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

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEhnRNPK-IN-1Cat.No.:HY-135691CASNo.:2313528-04-8分⼦式:C₂₃H₂₁N₃O₅分⼦量:419.43作⽤靶点:c-Myc;Apoptosis作⽤通路:Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:5mg/mL(11.92mM;ultrasonicandwarmingandheatto80°C)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.3842mL11.9209mL23.8419mL5mM0.4768mL2.3842mL4.7684mL10mM0.2384mL1.1921mL2.3842mL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hnRNPK-IN-1⼀种异质核糖核蛋⽩K(hnRNPK)结合配体，⽤SPR和MST测量的Kd值分别为4.6μM和2.6μM。hnRNPK-IN-1通过破坏hnRNPK和c-myc启动⼦的结合来抑制c-myc转录。hnRNPK-IN-1诱导Hela细胞凋亡(apoptosis)，并具有很强的抗肿瘤活性。IC50&TargetKd:4.6μM(hnRNPK;SPRassay)and2.6μM(hnRNPK;MSTassay)[1]1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE体外研究hnRNPK-IN-1(Compound25;1.25-5μM;24hours)treatmentinducesHelacellsapoptosiscouldbeduetoitsrepressionofcmyctranscription[1].hnRNPK-IN-1(1.25-5μM;48hours)treatmentdown-regulatesc-mycgenetranscriptionandexpressioninHelacellsinadose-dependentmanner[1].hnRNPK-IN-1showsaselectiveanti-proliferativeeffectonhumancancercelllines(Siha,A549,Hela,U2OS,A375,HuH7andHEK293cells)withIC50valuesrangedfrom1.36to3.59μM[1].hnRNPK-IN-1couldselectivelybindtohnRNPKwithoutsignificantinteractionwithc-mycpromoterDNA.ThebindingofhnRNPK-IN-1tohnRNPKcoulddisrupttheinteractionbetweenhnRNPKandc-mycpromoterDNAinvitroandincells[1].ApoptosisAnalysis[1]CellLine:HelacellsConcentration:1.25μM,2.5μM,5μMIncubationTime:24hoursResult:InducedHelacellsapoptosisandapoptosis-relatedproteinexpressions.RT-PCR[1]CellLine:HelacellsConcentration:1.25μM,2.5μM,5μMIncubationTime:48hoursResult:Causedareductionofc-mycmRNAinadose-dependentmannerinHelacells.WesternBlotAnalysis[1]CellLine:HelacellsConcentration:1.25μM,2.5μM,5μMIncubationTime:48hoursResult:Theexpressionlevelsofc-MYCalsodecreasedinadose-dependentmanner.体内研究hnRNPK-IN-1(Compound25;6.7-20mg/kg;i.p.;onceaday;forthreeweeks)exhibitsgoodtumorgrowthinhibitioninaHelaxenografttumormodel[1].AnimalModel:BALB/cfemalenudemice(fiveweeksold)bearingHelacells[1]Dosage:6.7mg/kg,20mg/kgAdministration:Intraperitonealinjection;onceaday;forthreeweeks2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEResult:InhibitedtumorgrowthinaHelacervicalxenograft.REFERENCES[1].BingShu,etal.SynthesesandevaluationofnewQuinolinederivativesforinhibitionofhnRNPKinregulatingoncogenec-myctranscription.BioorgChem.2019Apr;85:1-17.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedica