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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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