ML265
| 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 |
| 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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