tBID-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEtBIDCat.No.:HY-100464CASNo.:1639895-85-4分⼦式:C₁₁H₃Br₄N₃O₂分⼦量:528.78作⽤靶点:DYRK作⽤通路:ProteinTyrosineKinase/RTK储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:20mg/mL(37.82mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.8911mL9.4557mL18.9115mL5mM0.3782mL1.8911mL3.7823mL10mM0.1891mL0.9456mL1.8911mL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。BIOLOGICALACTIVITY⽣物活性tBID同结构域相互作⽤蛋⽩激酶2(HIPK2)的选择性抑制剂，IC50值为0.33μM。IC50&TargetIC50:0.33µM(HIPK2)[1]体外研究Homeodomain-interactingproteinkinase2(HIPK2)isaSer/Thrkinasecontrollingcellproliferationand1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEsurvival.TBID,displaystowardHIPK2unprecedentedefficacy(IC50=0.33µM)andselectivity(Ginicoefficient0.592outofapanelof76kinases).ThetwoothermembersoftheHIPKfamily,HIPK1andHIPK3,arealsoinhibitedbyTBIDalbeitlessefficientlythanHIPK2.ThemodeofactionofTBIDiscompetitivewithrespecttoATP,consistentwithmodelling.TBIDinteractswiththehingeregionthroughhydrophobicinteractionsbetweenVal213,Val261,Phe277,Leu280,Met331,Ile345,andthetetrabrominemoiety,whilethesymmetricnitrogenatomatposition3interactswiththecatalyticLys228,thusplayingacrucialroleinthebindingarchitecture[1].PROTOCOLCellAssay[1]HepG2cells(humanhepatocellularcarcinoma)areculturedinDulbecco'smodifiedEagle'smediumsupplementedwith10%fetalcalfserum,2mML-glutamine,100unit/mLpenicillinand100µg/mLstreptomycin.TreatmentswithTBIDareperformedinthesamemediumbutwith1%fetalcalfserum;controlcellsaretreatedwiththesolvent(DMSO).CellviabilityisevaluatedbymeansofMTT[1]MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•EBioMedicine.2022Sep28;85:104274.•ExpTherMed.2020Dec;20(6):171.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].CozzaG,etal.Synthesisandpropertiesofaselectiveinhibitorofhomeodomain-interactingproteinkinase2(HIPK2).PLoSOne.2014Feb24;9(2):e89176.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresea