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GNE-140 racemic

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产品信息

产品名称：GNE-140 racemic	纯度：98% min
CAS NO：1809794-70-4	溶解度：
分子式：C₂₅H₂₃ClN₂O₃S₂	包装：可按客户要求包装
分子量：499.045	贮存：-20 ℃

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备注说明

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.

参考文献

1: Boudreau A, Purkey HE, Hitz A, Robarge K, Peterson D, Labadie S, Kwong M, Hong
R, Gao M, Del Nagro C, Pusapati R, Ma S, Salphati L, Pang J, Zhou A, Lai T, Li Y,
Chen Z, Wei B, Yen I, Sideris S, McCleland M, Firestein R, Corson L, Vanderbilt
A, Williams S, Daemen A, Belvin M, Eigenbrot C, Jackson PK, Malek S,
Hatzivassiliou G, Sampath D, Evangelista M, O'Brien T. Metabolic plasticity
underpins innate and acquired resistance to LDHA inhibition. Nat Chem Biol. 2016
Oct;12(10):779-86. doi: 10.1038/nchembio.2143. Epub 2016 Aug 1. PubMed PMID:
27479743.