


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.MedChemEIPI-3063Cat. No.: HY-111510CAS No.: 1425043-73-7分式: CHNO分量: 455.51作靶点: PI3K作通路: PI3K/Akt/mTOR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 : 83.33 mg/mL (182.94 mM)* means soluble, but satu
2、ration unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.1953 mL 10.9767 mL 21.9534 mL5 mM 0.4391 mL 2.1953 mL 4.3907 mL10 mM 0.2195 mL 1.0977 mL 2.1953 mL请根据产品在不同溶剂中的溶解度,选择合适的溶剂配制储备液,并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 IPI-3063种有效的选择性 PI3K p110 抑制剂,IC50 为 2.51.2 nM。IC50 & Target p110 p
3、110 p110 p1102.5 nM (IC50) 1170 nM (IC50) 1508 nM (IC50) 2187 nM (IC50)体外研究IPI-3063 inhibits p110, p110, and p110 with IC50s of 1171533 nM, 1508624 nM, and 21871529 nM,1/2 Master of Small Molecules 您边的抑制剂师www.MedChemErespectively. IPI-3063 potently reduces mouse B cell proliferation, survival, and p
4、lasmablast differentiationwhile increasing antibody class switching to IgG1. IPI-3063 is a p110 selective compound with an IC50=0.1nM in p110-specific cell-based assays and cellular IC50 values for the other class I PI3K isoforms are atleast 1,000-fold higher (IC50=19011318 nM for p110, IC50=102.835
5、.7 nM for p110, IC50=418.8117.2nM for p110). IPI-3063 is very potent in reducing p-AKT (significant effect at 1nM). IPI-3063 also reduces p-ERK1/2 with a significant effect at 10nM. IPI-3063 is very potent, achieving a significant decrease in B cellsurvival when present at 10nM 1.PROTOCOLKinase Assa
6、y 1 Human recombinant PI3K-, PI3K-, PI3K-, and PI3K- are used. Phosphatidylinositol 4,5 bis phosphate(diC8-PtdIns(4,5)P2) is used. PI3K-, , and are heterodimers consisting of full length p110, p110, orp110 catalytic subunit and the p85 regulatory subunit. PI3K- is a monomer of the p110 catalytic sub
7、unit.Samples of kinase (10nM-, , and ; 20nM-) are incubated with IPI-3063 for 30min at room temperaturein reaction buffer (15mM HEPES pH 7.4, 20mM NaCl, 1mM EGTA, 0.02% Tween 20, 10mM MgCl2, 0.2mg/mL bovine-globulins) followed by addition of ATP/diC8-PtdIns(4,5)P2 mixture to give finalconcentrations
8、 of 3mM ATP and 500M diC8-PtdIns(4,5)P2. Reactions are incubated at room temperaturefor 2h, with PI3K activity is assessed. Plates are read on plate reader in luminescence mode 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Cell Assay 1 Peripheral bl
9、ood mononuclear cells (PBMCs) are first purified from blood by density gradient centrifugation.Human B cells are then purified from PBMCs by negative selection. B-cell purity is increased from 4% to70% as measured by FACS analysis using anti-CD19 PE conjugated antibody. Purified B cells are seededat
10、 a final concentration of 0.1106cells/mL and cultured with 2g/mL human CD40L+5g/mL anti-humanIgM/IgG+100g/mL hIL-2+100g/mL hIL-21. All B cells are cultured in RPMI 1640 supplemented with 10%(vol/vol) heat-inactivated FCS, 5mM Hepes, 2mM L-glutamine, 100U/mL Penicillin, 100g/mLStreptomycin, 50M 2-mer
11、captoethanol. Purified human B cells are pretreated with IPI-3063 (0.1, 1, 10, and100nM) for 30min, then stimulated with human CD40L+anti-human IgM/IgG+human IL-2+human IL-21 for120h 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Chiu H, et al. The Selective Phosphoinoside-3-Kinase p110 Inhibitor IPI-3063 Potently Suppresses B Cell Survival, Proliferation, andDifferentiation. Front Immunol. 2017 Jun 30;8:747.McePdfHeightCaution: Product
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
- 冬季绿化养护与管理
- 宣传写作课件学习
- 宠物日常护理课件图片
- 二零二五年度新能源电池采购合同协议
- 2025版茶叶品牌重塑与市场拓展合同
- 二零二五年度个人消费贷款借款合同
- 二零二五年度测绘仪器采购与测绘项目验收服务合同
- 2025版跨国公司财务全球税务筹划合同
- 2025版高端医疗器械采购合同作废及供应商变更协议
- 二零二五年度阿拉尔经济技术开发区土地经营权流转合同
- 初中英语跨学科教学的教学方法策略
- GB/T 1634.1-2025塑料负荷变形温度的测定第1部分:通用试验方法
- 肩袖修补术护理
- 政府委托代建合同范本
- 月子中心员工手册管理制度
- DB37-T 1933-2022 氯碱安全生产技术规范
- 2025中考数学专项复习:最值问题之瓜豆原理模型(含答案)
- 2025年浙江宁波北仑热力有限公司招聘笔试参考题库含答案解析
- 人教版英语九年级全一册单词表(合订)-副本
- 2025年浙江丽水景宁畲族自治县交通发展集团有限公司招聘笔试参考题库附带答案详解
- 印章保管责任书
评论
0/150
提交评论