PFKFB4-IN-1-生命科学试剂-MCE.pdfVIP

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PFKFB4-IN-1

Cat.No.:HY-178367

CASNo.:2664831-55-2

分⼦式:C₁₁H₆N₆O₆

分⼦量:318.2

作⽤靶点:Phosphatase;Apoptosis;Caspase;PARP

作⽤通路:MetabolicEnzyme/Protease;Apoptosis;CellCycle/DNA

Damage;Epigenetics

储存⽅式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

⽣物活性PFKFB4-IN-1是⼀种⾼效且选择性的ATP竞争性PFKFB4抑制剂(IC50=4.50μM)，可降低细胞内PFKFB4蛋

⽩⽔平。PFKFB4-IN-1对PFKFB1/4和PFKFB3/4亚型的选择性超过12倍。PFKFB4-IN-1可抑制癌细胞增殖、

诱导细胞凋亡(apoptosis)并抑制细胞迁移。PFKFB4-IN-1可抑制MDA-MB-231异种移植⼩⿏模型中肿瘤⽣长

。PFKFB4-IN-1可⽤于乳腺癌、肺癌和肝癌的相关研究[1]。

IC50TargetPFKFB4

4.50μM(IC50)

体外研究PFKFB4-IN-1(compound2v)(2-100μM,72h)demonstratesbroad-spectrumanticanceractivity,withIC50

valuesof4.02μM(MCF-7),11.07μM(HepG2),and11.2μM(A549),whileshowingsignificantlylower

cytotoxicitytowardnormalhumanlivercells(HL7702,IC5050μM)[1].

PFKFB4-IN-1(0-48h)inhibitsproliferationofMCF-7breastcancercellsinbothtime-andconcentration-

dependentmanner[1].

PFKFB4-IN-1(6-18μM,24h)inhibitsbothmigrationandcolonyformation,andinducesapoptosisinMCF