ZZW-115-hydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEZZW-115hydrochlorideCat.No.:HY-111838ACASNo.:10122-45-9分⼦式:C₂₄H₃₄Cl₃F₃N₄S分⼦量:573.97作⽤靶点:Apoptosis作⽤通路:Apoptosis储存⽅式:4°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性数据体外实验DMSO:83.33mg/mL(145.18mM;Needultrasonic)H2O:60mg/mL(104.54mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.7423mL8.7113mL17.4225mL5mM0.3485mL1.7423mL3.4845mL10mM0.1742mL0.8711mL1.7423mL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(storedundernitrogen)。-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(10.89mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥6.25mg/mL(10.89mM);Clearsolution3.请依序添加每种溶剂：PBSSolubility:50mg/mL(87.11mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性ZZW-115hydrochloride⼀种有效的NUPR1抑制剂，Kd为2.1μM，通过坏死和凋亡(apoptosis)诱导肿瘤细胞死亡。具有抗癌活性。体外研究ZZW-115hydrochloride(0.1-33μM;72hours)isefficientinkillingcancercells,withanIC50intherangeof0.84μM(ANOR)to4.93μM(HN14)[1].ZZW-115hydrochloride(0-100μM;24-72hours)isefficienttokillthesetumorcellswithanIC50intherangeof0.42μM(Hep2Gcells)to7.75μM(SaOS-2cells)[1].ZZW-115hydrochlorideinducespancreaticcelldeathbynecrosisandapoptosis.ZZW-115hydrochloridetreatmentinducesadecreaseinATPproductionandinducesaROSoverproduction[1].LDHreleaseissignificantlyhigherinZZW-115hydrochloride-treatedcells(MiaPaCa-2,02-063,LIPC,Foie8b,andHN14cells)thanincontrolcellsinaconcentration-dependentmanner.Similarly,caspase3/7activityisalsogreaterinZZW-115hydrochloride-treatedcells.TheseexperimentsdemonstratedthatZZW-115hydrochlorideexertedbothpronecroticandproapoptoticeffects[1].CellViabilityAssay[1]CellLine:ANORcells,MiaPaCa-2,02-063,01008,LIPC,02136,HN01,01046,AOIPC,Foie8b,HN14cellsConcentration:0.1-33μMIncubationTime:72hoursResult:Wasefficientinkillingcancercells,withanIC50intherangeof0.84μM(ANOR)to4.93μM(HN14).CellProliferationAssay[1]CellLine:U87,A375,U2OS,SaOS-2,HT29,SK-CO-1,LS174T,H1299andH358,HepG2,PC3,THP-1,Daudi,JurkatandMDA-MB-231cellsConcentration:0-100μMIncubationTime:24or72hoursResult:WasefficienttokillthesetumorcellswithanIC50intherangeof0.42μM(Hep2Gcells)to7.75μM(SaOS-2cells).体内研究ZZW-115hydrochloride(0.5-5mg/kg;injection;dailyfor30days)inhibitsthegrowthofpancreaticxenograftedtumors[1].2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEZZW-115hydrochloride(5mg/kgfor30days;immunocompetentC57BL/6micewereorthotopicallyimplantedwithPanc02cells)treatmentshowsthetumorsizeisalmostunmeasurableinsomecases[1].AnimalModel:NMRI-Foxn1nu/Foxn1numice(nudemice)xenograftedwithMiaPaCa-2cells[1]Dosage:5,2.5,1.0,or0.5mg/kgAdministration:Injection;dailyfor30daysResult:Whenthemicewereinjectedwith5mg/kgZZW-115hydrochloride,thetumorsstoppedgrowingafewdaysaftertreatmentandtheirsizedecreasedprogressively,almostdisappearingattheendofthetreatment.户使⽤本产品发表的科研⽂献•BMCMed.2022Oct19;20(1):365.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].Santofimia-CastañoP,etal.Ligand-baseddesignidentifiesapotentNUPR1inhibitorexertinganticanceractivityvianecroptosis.JClinInvest.2019;129(6):2500-2513.Published2019Mar28.[2].Santofimia-CastañoP,etal.TargetingtheStress-InducedProteinNUPR1toTreatPancreaticAdenocarcinoma.Cells.2019;8(11):1453.Published2019Nov17.McePdf