| Identification | Back Directory | [Name]
GNE-140 (racemate) | [CAS]
1802977-61-2 | [Synonyms]
GNE-140 (racemate)
GNE-140 racemate
(GNE 140 racemate
3-((2-chlorophenyl)thio)-6-(4-morpholinophenyl)-6-(thiophen-3-yl)piperidine-2,4-dione
2,4-Piperidinedione, 3-[(2-chlorophenyl)thio]-6-[4-(4-morpholinyl)phenyl]-6-(3-thienyl)- | [Molecular Formula]
C25H23ClN2O3S2 | [MOL File]
1802977-61-2.mol | [Molecular Weight]
499.04 |
| Chemical Properties | Back Directory | [Boiling point ]
739.0±60.0 °C(Predicted) | [density ]
1.43±0.1 g/cm3(Predicted) | [storage temp. ]
Sealed in dry,2-8°C | [solubility ]
DMSO : ≥ 34 mg/mL (68.13 mM) | [form ]
Solid | [pka]
9.61±0.70(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
GNE-140 racemate is a racemate mixture of (R)-GNE-140 and (S)-GNE-140. GNE-140 racemate is a potent lactate dehydrogenase A (LDHA) inhibitor | [Uses]
GNE-140 racemate is a racemate mixture of (R)-GNE-140 and (S)-GNE-140. GNE-140 racemate is a potent lactate dehydrogenase A (LDHA) inhibitor[1][2]. | [in vitro]
Increased glucose consumption distinguishes cancer cells from normal cells and is known as the “Warburg effect” because of increased glycolysis. Lactate dehydrogenase A (LDHA) is a key glycolytic enzyme, a hallmark of aggressive cancers, and believed to be the major enzyme responsible for pyruvate-to-lactate conversion. | [storage]
Store at -20°C | [References]
[1] ?dralevi? M, et al. Double genetic disruption of lactate dehydrogenases A and B is required to ablate the "Warburg effect" restricting tumor growth to oxidative metabolism. J Biol Chem. 2018 Oct 12;293(41):15947-15961. DOI:10.1074/jbc.RA118.004180
[2] Purkey HE, et al. Cell Active Hydroxylactam Inhibitors of Human Lactate Dehydrogenase with Oral Bioavailability in Mice. ACS Med Chem Lett. 2016 Aug 26;7(10):896-901. DOI:10.1021/acsmedchemlett.6b00190 |
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