Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemECSN5i-3Cat.No.:HY-112134CASNo.:2375740-98-8分?式:C??H??F?N?O?分?量:505.56作?靶點:Others作?通路:Others儲存?式:-20°C,protectfromlight,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light,storedundernitrogen)溶解性數(shù)據(jù)體外實驗DMSO:≥100mg/mL(197.80mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.9780mL9.8900mL19.7800mL5mM0.3956mL1.9780mL3.9560mL10mM0.1978mL0.9890mL1.9780mL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(fù)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(protectfromlight,storedundernitrogen)。-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(dāng)?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(dāng)保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)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:≥2.5mg/mL(4.95mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%cornoil1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(4.95mM);ClearsolutionBIOLOGICALACTIVITY?物活性CSN5i-3?種有效的，選擇性和?服的CSN5/Jab1抑制劑，抑制CSN催化的Cul1deneddylationIC50值為5.8nM[1]。IC50&TargetIC50:5.8nM(CSN5)[1]體外研究CSN5i-3trapsCRLsintheneddylatedstate,whichleadstoinactivationofasubsetofCRLsbyinducingdegradationoftheirsubstraterecognitionmodule[1].體內(nèi)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.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?SciImmunol.2021Apr30;6(58):eabe2933.?BiochemBiophysResCommun.2022.?bioRxiv.August09,2021.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].SchlierfA,etal.TargetedinhibitionoftheCOP9signalosomefortreatmentofcancer.NatCommun.2016Oct24;7:13166.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalap