 27;295(13):4237-4251	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.
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
S9092	Norisoboldine Norisoboldine, a natural aryl hydrocarbon receptor (AhR) agonist, attenuates ulcerative colitis (UC) and induces the generation of Treg cells.
S5839	L-Kynurenine L-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

S7510

UM729

UM729 是一种aryl hydrocarbon receptor (AhR)拮抗剂的增强剂。

Front Oncol, 2020, 1;10:393

Haematologica, 2019, 10.3324/haematol.2018.212886

Blood Adv, 2019, 3(19):2825-2835