GSK2194069-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEGSK2194069Cat.No.:HY-12325CASNo.:1332331-08-4分⼦式:C₂₅H₂₄N₄O₃分⼦量:428.48作⽤靶点:FattyAcidSynthase(FASN)作⽤通路:MetabolicEnzyme/Protease储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥100mg/mL(233.38mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM2.3338mL11.6692mL23.3383mL5mM0.4668mL2.3338mL4.6677mL10mM0.2334mL1.1669mL2.3338mL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；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(5.83mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(5.83mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.83mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性GSK2194069脂酸合成酶(FASN)的β-酮还原酶(KR)的有效抑制剂，IC50为7.7nM。GSK2194069通过作⽤⼄酰⼄酰辅酶A、NADPH(IC50或Ki分别为4.8nM和5.6nM)，抑制表达FAS的癌细胞。体外研究GSK2194069(100nM;24h)inhibitsfattyacidsynthase(FAS)incancercelllines(KATO-III,MKN45,A549,SNU-1)withoutreducingFASproductionproteinlevel[1].GSK2194069decreasesphosphatidylcholinelevelsinA549cellswithahalf-maximumeffectiveconcentration(EC50)valueof15.5±9nM(n=78),correlatingwiththedecreasedpalmitatesynthesis[1].GSK2194069(5μMand20μM)showshigherefficacyinFASN-positiveLNCaPcellsratherthanFASN-negativePC3cells,withthehigherFASNExpressionlevelinLNCaPcells[2].GSK2194069(50μM;24h)inhibitsthegrowthofLNCaP-LN3humanprostatecancercells[3].GSK2194069(60.4nM;24h)displayspropertiesofmetabolomics,includingL-acetylcarnitine,stearoylcarnitine,vaccenylcarnitine,andpalmitoyl-L-carnitinedecreaseinLNCaP-LN3cells[3].WesternBlotAnalysis[1]CellLine:A549Concentration:0,10,100,1000nMIncubationTime:48hoursor120hoursResult:Didn’tdecreaseFASproteinlevel.WesternBlotAnalysis[2]CellLine:FASN-positiveLNCaPcells,andFASN-negativePC3cellsConcentration:1nM-0.1mMIncubationTime:48hoursResult:Inhibitedtumorcellsgrowthsignificantly,andreducedLNCaPcellsmuchbetter.户使⽤本产品发表的科研⽂献•AnalChem.2020Mar17;92(6):4419-4426.•PLoSOne.2017Jul13;12(7):e0181243.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESeemorecustomervalidationsonwww.MedChemEREFERENCES[1].KellyJM,etal.SynthesisandEvaluationof11C-LabeledTriazolonesasProbesforImagingFattyAcidSynthaseExpressionbyPositronEmissionTomography.Molecules.2022Feb25;27(5):1552.[2].OhJE,etal.DecipheringFattyAcidSynthaseInhibition-TriggeredMetabolicFlexibilityinProstateCancerCellsthroughUntargetedMetabolomics.Cells.2020Nov10;9(11):2447.[3].HardwickeMA,etal.Ahumanfattyacidsynthaseinhibitorbindsβ-ketoacylreductaseintheketo-substratesite.NatChemBiol.2014Sep;10(9):774-9.McePdfHeightCaution:Producthasnotbeenfu