RGB-286147-DataSheet-生命科學(xué)試劑-MCE

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemERGB-286147Cat.No.:HY-112346CASNo.:784211-09-2分?式:C??H??Cl?N?O?分?量:473.35作?靶點:CDK;Apoptosis作?通路:CellCycle/DNADamage;Apoptosis儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性RGB-286147?種選擇性和ATP競爭性CDK和CDK相關(guān)激酶(CRK)抑制劑，IC50值范為9-839nM。RGB-286147對其他?CDK/CRK激酶的活性較低。RGB-286147誘導(dǎo)細(xì)胞凋亡(apoptosis)，并具有抗腫瘤活性。IC50&TargetCDK1/cyclinBCDK2/ECDK4/D1cdk6/cyclinD348nM(IC50)15nM(IC50)839nM(IC50)232nM(IC50)體外研究RGB-286147(50-100nM;24-48hr)inducescellcyclearrestintheG1phase,causesamarkedinhibitionofDNAreplication,andinducesapoptosisinHCT116cells[1].RGB-286147(100nM;48hr)resultsinproteolyticcleavageofPARPinHCT116cells[1].RGB-286147(24-72hr)showspotentandirreversiblecellkillingactivityinHCT116cells.TheIC50valueforinhibitionofcolonyformationbyRGB-286147is57nM[1].RGB-286147(48hr)exhibitsbroadanti-tumoractivitywithanaverageGI50valueof50valueof40nM[1].CellCycleAnalysis[1]CellLine:HCT116cellsConcentration:50nMand100nMIncubationTime:24or48hrResult:CausedamarkedinhibitionofDNAreplicationandinducedcellcyclearrest.WesternBlotAnalysis[1]1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECellLine:HCT116cellsConcentration:100nMIncubationTime:48hrResult:ResultedinproteolyticcleavageofPARP.REFERENCES[1].MaureenCaligiuri,etal.Aproteome-wideCDK/CRK-specifickinaseinhibitorpromotestumorcelldeathintheabsenceofcellcycleprogression.ChemBiol.2005Oct;12(10):1103-15.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792;02