| Cas No.: | 2003234-63-5 |
| Chemical Name: | R-GNE-140 |
| Synonyms: | (R)-GNE-140;(R)-3-((2-chlorophenyl)thio)-4-hydroxy-6-(4-morpholinophenyl)-6-(thiophen-3-yl)-5,6-dihydropyridin-2(1H)-one;(2~{r})-5-(2-Chlorophenyl)sulfanyl-2-(4-Morpholin-4-Ylphenyl)-4-Oxidanyl-2-Thiophen-3-Yl-1,3-Dihydropyridin-6-One;BDBM197160;s6675;AK00798569;J3.623.769D;Q27460797 |
| 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: | 499.04 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | (R)-GNE-140 (GNE-140) is a novel potent, selective lactate dehydrogenase (LDH) inhibitor with IC50 of 3, 5, and 5 nM for LDHA, LDHB, and LDHC, respectively; displays no inhibition on malate MDH-1, MDH-2 (IC50>10 uM for both enzymes), and no appreciable inhibition against a panel of 301 kinases (<50% inhibition at 1 uM); perturbs glycolysis and inhibits proliferation in MIA PaCa-2 cells (IC50=0.43 uM), decreases glucose uptake (IC50=0.47 uM); pancreatic cell lines that utilize oxidative OXPHOS rather than glycolysis are inherently resistant to GNE-140, which can be resensitized to GNE-140 with the OXPHOS inhibitor phenformin. Pancreatic Cancer Phase 1 Clinical |

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