GNE-140 (racemate) Chemical Properties

Boiling point:

739.0±60.0 °C(Predicted)

Density 

1.43±0.1 g/cm3(Predicted)

storage temp. 

2-8°C

solubility 

DMSO : ≥ 34 mg/mL (68.13 mM)

pka

9.61±0.70(Predicted)

form 

Solid

color 

White to off-white

GNE-140 (racemate) Usage And Synthesis

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.

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

GNE-140 (racemate)(1802977-61-2)Related Product Information

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