Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemECDK8-IN-12Cat.No.:HY-148561CASNo.:2613307-67-6分?式:C??H??ClN?O?分?量:381.86作?靶點(diǎn):CDK;GSK-3;PKC作?通路:CellCycle/DNADamage;PI3K/Akt/mTOR;StemCell/Wnt;Epigenetics;TGF-beta/Smad儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性CDK8-IN-12?種具有?服活性的有效CDK8抑制劑，Ki為14nM。CDK8-IN-12對GSK-3α、GSK-3β、PCK-θ具有脫靶激酶抑制作?，Ki分別為13nM、4nM、109nM。CDK8-IN-12選擇性地對MV4-11細(xì)胞顯?出有效的抗增殖作?。CDK8-IN-12?種抗癌劑。IC50&TargetCDK8GSK-3αGSK-3βPKCθ14nM(Ki)13nM(Ki)4nM(Ki)109nM(Ki)體外研究CDK8-IN-12(compound38)selectivelyinhibitstheproliferationofMV4-11acutemyeloidleukaemiacellswithaGI50of0.36μM[1].CDK8-IN-12(0.36,0.72μM;2hours)significantlyreducesthephosphorylationofserine727onSTAT1[1].WesternBlotAnalysis[1]CellLine:MV4-11cellsConcentration:0.36,0.72μMIncubationTime:2hoursResult:Significantlyreducedthephosphorylationofserine727onSTAT1atconcentrationsoftheirrespective1×GI50values,butbarelyaffectedtheleveloftotalSTAT1.體內(nèi)研究CDK8-IN-12(compound38;IV;5mg/kgforratand2mg/kgformouse)hasaT1/2of0.9hoursand0.34hoursforratandmouse,respectively[1].1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEPharmacokineticParametersofCDK8-IN-12[1].IV(Rat5mg/kg)PO(Rat20mg/kg)IV(Mouse2mg/kg)PO(Mouse10mg/kg)Tmax(h)0.042.750.040.42Cmax(μM)14.42.773.445.01AUC0-24(μM?h)9.714.61.392.30T1/2(ng/mL)41.11CL(L/h?kg)1.393.78Vss(L/kg)1.111.99F(%)3833REFERENCES[1].MingfengYu,etal.PotentandorallybioavailableCDK8inhibitors:Design,synthesis,structure-activityrelationshipanalysisandbiologicalevaluation.EurJMedChem.2021Mar15;214:113248.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-37