Hck-IN-1-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemEHck-IN-1Cat.No.:HY-125028CASNo.:1473404-51-1分⼦式:C₁₆H₁₁ClN₆O₃S分⼦量:402.81作⽤靶点:Src;HIV作⽤通路:ProteinTyrosineKinase/RTK;Anti-infection储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:12.5mg/mL(31.03mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.4826mL12.4128mL24.8256mL5mM0.4965mL2.4826mL4.9651mL10mM0.2483mL1.2413mL2.4826mL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，并请注意储备液的保存⽅式和期限。BIOLOGICALACTIVITY⽣物活性Hck-IN-1(compoundB9)⼀种⼆苯吡唑啉化合物，选择性的Nef依赖性Hck抑制剂，对Nef：Hck复合物和Hck的IC50分别为2.8μM和>20μM。Hck-IN-1⼀种直接且⼴泛的HIV-1Nef拮抗剂，对于野⽣型HIV-1复制的IC50为100-300nM。Hck-IN-1结合⼝袋残Asn126，具有抗逆转录病毒活性。IC50&TargetHIV-1Nef100-300nM(IC50)1/2MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemE体外研究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