iMQT-020-生命科学试剂-MCE.pdfVIP

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  • 2026-02-03 发布于上海
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Inhibitors•ScreeningLibraries•Proteins

www.MedChemE

iMQT_020

Cat.No.:HY-179557

CASNo.:2463893-46-9

分⼦式:C₁₄H₈ClFN₂O₃

分⼦量:306.68

作⽤靶点:GlutathionePeroxidase;ReactiveOxygenSpecies(ROS);

Apoptosis;Ferroptosis;PD-1/PD-L1

作⽤通路:Apoptosis;MetabolicEnzyme/Protease;

Immunology/Inflammation;NF-κB

储存⽅式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

⽣物活性iMQT_020是⼀种选择性变构SLC1A5_var抑制剂。iMQT_020可破坏SLC1A5_var的三聚体组装,导致癌细

胞代谢危机并选择性抑制其⽣长。iMQT_020可降低⾕氨酰胺的补充代谢和氧化磷酸化,从⽽⼴泛扰乱癌细胞

的代谢。iMQT_020可降低GSH⽔平并增加细胞内ROS和线粒体ROS的⽔平。iMQT_020可诱导细胞凋亡(

apoptosis)和铁死亡(ferroptosis)。iMQT_020可通过表观遗传机制上调PD-L1的表达。iMQT_020可⽤于胰

腺癌,肺癌和结肠癌的研究[1]。

体外研究iMQT_020showsthestrongestinhibitoryeffectonmitochondrialglutamineuptake(IC50=6.156μM)ata

concentrationof10μM[1].

iMQT_020(0-100μM)directlybindstoSLC1A5_varWTprotein(Kd=4.473μM),butdoesnotbindto

FIL/AAAmutants[1].

iMQT_020(4μM)significantlyreducestheCDsignaloftheSLC1A5_varWTprotein,indicatingastructural

change[1].

iMQT_020(10μM)reducesglutamine-derivedTCAcycl

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