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SMI481

    
10mM in DMSO

(4-Chloro-3-nitrophenyl)(4-(2-fluorophenyl)piperazin-1-yl)Methanone

源叶(MedMol)
T28248 一键复制产品信息
432020-20-7
C17H15ClFN3O3
363.7707032
SMI481; SMI-481 SMI 481; NPPM 6748-481; NPPM 6748481; NPPM6748481; NPPM-6748-481
货号 规格 价格 上海 北京 珠海 重庆 武汉 购买数量
T28248-1ml
10mM in DMSO

¥300.00

货期:3-5天 - - - -
产品介绍 参考文献 质检证书(COA) 摩尔浓度计算器 相关产品
产品描述: SMI481 is the first small-molecule Sec14-like phosphatidylinositol transfer proteins (PITPs) inhibitor
体外研究: Sec14-like phosphatidylinositol transfer proteins (PITPs) integrate diverse territories of intracellular lipid metabolism with stimulated phosphatidylinositol-4-phosphate production and are discriminating portals for interrogating phosphoinositide signaling. Yet, neither Sec14-like PITPs nor PITPs in general have been exploited as targets for chemical inhibition for such purposes. Herein, we validate what is to our knowledge the first small-molecule inhibitors (SMIs) of the yeast PITP Sec14. These SMIs are nitrophenyl(4-(2-methoxyphenyl)piperazin-1-yl)methanones (NPPMs) and are effective inhibitors in vitro and in vivo. We further establish that Sec14 is the sole essential NPPM target in yeast and that NPPMs exhibit exquisite targeting specificities for Sec14 (relative to related Sec14-like PITPs), propose a mechanism for how NPPMs exert their inhibitory effects and demonstrate that NPPMs exhibit exquisite pathway selectivity in inhibiting phosphoinositide signaling in cells. These data deliver proof of concept that PITP-directed SMIs offer new and generally applicable avenues for intervening with phosphoinositide signaling pathways with selectivities superior to those afforded by contemporary lipid kinase-directed strategies.
参考文献: 1. Nile AH, Tripathi A, Yuan P, Mousley CJ, Suresh S, Wallace IM, Shah SD, Pohlhaus DT, Temple B, Nislow C, Giaever G, Tropsha A, Davis RW, St Onge RP, Bankaitis VA. PITPs as targets for selectively interfering with phosphoinositide signaling in cells. Nat Chem Biol. 2014 Jan;10(1):76-84. doi: 10.1038/nchembio.1389. Epub 2013 Nov 24. PubMed PMID: 24292071; PubMed Central PMCID: PMC4059020.
溶解性: Soluble  in  DMSO
保存条件: -80℃(运输条件:冰袋低温运输)
配置溶液浓度参考:
1mg 5mg 10mg
1 mM 2.749 ml 13.745 ml 27.49 ml
5 mM 0.55 ml 2.749 ml 5.498 ml
10 mM 0.275 ml 1.374 ml 2.749 ml
50 mM 0.055 ml 0.275 ml 0.55 ml
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参考文献

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