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    InvivoChem Cat #: V4546
    CAS #: 2003234-63-5 (R-isomer)Purity ≥98%

    Description: (R)-GNE-140, the S-enantiomer of GNE-140, is a novel and potent lactate dehydrogenase (LDHA) inhibitor with IC50s of 3 nM and 5 nM for LDHA and LDHB, respectively. Metabolic reprogramming in tumors represents a potential therapeutic target. Herein we used shRNA depletion and a novel lactate dehydrogenase (LDHA) inhibitor, GNE-140, to probe the role of LDHA in tumor growth in vitro and in vivo. In MIA PaCa-2 human pancreatic cells, LDHA inhibition rapidly affected global metabolism, although cell death only occurred after 2 d of continuous LDHA inhibition. Pancreatic cell lines that utilize oxidative phosphorylation (OXPHOS) rather than glycolysis were inherently resistant to GNE-140, but could be resensitized to GNE-140 with the OXPHOS inhibitor phenformin. Acquired resistance to GNE-140 was driven by activation of the AMPK-mTOR-S6K signaling pathway, which led to increased OXPHOS, and inhibitors targeting this pathway could prevent resistance. Thus, combining an LDHA inhibitor with compounds targeting the mitochondrial or AMPK-S6K signaling axis may not only broaden the clinical utility of LDHA inhibitors beyond glycolytically dependent tumors but also reduce the emergence of resistance to LDHA inhibition.

    References:  2016 Oct;12(10):779-86;  2016 Aug 26;7(10):896-901. 

    Related CAS: 2003234-63-5 (R-isomer); 1809794-70-4 (racemate); 1802977-61-2; 2003234-64-6 (S-isomer)

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    Name: R-GNE-140
    CAS#: 2003234-63-5 (R-isomer)
    Chemical Formula: C25H23ClN2O3S2
    Exact Mass: 498.0839
    Molecular Weight: 499.04
    Elemental Analysis: C, 60.17; H, 4.65; Cl, 7.10; N, 5.61; O, 9.62; S, 12.85
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Technical InformationSynonym: R-GNE-140; (R)-GNE-140; GNE 140; GNE140.
    IUPAC/Chemical Name: (R)-3-((2-Chlorophenyl)thio)-4-hydroxy-6-(4-morpholinophenyl)-6-(thiophen-3-yl)-5,6-dihydropyridin-2(1H)-one
    InChi Code: InChI=1S/C25H23ClN2O3S2/c26-20-3-1-2-4-22(20)33-23-21(29)15-25(27-24(23)30,18-9-14-32-16-18)17-5-7-19(8-6-17)28-10-12-31-13-11-28/h1-9,14,16,29H,10-13,15H2,(H,27,30)/t25-/m1/s1
    SMILES Code: O=C1C(SC2=CC=CC=C2Cl)=C(O)C[[email protected]](C3=CSC=C3)(C4=CC=C(N5CCOCC5)C=C4)N1

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    Overlay of previously disclosed X-ray structures of LDHA/diketone-containing inhibitor complexes 4QO7 (cyan) and 4QO8 (white). Hydrogen bonds from 4QO7 are shown as yellow dashed lines.  2016 Aug 26;7(10):896-901.


    Compound 9 (cyan) cocrystallized with LDHA (white) [PDB: 5IXS]. The NADH cofactor is shown in green sticks, the crystallographic water as a red sphere, and hydrogen bonds are yellow dashed lines.  2016 Aug 26;7(10):896-901.


    Overlay of the crystal structures 29 (white) [PDB: 4ZVV] and 30 (cyan) [PDB: 5IXY] bound to LDHA. Hydrogen bonds are shown as yellow dashed lines.  2016 Aug 26;7(10):896-901.


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