Original: R-GNE-140 2003234-63-5 , stock more than 100g

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Description: R-GNE-140 a novel potent lactate dehydrogenase (LDHA) inhibitor with IC50 3nM for LDHA and 5 nM for LDHB. 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.

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

Related CAS #: 2003234-63-5 (R-isomer)   1809794-70-4 (racemic)    

Synonym: 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 Key: SUFXXEIVBZJOAP-RUZDIDTESA-N

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[C@](C3=CSC=C3)(C4=CC=C(N5CCOCC5)C=C4)N1

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code: 293490

ADDITIONAL INFORMATION

Metabolic reprogramming in tumors represents a potential therapeutic target. 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

1: Boudreau A, Purkey HE, Hitz A, Robarge K, Peterson D, Labadie S, Kwong M, Hong 

R, Gao M, Del Nagro C, Pusapati R, Ma S, Salphati L, Pang J, Zhou A, Lai T, Li Y, 

Chen Z, Wei B, Yen I, Sideris S, McCleland M, Firestein R, Corson L, Vanderbilt 

A, Williams S, Daemen A, Belvin M, Eigenbrot C, Jackson PK, Malek S, 

Hatzivassiliou G, Sampath D, Evangelista M, O'Brien T. Metabolic plasticity 

underpins innate and acquired resistance to LDHA inhibition. Nat Chem Biol. 2016 

Oct;12(10):779-86. doi: 10.1038/nchembio.2143. Epub 2016 Aug 1. PubMed PMID: 

27479743.