• 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： 2-8°C

• 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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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *