STAT3-IN-1-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemESTAT3-IN-1Cat.No.:HY-100753CASNo.:2059952-75-7分⼦式:C₂₈H₂₉NO₆分⼦量:475.53作⽤靶点:STAT;Apoptosis作⽤通路:JAK/STATSignaling;StemCell/Wnt;Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:125mg/mL(262.86mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.1029mL10.5146mL21.0292mL5mM0.4206mL2.1029mL4.2058mL10mM0.2103mL1.0515mL2.1029mL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%salineSolubility:6.25mg/mL(13.14mM);Suspendedsolution;Needultrasonic1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性STAT3-IN-1(compound7d)强效的、选择性的、⼝服有效的STAT3的抑制剂，其在HT29和MDA-MB231细胞中的IC50值分别为1.82μM和2.14μM。STAT3-IN-1(compound7d)可诱导肿瘤细胞凋亡。IC50&TargetStat-3Stat-31.82μM(IC50,inHT29cells)2.14μM(IC50,inMDA-MB231cells)体外研究STAT3-IN-1(compound7d:0-10μM,48h)inhibitstheSTAT3acetylationatlysine685andaffecteditsspecificgenesexpressions[1].STAT3-IN-1(compound7d:0-10μM,48h)inducestumorcellsapoptosisinMDA-MB-231cells[1].ApoptosisAnalysis[1]CellLine:MDA-MB-231celllines.Concentration:0-10μM.IncubationTime:48hours.Result:Theinducedapoptosisrates(earlyandlateapoptosis)at1,2,5,8and10μMwere9.0%,11.2%,20.9%,43.3%and85.2%versuscontrol3.0%.WesternBlotAnalysis[1]CellLine:MDA-MB-231andHT-29celllines.Concentration:0-10μM.IncubationTime:48hours.Result:InhibitedSTAT3acetylationandSTAT3tyrosinephosphorylationinMDA-MB-231cells.Increasedtheexpressionsofthesetumor-suppressorgenes(PTPN6(SHP-1),CDKN2AandDLEC1)whichwererelatedtoSTAT3acetylationatLys685.体内研究STAT3-IN-1(compound7d:10,20mg/kg,twoweeks)arreststumorgrowthwithlowtoxicityinmouse-xenograftmodel[1].AnimalModel:Mouse-xenograftmodelbearinginoculationofmicebreastcancer4T1cells[1].Dosage:10,20mg/kg.Administration:Oraladministrationonceeveryotherdayfortwoweeks.Result:Arrestedtumorgrowthwithnoobviousbodyweightloss.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE户使⽤本产品发表的科研⽂献•RedoxBiol.3September2022,102461.•BiochemPharmacol.2020Oct;180:114126.•CellBiolInt.2021May18.•ResearchSquarePrint.2022May.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].LiS,etal.Discoveryoforal-availableresveratrol-caffeicacidbasedhybridsinhibitingacetylatedandphosphorylatedSTAT3protein.EurJMedChem.2016Nov29;124:1006-1018.McePdfHeightCaution:Producthasnotbeenfullyvalidatedform