USP7-USP47-inhibitor-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEUSP7/USP47inhibitorCat.No.:HY-13487CASNo.:1247825-37-1分⼦式:C₁₈H₁₁Cl₂N₃O₃S₃分⼦量:484.4作⽤靶点:Deubiquitinase作⽤通路:CellCycle/DNADamage储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:50mg/mL(103.22mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.0644mL10.3220mL20.6441mL5mM0.4129mL2.0644mL4.1288mL10mM0.2064mL1.0322mL2.0644mL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>>90%cornoilSolubility:≥2.5mg/mL(5.16mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性USP7/USP47inhibitor⼀种选择性的泛素蛋⽩特异性蛋⽩酶7/47(USP7/USP47)抑制剂，EC50值分别为0.42μM和1.0μM。IC50&TargetEC50:0.42μM(USP7),1.0μM(USP47)[1]体外研究USP7/USP47inhibitor(compound14)isaselectiveinhibitorofUSP7/USP47withEC50sof0.42μMand1μM,respectively.USP7/USP47inhibitordoesnotinhibitcaspase3,calpain1,20Sproteasome,andapanelofrepresentativeUSPs(USP2,USP5,USP8,USP21,andUSP28;EC50>31.6μM).USP7/USP47inhibitorinhibitsthegrowthofHCT-116cellswithanEC50of7.6μM[1].PROTOCOLKinaseAssay[1]Thecloning,expressionandpurificationofUSP21fromBL21(DE3)bacteriaareperformedusingstandardmolecularbiologytechniques.USP2,USP5,USP7,USP8,USP28,USP47,Ub-PLA2(Ub-CHOP)andUb-EKL(Ub-CHOP2)aregenerated.Caspase3andthecaspase3substrateDEVD-Rh110areused.Deubiquitylatingenzyme,cathepsinBand20Sproteasomechymotrypsinlikeproteaseactivitiesaremeasured.Caspase3activityisdeterminedusingasimilarprotocol.Briefly,doserangesofcompound(includingUSP7/USP47inhibitor)areincubatedwithcaspase3for30minutesbeforetheadditionofDEVD-Rh110andreadingonafluorometricplatereaderusingexcitationandemissionmaximaof485nmand531nmrespectively.Thefinalconcentrationsofcaspase3andDEVD-Rh110are2nMand100nMrespectively[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•CellChemBiol.2021Apr27;S2451-9456(21)00213-0.•JMedChem.2022Oct11.•HarvardMedicalSchoolLINCSLIBRARYSeemorecustomervalidationsonwww.MedChemEREFERENCES[1].WeinstockJ,etal.SelectiveDualInhibitorsoftheCancer-RelatedDeubiquitylatingProteasesUSP7andUSP47.ACSMedChemLett.2012Sep11;3(10):789-92.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalap