RA190-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemERA190Cat.No.:HY-100739CASNo.:1617495-03-0分⼦式:C₂₈H₂₃Cl₅N₂O₂分⼦量:596.76作⽤靶点:Proteasome作⽤通路:MetabolicEnzyme/Protease储存⽅式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验DMSO:≥100mg/mL(167.57mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM1.6757mL8.3786mL16.7572mL5mM0.3351mL1.6757mL3.3514mL10mM0.1676mL0.8379mL1.6757mL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(sealedstorage,awayfrommoisture)。-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:≥2.38mg/mL(3.99mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性RA190双亚苄哌啶，通过与泛素受体RPN13的半胱氨酸88共价结合来抑制蛋⽩酶体功能。IC50&TargetIC50:0.15μM(HeLacell)体外研究RA190covalentlybindstocysteine88ofubiquitinreceptorRPN13inthe19Sregulatoryparticleandinhibitsproteasomefunction,triggeringrapidaccumulationofpolyubiquitinatedproteins.Multiplemyeloma(MM)lines,eventhoseresistanttobortezomib,aresensitivetoRA190viaendoplasmicreticulumstress-relatedapoptosis.RA190stabilizestargetsofhumanpapillomavirus(HPV)E6oncoprotein,andpreferentiallykillsHPV-transformedcells[1].体内研究RA190distributestoplasmaandmajororgansexceptingbrain,andinhibitsproteasomefunctioninskinandmuscle.RA190administrationprofoundlyreducesgrowthofmultiplemyelomaandovariancancerxenografts,andoralRA190treatmentretardsHPV16+syngeneicmousetumorgrowth,withoutimpactingspontaneousHPV-specificCD8+Tcellresponses[1].PROTOCOLCellAssay[1]RA190isdissolvedinDMSOanddilutedwithcellculturemedium.HeLacellsaretreatedwithRA190(0.2,0.4,0.6,0.8,1,2,3,4,5μM)for48hr.Cellviabilityisassayedusingcommericalkit[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalMice:Micearedividedintotwogroupsandtreateddailyi.p.withRA190(10mg/kg)orvehicle,andimagedAdministration[1]againonday7andday14.NOGmice(5pergroup)areinoculatedwith1X106NCI-H929-GFP-Luccellsi.v.,andafter4weeks,miceareimagedfortheirluciferaseactivityanddividedintotwogroups.Micearetreatedi.p.withRA190(20mg/kg)orvehicle,andimagedagainattheendofthetreatmentfortheirluciferaseactivity[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•JVirol.2021Feb3;JVI.02399-20.•KaohsiungJMedSci.2021Jan;37(1):47-54.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].AnchooriRK,etal.Abis-benzylidinepiperidonetargetingproteasomeubiquitinreceptorRPN13/ADRM1asatherapyforcancer.CancerCell.2013Dec9;24(6):791-805.McePdfHeight2/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECaution:Producthasnotbeenfully