TRi-1-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemETRi-1Cat.No.:HY-125006CASNo.:246020-68-8分⼦式:C₁₂H₉ClN₂O₅S分⼦量:328.73作⽤靶点:Others作⽤通路:Others储存⽅式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性数据体外实验DMSO:62.5mg/mL(190.13mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.0420mL15.2100mL30.4201mL5mM0.6084mL3.0420mL6.0840mL10mM0.3042mL1.5210mL3.0420mL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(protectfromlight)。-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:≥2.08mg/mL(6.33mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(6.33mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性TRi-1有效的、特异性的、不可逆的胞质硫氧还蛋⽩还原酶1(TXNRD1)的抑制剂，其IC50值为12nM。TRi-1有抗肿瘤活性，且线粒体毒性很⼩。IC50&TargetIC50:12nM(TXNRD1)[1].体外研究TRi-1(0.679and6.79μM;6h)hasnoeffectoncellularglutathione(GSH)concentrationsinFaDucells,efficientlyactivatesJNKandp38phosphorylation[1].TRi-1(2μM)irreversiblyinhibitTXNRD1inanNADPH-dependentmanner[1].TRi-1(0.1-10μM;0-10h)increasescellularH2O2productioninculturedFaDucellsinaconcentration-andtime-dependentmanner[1].TRi-1(10nM-100μM;48h)showscytotoxicitytowardcancercells[1].WesternBlotAnalysis[1]CellLine:FaDucellsConcentration:0.679and6.79μMIncubationTime:6hResult:EfficientlyactivatedJNKandp38phosphorylation.CellCytotoxicityAssay[1]CellLine:Leukemia,non-smallcelllung,CNS,colon,melanoma,ovarian,renal,prostateandbreastcancercellsConcentration:10nM-100μMIncubationTime:48hResult:Displayedpotencyagainsteverycelllinetested,withanaveragegrowthinhibitionto50%(GI50)of6.31μM.体内研究TRi-1(10mg/kg;i.v.;twiceadayfor4daysor5mg/kg;i.p.;twiceaweekfor3weeks)impairesgrowthandviabilityofhumantumorxenograftsandsyngeneicmousetumors[1].AnimalModel:SCIDmicebearingestablishedhumanFaDucellxenografts[1]Dosage:10mg/kgAdministration:Intravenousinjection,twiceadayfor4daysResult:Resultedindecreasedtumorgrowthcomparedtovehiclecontrolswithinfourdayswith2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEnosignsofoverttoxicityorchangesinmouseweightrelativetovehiclecontrol.AnimalModel:PyMT-MMTVmicethatspontaneouslydevelopmalignantbreastcancertumors[1]Dosage:5mg/kgAdministration:Intraperitonealinjection,twiceaweekfor3weeksResult:Impairedtumorgrowth,significantlyreducedtumorvolumes.户使⽤本产品发表的科研⽂献•Antioxidants(Basel).2022Jul19;11(7):1399.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].StaffordWC,etal.Irreversibleinhibitionofcytosolicthioredoxinreductase1asamechanisticbasisforanticancertherapy.SciTranslMed.2018Feb14;10(428).pii:eaaf7444.McePdfHeightCaution:Producthasnotbeenfully