tBID-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEtBIDCat.No.:HY-100464CASNo.:1639895-85-4分?式:C??H?Br?N?O?分?量:528.78作?靶點(diǎn):DYRK作?通路:ProteinTyrosineKinase/RTK儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:20mg/mL(37.82mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.8911mL9.4557mL18.9115mL5mM0.3782mL1.8911mL3.7823mL10mM0.1891mL0.9456mL1.8911mL請(qǐng)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(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。BIOLOGICALACTIVITY?物活性tBID同結(jié)構(gòu)域相互作?蛋?激酶2(HIPK2)的選擇性抑制劑，IC50值為0.33μM。IC50&TargetIC50:0.33μM(HIPK2)[1]體外研究Homeodomain-interactingproteinkinase2(HIPK2)isaSer/Thrkinasecontrollingcellproliferationand1/2MasterofBioactiveMolecules—您?邊的抑制劑?師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.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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