CAS:1802977-61-2GNE-140 racemate

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GNE-140 racemate is a LDHA inhibitor.

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18817579266

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18817579266

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实验数据

技术信息

CAS号

1802977-61-2

储存条件

分子式

C25H23ClN2O3S2

运输

蓝冰

分子量

499.04

别名

溶解度

DMSO	34.0 mg/mL (68.1 mM)

动物实验配方

生物活性

描述GNE-140 racemate is a potent lactate dehydrogenase A (LDHA) inhibitor. LDHA is a key glycolytic enzyme, a hallmark of aggressive cancers, and believed to be the major enzyme responsible for pyruvate-to-lactate conversion^[2]. 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^[3].