Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemERA190Cat.No.:HY-100739CASNo.:1617495-03-0分?式:C??H??Cl?N?O?分?量:596.76作?靶點:Proteasome作?通路:MetabolicEnzyme/Protease儲存?式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性數(shù)據(jù)體外實驗DMSO:≥100mg/mL(167.57mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.6757mL8.3786mL16.7572mL5mM0.3351mL1.6757mL3.3514mL10mM0.1676mL0.8379mL1.6757mL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(sealedstorage,awayfrommoisture)。-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?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，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；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:≥2.38mg/mL(3.99mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性RA190雙亞芐哌啶，通過與泛素受體RPN13的半胱氨酸88共價結(jié)合來抑制蛋?酶體功能。IC50&TargetIC50:0.15μM(HeLacell)體外研究RA190covalentlybindstocysteine88ofubiquitinreceptorRPN13inthe19Sregulatoryparticleandinhibitsproteasomefunction,triggeringrapidaccumulationofpolyubiquitinatedproteins.Multiplemyeloma(MM)lines,eventhoseresistanttobortezomib,aresensitivetoRA190viaendoplasmicreticulumstress-relatedapoptosis.RA190stabilizestargetsofhumanpapillomavirus(HPV)E6oncoprotein,andpreferentiallykillsHPV-transformedcells[1].體內(nèi)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.戶使?本產(chǎn)品發(fā)表的科研?獻?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?邊的抑制劑?師www.MedChemECaution:Producthasnotbeenfully