hnRNPK-IN-1-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEhnRNPK-IN-1Cat.No.:HY-135691CASNo.:2313528-04-8分?式:C??H??N?O?分?量:419.43作?靶點:c-Myc;Apoptosis作?通路:Apoptosis儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:5mg/mL(11.92mM;ultrasonicandwarmingandheatto80°C)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.3842mL11.9209mL23.8419mL5mM0.4768mL2.3842mL4.7684mL10mM0.2384mL1.1921mL2.3842mL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；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。BIOLOGICALACTIVITY?物活性hnRNPK-IN-1?種異質(zhì)核糖核蛋?K(hnRNPK)結(jié)合配體，?SPR和MST測量的Kd值分別為4.6μM和2.6μM。hnRNPK-IN-1通過破壞hnRNPK和c-myc啟動?的結(jié)合來抑制c-myc轉(zhuǎn)錄。hnRNPK-IN-1誘導(dǎo)Hela細胞凋亡(apoptosis)，并具有很強的抗腫瘤活性。IC50&TargetKd:4.6μM(hnRNPK;SPRassay)and2.6μM(hnRNPK;MSTassay)[1]1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE體外研究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.體內(nèi)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?邊的抑制劑?師www.MedChemEResult:InhibitedtumorgrowthinaHelacervicalxenograft.REFERENCES[1].BingShu,etal.SynthesesandevaluationofnewQuinolinederivativesforinhibitionofhnRNPKinregulatingoncogenec-myctranscription.BioorgChem.2019Apr;85:1-17.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedica