Cas No.: | 1809794-70-4 |
Chemical Name: | GNE-140 racemic |
Synonyms: | 3-((2-Chlorophenyl)thio)-4-hydroxy-6-(4-morpholinophenyl)-6-(thiophen-3-yl)-5,6-dihydropyridin-2(1H)-one;BCP20732;BDBM50534334;OC1=C(SC2=C(Cl)C=CC=C2)C(=O)NC(C1)(C1=CSC=C1)C1=CC=C(C=C1)N1CCOCC1;(2R)-5-(2-chlorophenyl)sulfanyl-4-hydroxy-2-(4-morpholin-4-ylphenyl)-2-thiophen-3-yl-1,3-dihydropyri;GNE-140 racemic |
SMILES: | ClC1=C([H])C([H])=C([H])C([H])=C1SC1C(N([H])C(C2=C([H])SC([H])=C2[H])(C2C([H])=C([H])C(=C([H])C=2[H])N2C([H])([H])C([H])([H])OC([H])([H])C2([H])[H])C([H])([H])C=1O[H])=O |
Formula: | C25H23ClN2O3S2 |
M.Wt: | 499.0447 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | 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. |