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文件名称:CDK2-PIM1-IN-1-生命科学试剂-MCE.pdf
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文档摘要

Hotline:400-820-3792

Inhibitors?ScreeningLibraries?Proteins

www.MedChemE

CDK2/PIM1-IN-1

Cat.No.:HY-173224

分?式:C??H??N?O?

分?量:421.49

作?靶点:CDK;Pim

作?通路:CellCycle/DNADamage;JAK/STATSignaling

储存?式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

?物活性CDK2/PIM1-IN-1是CDK2(IC50:0.27μM)和PIM1(IC50:0.67μM)激酶的抑制剂。CDK2/PIM1-IN-1可诱导

细胞凋亡(apoptosis),并降低促进肿瘤的TNF-α表达。CDK2/PIM1-IN-1具有抗肿瘤活性。

IC50TargetCDK2PIM1

0.27μM(IC50)0.67μM(IC50)

体外研究CDK2/PIM1-IN-1(Compound6b)(24h)showsantiproliferativeeffectsonMCF7cells(IC50:5.54μM),HCT-

116cells(IC50:2.62μM),HepG2cells(IC50:3.99μM)andHeLacelllines(IC50:8.31μM),withmoderate

safetyinthenormalbreastcelllineMCF-10A(IC50:39.44μM)[1].

CDK2/PIM1-IN-1(24h)inhibitsHCT116celllineattheG0-G1phase(%G0-G1:83.43%)andinduced

significantearly(8.28%)andlate(20.09%)cellapoptosis[1].

CDK2/PIM1-IN-1(24h)showsinhibitoryeffectsonbothCDK(IC50:0.27μM)andPIM1(IC50:0.67μM)in

HCT116celllines[1].

CellViabilityAss