Hck-IN-1-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemEHck-IN-1Cat.No.:HY-125028CASNo.:1473404-51-1分?式:C??H??ClN?O?S分?量:402.81作?靶點:Src;HIV作?通路:ProteinTyrosineKinase/RTK;Anti-infection儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:12.5mg/mL(31.03mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.4826mL12.4128mL24.8256mL5mM0.4965mL2.4826mL4.9651mL10mM0.2483mL1.2413mL2.4826mL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，并請注意儲備液的保存?式和期限。BIOLOGICALACTIVITY?物活性Hck-IN-1(compoundB9)?種?苯吡唑啉化合物，選擇性的Nef依賴性Hck抑制劑，對Nef：Hck復合物和Hck的IC50分別為2.8μM和>20μM。Hck-IN-1?種直接且?泛的HIV-1Nef拮抗劑，對于野?型HIV-1復制的IC50為100-300nM。Hck-IN-1結(jié)合?袋殘Asn126，具有抗逆轉(zhuǎn)錄病毒活性。IC50&TargetHIV-1Nef100-300nM(IC50)1/2MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemE體外研究Hck-IN-1(compoundB9)showsweakactivityagainstotherSrc-familymembersinvitro,withIC50values>20μMforc-Src,LckandLyn[1].B9(1μM;8days)completelyinhibitsNef-dependentSFKactivationataconcentrationof1.0μM[1].Hck-IN-1(0.1,0.3,1,3μM)alsoinhibitsNef-mediatedenhancementofHIV-1infectivityinaconcentration-dependentmannerinthereportercellline,TZM-bl[1].Hck-IN-1inhibitsthereplicationofallelevenHIV-1NefchimeraswithIC50valuesof~300nMinCEM-T4cells,demonstratingthatthecompoundisbroadlyactiveagainstHIVreplicationsupportedbyawiderangeofHIV-1Nefproteins[1].WesternBlotAnalysis[1]CellLine:CEM-T4cellsConcentration:1μMIncubationTime:8daysResult:CompletelyinhibitedNef-dependentSFKactivationataconcentrationof1.0μM.REFERENCES[1].Emert-SedlakLA,etal.Effectorkinasecouplingenableshigh-throughputscreensfordirectHIV-1Nefantagonistswithantiretroviralactivity.ChemBiol.2013Jan24;20(1):82-91.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400