EasySep™小鼠TIL（CD45）正选试剂盒
产品号 #72732_C
芳烃受体（AHR）拮抗剂
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总览
CH223191是一种高效的特异性芳烃受体（AHR）拮抗剂，可阻断2,3,7,8-四氯二苯并-对二恶英(TCDD）的激活（IC50 = 0.03µm）（Kim et al.)。它还可以抑制TCDD在HepG2细胞和小鼠肝脏中诱导细胞色素P450 1A1 的表达（Kim et al.）。
维持和自我更新
·促进人CD34+造血干细胞和祖细胞在体外的扩增（Boitano et al.）。
细胞类型
造血干/祖细胞
种属
人，小鼠，非人灵长类，其它细胞系，大鼠
应用
扩增
研究领域
干细胞生物学
CAS 编号
301326-22-7
化学式
C₁₉H₁₉N₅O
纯度
≥ 95 %
通路
AHR
靶点
AHR
产品说明书及文档
请在《产品说明书》中查找相关支持信息和使用说明，或浏览下方更多实验方案。
应用领域
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相关材料与文献
技术资料 (1)
文献 (2)
Aryl hydrocarbon receptor antagonists promote the expansion of human hematopoietic stem cells. Science (New York, N.Y.) 2010 SEP
Abstract
Although practiced clinically for more than 40 years, the use of hematopoietic stem cell (HSC) transplants remains limited by the ability to expand these cells ex vivo. An unbiased screen with primary human HSCs identified a purine derivative, StemRegenin 1 (SR1), that promotes the ex vivo expansion of CD34+ cells. Culture of HSCs with SR1 led to a 50-fold increase in cells expressing CD34 and a 17-fold increase in cells that retain the ability to engraft immunodeficient mice. Mechanistic studies show that SR1 acts by antagonizing the aryl hydrocarbon receptor (AHR). The identification of SR1 and AHR modulation as a means to induce ex vivo HSC expansion should facilitate the clinical use of HSC therapy.
Novel compound 2-methyl-2H-pyrazole-3-carboxylic acid (2-methyl-4-o-tolylazo-phenyl)-amide (CH-223191) prevents 2,3,7,8-TCDD-induced toxicity by antagonizing the aryl hydrocarbon receptor. Molecular pharmacology 2006 JUN
Abstract
2,3,7,8-Tetrachlorodibenzo-p-dioxin (TCDD) is a widespread environmental pollutant with many toxic effects, including endocrine disruption, reproductive dysfunction, immunotoxicity, liver damage, and cancer. These are mediated by TCDD binding to and activating the aryl hydrocarbon receptor (AhR), a basic helix-loop-helix transcription factor. In this regard, targeting the AhR using novel small molecule inhibitors is an attractive strategy for the development of potential preventive agents. In this study, by screening a chemical library composed of approximately 10,000 compounds, we identified a novel compound, 2-methyl-2H-pyrazole-3-carboxylic acid (2-methyl-4-o-tolylazo-phenyl)-amide (CH-223191), that potently inhibits TCDD-induced AhR-dependent transcription. In addition, CH-223191 blocked the binding of TCDD to AhR and inhibited TCDD-mediated nuclear translocation and DNA binding of AhR. These inhibitory effects of CH-223191 prevented the expression of cytochrome P450 enzymes, target genes of the AhR. Unlike many known antagonists of AhR, CH-223191 did not have detectable AhR agonist-like activity or estrogenic potency, suggesting that CH-223191 is a specific antagonist of AhR. It is noteworthy that CH-223191 potently prevented TCDD-elicited cytochrome P450 induction, liver toxicity, and wasting syndrome in mice. Taken together, these results demonstrate that this novel compound, CH-223191, may be a useful agent for the study of AhR-mediated signal transduction and the prevention of TCDD-associated pathology.
更多信息
| 种属 | Human, Mouse, Non-Human Primate, Other, Rat |
|---|---|
| Cas Number | 301326-22-7 |
| Chemical Formula | C₁₉H₁₉N₅O |
| 纯度 | ≥ 95% |
| Target | AHR |
| Pathway | AHR |
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