CSN5i-3-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemECSN5i-3Cat.No.:HY-112134CASNo.:2375740-98-8分⼦式:C₂₈H₂₉F₂N₅O₂分⼦量:505.56作⽤靶点:Others作⽤通路:Others储存⽅式:-20°C,protectfromlight,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light,storedundernitrogen)溶解性数据体外实验DMSO:≥100mg/mL(197.80mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM1.9780mL9.8900mL19.7800mL5mM0.3956mL1.9780mL3.9560mL10mM0.1978mL0.9890mL1.9780mL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,storedundernitrogen)。-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:≥2.5mg/mL(4.95mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoil1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(4.95mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性CSN5i-3⼀种有效的，选择性和⼝服的CSN5/Jab1抑制剂，抑制CSN催化的Cul1deneddylationIC50值为5.8nM[1]。IC50&TargetIC50:5.8nM(CSN5)[1]体外研究CSN5i-3trapsCRLsintheneddylatedstate,whichleadstoinactivationofasubsetofCRLsbyinducingdegradationoftheirsubstraterecognitionmodule[1].体内研究CSN5i-3showsagoodpharmacokineticprofile.CSN5i-3inhibitsgrowthofhumanxenograft.TreatmentwithCSN5i-3triggerstheformationofcleavedPARPandcleavedcaspase3indicativeofapoptosisinduction[1].PROTOCOLCellAssayCellviabilityismeasuredusingtheCellTiter-GloAssay.Cells(THP-1,HCT116,NCI-H2030andTE-1)aretreatedwithCSN5i-3(1nM,10nM,100nM,1μM,10μM)for72hours[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalMice[1]Administration[1]SU-DHL-1xenograftsweregrowninSCID-bgmiceanddosedbyoraladministrationwitheithervehiclecontrolorCSN5i-3attheindicateddoses(50mg/kgBID,100mg/kgQD)andschedules(3,7,10,14day).Tumourresponseisreportedaspercentagechangeintumourvolumeatthelastdayoftreatmentrelativetostartoftreatment.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•SciImmunol.2021Apr30;6(58):eabe2933.•BiochemBiophysResCommun.2022.•bioRxiv.August09,2021.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].SchlierfA,etal.TargetedinhibitionoftheCOP9signalosomefortreatmentofcancer.NatCommun.2016Oct24;7:13166.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalap