ML265

  • 化学数据
CAS号 1221186-53-3 货号 BCP12877
中文名 ML265
英文名 ML265
中文别名
英文别名 ML 265;ML-265;TEPP-46;TEPP 46;TEPP46; CID44246499; CID-44246499; CID 44246499; NCGC00186528; NCGC 00186528; NCGC-00186528;
分子式 C17H16N4O2S2 分子量 372.46
  • 用途
生物活性 ML265 is a potent PKM2 activator induces tetramerization and reduces tumor formation and size in a mouse xenograft model. Cancer cells have altered metabolic processes compared to normal differentiated cells and the expression of the M2 isozyme of pyruvate kinase (PKM2) plays an important role in this aberrant metabolism. ML265 induces the more active tetrameric state of PKM2 and the X-ray co-crystal structure shows that the activator binds at the dimer-dimer interface between two subunits of PKM2. ML265 was tested in a H1299 mouse xenograft model and showed significant reduction in tumor size, weight, and occurrence with no apparent toxicity over the 7-week experiment.
信号通路 Protease/Metabolic Enzyme 
靶 点 Pyruvate Kinase 

结构式

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