| 產(chǎn)品編號(hào) | D51598 |
| 英文名稱 | R-GNE-140 |
| 中文名稱 | |
| 別 名 | LDHA抑制劑 |
| 克 隆 號(hào) | |
| CAS | 2003234-63-5 |
| 理論分子量 | 499.04 kDa |
| 檢測(cè)分子量 | |
| 性 狀 | Lyophilized |
| 保存條件 | Store in dry, dark place for one year. |
| 注意事項(xiàng) | This product as supplied is intended for research use only, not for use in human, therapeutic or diagnostic applications. |
| 產(chǎn)品介紹 |
R-GNE-140 a novel potent lactate dehydrogenase (LDHA) inhibitor with IC50 3nM for LDHA and 5 nM for LDHB. 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. |
