MALT1-inhibitor-MI-2-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEMALT1inhibitorMI-2Cat.No.:HY-12276CASNo.:1047953-91-2分⼦式:C₁₉H₁₇Cl₃N₄O₃分⼦量:455.72作⽤靶点:MALT1作⽤通路:MetabolicEnzyme/Protease;NF-κB储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥46mg/mL(100.94mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM2.1943mL10.9716mL21.9433mL5mM0.4389mL2.1943mL4.3887mL10mM0.2194mL1.0972mL2.1943mL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%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(5.49mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.49mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性MALT1inhibitorMI-2⼀种MALT1抑制剂(IC50=5.84μM)，MALT1inhibitorMI-2直接与MALT1结合，不可逆地抑制蛋⽩酶功能，并伴有NF-κB报告⼦活性抑制、c-REL核定位抑制和NF-κB靶因下调。MALT1inhibitorMI-2对动物⽆毒[1]。IC50&TargetIC50:5.84μM(MALT1)[1]体外研究MALT1inhibitorMI-2(1-1000nM;48hours)selectivelysuppressesMALT1-dependentDLBCLcelllines,andtheGI50inHBL-1,TMD8,OCI-Ly3,andOCI-Ly10cellsis0.2,0.5,0.4,and0.4µM,respectively[1].MALT1inhibitorMI-2(62-1000nM;24hours)causesadose-dependentdecreaseinMALT1-mediatedcleavage[1].CellProliferationAssay[1]CellLine:HBL-1,TMD8,OCI-Ly3,OCI-Ly10cellsConcentration:1,10,100,1000nMIncubationTime:48hoursResult:TheGI50inHBL-1,TMD8,OCI-Ly3,andOCI-Ly10cellswas0.2,0.5,0.4,and0.4µM,respectively.WesternBlotAnalysis[1]CellLine:HBL-1cellsConcentration:62,125,250,500,1000nMIncubationTime:24hoursResult:InhibitsMALT1cleavageofCYLDinHBL-1cells.体内研究MALT1inhibitorMI-2(25mg/kg;i.p.;dailyfor14days)profoundlysuppressesthegrowthofboththeTMD8andHBL-1ABC-DLBCLxenografts[1].AnimalModel:Eight-week-oldmaleSCIDNOD(bearingHBL-1andTMD8cells)[1]Dosage:25mg/kgAdministration:Intraperitonealinjection;dailyfor14days2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEResult:ProfoundlysuppressedthegrowthofboththeTMD8andHBL-1ABC-DLBCLxenograftsversusvehicle.户使⽤本产品发表的科研⽂献•JVirol.2019Nov26;93(24):e01499-19.•FrontMicrobiol.2021Feb2;12:607451.•ParasitVectors.2018May18;11(1):305.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].FontanL,etal.MALT1smallmoleculeinhibitorsspecificallysuppressABC-DLBCLinvitroandinvivo.CancerCell.2012Dec11;22(6):812-24.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedic