GSK2593074A-GSK-074-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEGSK2593074ACat.No.:HY-122909CASNo.:1337531-06-2Synonyms:GSK'074分⼦式:C₂₇H₂₃N₅OS分⼦量:465.57作⽤靶点:RIPkinase作⽤通路:Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:41.67mg/mL(89.50mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.1479mL10.7395mL21.4790mL5mM0.4296mL2.1479mL4.2958mL10mM0.2148mL1.0740mL2.1479mL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%saline1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.08mg/mL(4.47mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性GSK2593074A(GSK’074)⼀种程序性坏死(necroptosis)抑制剂,抑制RIP1和RIP3[1]。IC50&TargetRIP1,RIP3[1]体外研究GSK2593074A(GSK’074;0.01,0.1,1,10,and100nM;6ꢀhoursforMOVAScells;3hoursforL929cells)completelyrescuescellsfromnecroptosisunderdifferentstimuliinbothhumanandmurinecellsatIC50~3ꢀnM.InmultiplecelltypesincludingmouseSMCs,fibroblasts(L929),bonemarrowderivedmacrophages(BMDM),andhumancolonepithelialcells(HT29),GSK2593074AinhibitsnecroptosiswithanIC50of~3ꢀnM[1].CellViabilityAssay[1]CellLine:MousesmoothmusclecelllineMOVAS;MousefibroblastcelllineL929Concentration:0.01,0.1,1,10,and100nMIncubationTime:6ꢀhoursforMOVAScells;3hoursforL929cellsResult:InhibitedMOVASandL929cellswiththeIC50of3nM.体内研究GSK2593074A(GSK’074;0.93ꢀmg/kg/day;i.p.injection;14or28days)isadministratedtoApoe-/-miceimmediatelyfollowingpumpimplantation.ComparedtotheDMSOgroup,GSK2593074A-treatedmiceshowsignificantlyalleviatedaneurysmformation,reflectedbyamuchsmalleraorticdilatation(DMSO85.39±15.76%vsGSK2593074A36.28±5.76%;P[1].AnimalModel:Apoe-/-femalemice(9-10months)[1]Dosage:0.93ꢀmg/kg/day;200ꢀµLAdministration:Dailyi.p.injection;14or28daysResult:Inhibitedaneurysmformationinmousemodelsofaneurysms.REFERENCES[1].ZhouT,etal.IdentificationofanovelclassofRIP1/RIP3dualinhibitorsthatimpedecelldeathandinflammationinmouseabdominalaorticaneurysmmodels.CellDeathDis.2019Mar6;10(3):226.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.