Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEZZW-115hydrochlorideCat.No.:HY-111838ACASNo.:10122-45-9分?式:C??H??Cl?F?N?S分?量:573.97作?靶點:Apoptosis作?通路:Apoptosis儲存?式:4°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性數(shù)據(jù)體外實驗DMSO:83.33mg/mL(145.18mM;Needultrasonic)H2O:60mg/mL(104.54mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.7423mL8.7113mL17.4225mL5mM0.3485mL1.7423mL3.4845mL10mM0.1742mL0.8711mL1.7423mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month(storedundernitrogen)。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥6.25mg/mL(10.89mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥6.25mg/mL(10.89mM);Clearsolution3.請依序添加每種溶劑：PBSSolubility:50mg/mL(87.11mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性ZZW-115hydrochloride?種有效的NUPR1抑制劑，Kd為2.1μM，通過壞死和凋亡(apoptosis)誘導(dǎo)腫瘤細胞死亡。具有抗癌活性。體外研究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).體內(nèi)研究ZZW-115hydrochloride(0.5-5mg/kg;injection;dailyfor30days)inhibitsthegrowthofpancreaticxenograftedtumors[1].2/3MasterofBioactiveMolecules—您?邊的抑制劑?師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.戶使?本產(chǎn)品發(fā)表的科研?獻?BMCMed.2022Oct19;20(1):365.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].Santofimia-Casta?oP,etal.Ligand-baseddesignidentifiesapotentNUPR1inhibitorexertinganticanceractivityvianecroptosis.JClinInvest.2019;129(6):2500-2513.Published2019Mar28.[2].Santofimia-Casta?oP,etal.TargetingtheStress-InducedProteinNUPR1toTreatPancreaticAdenocarcinoma.Cells.2019;8(11):1453.Published2019Nov17.McePdf