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(R)-GNE-140

Names

[ CAS No. ]:
2003234-63-5

[ Name ]:
(R)-GNE-140

[Synonym ]:
MFCD31560470

Biological Activity

[Description]:

(R)-GNE-140 is a potent lactate dehydrogenase A (LDHA) inhibitor, with IC50s of 3 nM and 5 nM for LDHA and LDHB, respectively; (R)-GNE-140 is 18-fold more potent than S enantiomer.

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> Lactate Dehydrogenase
Research Areas >> Cancer

[Target]

IC50: 3 nM (LDHA), 5 nM (LDHB)[1]


[In Vitro]

(R)-GNE-140 inhibits proliferation in 37 of 347 cancer cell lines tested at a potency cut off of 5 μM. (R)-GNE-140 shows inhibitory effect on two chondrosarcoma (bone) cancer cell lines that harbor IDH1 mutations, with IC50 of 0.8 μM[1].

[In Vivo]

(R)-GNE-140 (5 mg/kg) has high bioavailability in mice. At higher oral doses, ranging from 50 to 200 mg/kg, (R)-GNE-140 displays greater exposure.

[References]

[1]. 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.


[Related Small Molecules]

GNE-140 racemate | GSK 2837808A | LDH-IN-1 | FX-11 | Nifurtimox

Chemical & Physical Properties

[ Molecular Formula ]:
C25H23ClN2O3S2

[ Molecular Weight ]:
499.04

[ Storage condition ]:
-20℃

Related Compounds