


下载本文档
版权说明:本文档由用户提供并上传,收益归属内容提供方,若内容存在侵权,请进行举报或认领
文档简介
1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemERA190Cat. No.: HY-100739CAS No.: 1617495-03-0分式: CHClNO分量: 596.76作靶点: Proteasome作通路: Metabolic Enzyme/Protease储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (167.57 mM)H2O : 40%
2、PEG300 5% Tween-80 45% salineSolubility: 2.38 mg/mL (3.99 mM); Clear solutionBIOLOGICAL ACTIVITY1/2 Master of Small Molecules 您边的抑制剂师www.MedChemE物活性 RA190双亚苄 哌啶,通过与泛素受体RPN13的半胱氨酸88共价结合来抑制蛋酶体功能。IC50 & Target IC50: 0.15 M (HeLa cell)体外研究 RA190 covalently binds to cysteine 88 of ubiquitin receptor RPN1
3、3 in the 19S regulatory particle and inhibitsproteasome function, triggering rapid accumulation of polyubiquitinated proteins. Multiple myeloma (MM)lines, even those resistant to bortezomib, are sensitive to RA190 via endoplasmic reticulum stress-relatedapoptosis. RA190 stabilizes targets of human p
4、apillomavirus (HPV) E6 oncoprotein, and preferentially killsHPV-transformed cells 1.体内研究 RA190 distributes to plasma and major organs excepting brain, and inhibits proteasome function in skin andmuscle. RA190 administration profoundly reduces growth of multiple myeloma and ovarian cancerxenografts,
5、and oral RA190 treatment retards HPV16+ syngeneic mouse tumor growth, without impactingspontaneous HPV-specific CD8+ T cell responses 1.PROTOCOLCell Assay 1 RA190 is dissolved in DMSO and diluted with cell culture medium. HeLa cells are treated with RA190 (0.2,0.4, 0.6, 0.8, 1, 2, 3, 4, 5 M) for 48
6、hr. Cell viability is assayed using commerical kit 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice: Mice are divided into two groups and treated daily i.p. with RA190 (10 mg/kg) or vehicle, and imagedAdministration 1 again on day 7 and day
7、 14. NOG mice (5 per group) are inoculated with 1X106 NCI-H929-GFP-Luc cells i.v.,and after 4 weeks, mice are imaged for their luciferase activity and divided into two groups. Mice are treatedi.p. with RA190 (20 mg/kg) or vehicle, and imaged again at the end of the treatment for their luciferaseacti
8、vity 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Anchoori RK, et al. A bis-benzylidine piperidone targeting proteasome ubiquitin receptor RPN13/ADRM1 as a therapy for cancer. CancerCell. 2013 Dec 9;24(6):791-805.McePdfHeightCaution: Product has not been fully validated for medical applications.
温馨提示
- 1. 本站所有资源如无特殊说明,都需要本地电脑安装OFFICE2007和PDF阅读器。图纸软件为CAD,CAXA,PROE,UG,SolidWorks等.压缩文件请下载最新的WinRAR软件解压。
- 2. 本站的文档不包含任何第三方提供的附件图纸等,如果需要附件,请联系上传者。文件的所有权益归上传用户所有。
- 3. 本站RAR压缩包中若带图纸,网页内容里面会有图纸预览,若没有图纸预览就没有图纸。
- 4. 未经权益所有人同意不得将文件中的内容挪作商业或盈利用途。
- 5. 人人文库网仅提供信息存储空间,仅对用户上传内容的表现方式做保护处理,对用户上传分享的文档内容本身不做任何修改或编辑,并不能对任何下载内容负责。
- 6. 下载文件中如有侵权或不适当内容,请与我们联系,我们立即纠正。
- 7. 本站不保证下载资源的准确性、安全性和完整性, 同时也不承担用户因使用这些下载资源对自己和他人造成任何形式的伤害或损失。
最新文档
- 2025中菲机械制造与维修服务合同
- 2025型材购销合同书范本
- 2025建设用地使用权出让合同样本
- 2025吊车租赁合同(台班版)
- 9.1《日益完善的法律体系》- 课件 2024-2025学年统编版道德与法治七年级下册
- 2025商业房产租赁合同
- 《高血压自我管理手册》课件
- 六年级思想品德下册 中国人民站起来了教学设计 泰山版
- 《癌痛疼痛治疗方案》课件
- 新质生产力局长
- DB65T 8020-2024 房屋建筑与市政基础设施工程施工现场从业人员配备标准
- 酒店餐饮销售培训
- 情报信息发布规范
- 无卤阻燃剂知识培训课件
- DB42∕T 1496-2019 公路边坡监测技术规程
- 2025-2030年中国小麦加工产业运行动态及发展可行性分析报告
- 乾坤未定皆有可能-2025届高三百日誓师班会课件
- 2025年山西汾西矿业集团公司招聘笔试参考题库含答案解析
- 2024年度英语课件容貌焦虑
- 神经外科质量与安全管理工作计划
- 城市违建拆除施工方案
评论
0/150
提交评论