2003234-63-5

2003234-63-5 structure

Name: (R)-GNE-140
Chemical Name: (R)-GNE-140
CAS Number: 2003234-63-5
Molecular Formula: C₂₅H₂₃ClN₂O₃S₂
Molecular Weight: 499.04
Catalog: Signaling Pathways Metabolic Enzyme/Protease Lactate Dehydrogenase
Create Date: 2018-02-02 21:11:26
Modify Date: 2024-01-05 14:51:06
(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.

Name	(R)-GNE-140
Synonyms	MFCD31560470

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.