RJW100

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

RJW100 

RJW100 是一种有效的肝受体同源物 1 (LRH-1NR5A2) 和类固醇生成因子-1 (SF-1NR5A1) 激动剂,pEC50 分别为 6.6 和 7.5。RJW100 还可有效激活 miR-200c (miRNA-200c, microRNA-200c) 启动子。

RJW100

RJW100 Chemical Structure

CAS No. : 1276664-20-0

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生物活性

RJW100 is a potent liver receptor homolog 1 (LRH-1, NR5A2) and steroidogenic factor-1 (SF-1, NR5A1) agonist with pEC50s of 6.6 and 7.5, respectively[1]. RJW100 also causes strong activation of the miR-200c (miRNA-200c, microRNA-200c) promoter[2].

IC50 & Target

pEC50: 6.6 (LRH-1) and 7.5 (SF-1)[1]

体外研究
(In Vitro)

RJW100 (compound 24-exo) treatment induces a significant dose-dependent increase in small/short heterodimer partner (SHP) transcripts beginning at 5 µM[1].
RJW100 (compound 24-exo) clearly displaces the bound PIP2 phospholipid from SF-1 almost completely at 1 µM[1].
Using hLRH-1 LBD alone that had not been complexed with any phospholipids, the result shows a clear dose-dependent shift in hLRH-1 LBD (ligand binding domain) native PAGE migration upon RJW100 (compound 24-exo; 0-100 µM) binding[1].
RJW100 causes strong activation of the miR-200c promoter and exhibits strong ability to downregulate ZEB1 and ZEB2 proteins[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

RT-PCR[1]

Cell Line: HEK293 cells
Concentration: 1 µM, 5 µM, 10 µM
Incubation Time: 24 hours
Result: Induced a significant dose-dependent increase in SHP transcripts beginning at 5 µM.

分子量

386.57

Formula

C28H34O

CAS 号

1276664-20-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Richard J Whitby, et al. Small molecule agonists of the orphan nuclear receptors steroidogenic factor-1 (SF-1, NR5A1) and liver receptor homologue-1 (LRH-1, NR5A2). J Med Chem. 2011 Apr 14;54(7):2266-81.

    [2]. Yuxia Zhang, et al. Regulation of miR-200c by nuclear receptors PPARα, LRH-1 and SHP. Biochem Biophys Res Commun. 2011 Dec 9;416(1-2):135-9.

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