Hotline:400-820-3792
Inhibitors?ScreeningLibraries?Proteins
www.MedChemE
PLK1-IN-12
Cat.No.:HY-172364
分?式:C??H??ClN?O?
分?量:558.12
作?靶点:Polo-likeKinase(PLK)
作?通路:CellCycle/DNADamage
储存?式:Pleasestoretheproductundertherecommendedconditionsin
theCertificateofAnalysis.
BIOLOGICALACTIVITY
?物活性PLK1-IN-12是?种?选择性、具有?服活性的PLK1抑制剂，IC50为20nM。PLK1-IN-12对PLK1的选择性?
于PLK2(IC50:10000nM)和PLK3(IC50:3953nM)。PLK1-IN-12在?泛的细胞系中表现出抗癌效?。PLK1-
IN-12能够?于抗??病研究。
IC50TargetPLK1PLK2PLK3
20nM(IC50)10000nM(IC50)3953nM(IC50)
体外研究PLK1-IN-12(CompoundB31)(0.508nM-10μM,24h)showsantiproliferativeeffectsinH460(IC50:12nM),
A549(IC50:32nM),SW620(IC50:8.2nM),HL-60(IC50:59nM),K562(IC50:0.08nM)andCCRF-CEM
(IC50:41nM)celllines[1].
PLK1-IN-12(1μM,5min)showsrapidclearanceinhuman,mouseanddoglivermicrosomes(Clint:68.3-
210μL/min/mgprotein)[1].
PLK1-IN-12(0.1-30μM,24h)hasalowinhibitoryeffectonHEK293Tcellsviability(68%)[1].
PLK1-IN-12(0.4-100μM)hasalowinhibitoryeffectonhERGpotassiumchannel