NSD2-H3K36me2-modulator-1-生命科学试剂-MCE.pdfVIP

Hotline:400-820-3792

Inhibitors•ScreeningLibraries•Proteins

www.MedChemE

NSD2/H3K36me2modulator-1

Cat.No.:HY-179427

分⼦式:C₄₁H₅₉ClN₂O₅

分⼦量:695.37

作⽤靶点:HistoneMethyltransferase;Apoptosis;ReactiveOxygen

Species(ROS)

作⽤通路:Epigenetics;Apoptosis;Immunology/Inflammation;Metabolic

Enzyme/Protease;NF-κB

储存⽅式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

⽣物活性NSD2/H3K36me2modulator-1是⼀种⼝服有效的NSD2/H3K36me2调节剂。NSD2/H3K36me2modulator-1

与NSD2的SAM⼝袋竞争性结合，有效抑制NSD2表达并抑制H3K36me2甲基化。NSD2/H3K36me2

modulator-1还能逆转上⽪-间质转化(EMT)，抑制细胞迁移，并诱导G0/G1期阻滞和细胞凋亡(apoptosis)。

NSD2/H3K36me2modulator-1可降低线粒体膜电位(MMP)并导致活性氧(ROS)⽣成。NSD2/H3K36me2

modulator-1可⽤于研究靶向NSD2的表观遗传抗癌策略在肝细胞癌(HCC)中的应⽤[1]。

IC50TargetNSD2

体外研究NSD2/H3K36me2modulator-1(Compound5b)(24h)displaysIC505μMagainstallfivecancercelllines

(IC50valuesof4.67,2.12,2.64,4.56,4.99μMinA549,HepG-2,PC-3,HCT-116,MCF-7cellsrespectively),

confirmingitsexceptionalbroad-spectrumantitumoractivity[1].

NSD2/H3K36me2modulator-1exhibitsahightumorselectivityforHepG-2cellsoverHaCaTcells(IC50

19.2μM)(selectivi