GNE-140 racemic
CAS号 | 1809794-70-4 | 货号 | BCP37998 |
中文名 | GNE-140 racemic | ||
英文名 | GNE-140 racemic | ||
中文别名 | |||
英文别名 | GNE140 racemic;GNE 140 racemic; | ||
分子式 | C25H23ClN2O3S2 | 分子量 | 499.04 |
生物活性 | GNE-140 racemic is a novel potent lactate dehydrogenase (LDHA) inhibitor. In MIA PaCa-2 human pancreatic cells, LDHA inhibition rapidly affected global metabolism, although cell death only occurred after 2 d of continuous LDHA inhibition. Pancreatic cell lines that utilize oxidative phosphorylation (OXPHOS) rather than glycolysis were inherently resistant to GNE-140, but could be resensitized to GNE-140 with the OXPHOS inhibitor phenformin. Acquired resistance to GNE-140 was driven by activation of the AMPK-mTOR-S6K signaling pathway, which led to increased OXPHOS, and inhibitors targeting this pathway could prevent resistance. |
结构式
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