AhR
抑制剂选择性比较
AhR产品
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S3205New |
PerillaldehydePerillaldehyde (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。 |
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| S8842 |
BAY-218BAY-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。 |
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| S1177 |
PD98059PD98059 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。 |
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. |
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| 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。 |
(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
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| S7711 |
CH-223191CH-223191是一种有效的特定aryl hydrocarbon receptor (AhR)拮抗剂，IC50为30 nM。 |
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).
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| S6926New |
GNF351GNF351 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。 |
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| S8995New |
BAY 2416964BAY 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。 |
||
| S0155New |
PDM-11PDM-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。 |
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| S6560 |
PDM2PDM2是一种有效的、选择性aryl hydrocarbon receptor (AhR)拮抗剂。 |
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| S2929 |
Pifithrin-α (PFTα) HBrPifithrin-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。 |
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. |
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| S1247 |
LeflunomideLeflunomide (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。 |
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. |
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| S9700New |
TapinarofTapinarof (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。 |
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| S9682New |
FICZFICZ (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。 |
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| S0154New |
CAY10465CAY 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。 |
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| S2292 |
DiosminDiosmin 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。 |
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| S9092 |
NorisoboldineNorisoboldine (Laurelliptine), a natural aryl hydrocarbon receptor (AhR) agonist, attenuates ulcerative colitis (UC) and induces the generation of Treg cells. |
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| S5839 |
L-KynurenineL-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 |
|---|---|---|---|
| S3205New |
PerillaldehydePerillaldehyde (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-218BAY-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 |
PD98059PD98059 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。 |
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。 |
(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-223191CH-223191是一种有效的特定aryl hydrocarbon receptor (AhR)拮抗剂，IC50为30 nM。 |
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).
|
|
| S6926New |
GNF351GNF351 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。 |
||
| S8995New |
BAY 2416964BAY 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。 |
||
| S0155New |
PDM-11PDM-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 |
PDM2PDM2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) HBrPifithrin-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。 |
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 |
LeflunomideLeflunomide (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。 |
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. |
|
| S9700New |
TapinarofTapinarof (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。 |
||
| S9682New |
FICZFICZ (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。 |
||
| S0154New |
CAY10465CAY 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 |
DiosminDiosmin 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。 |
||
| S9092 |
NorisoboldineNorisoboldine (Laurelliptine), a natural aryl hydrocarbon receptor (AhR) agonist, attenuates ulcerative colitis (UC) and induces the generation of Treg cells. |
||
| S5839 |
L-KynurenineL-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）。 |
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