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Merck
CN

SML2580

Sigma-Aldrich

GNE-140

≥98% (HPLC), lactate dehydrogenase (LDH) inhibitor, powder

Synonym(s):

(6R)-3-[(2-Chlorophenyl)thio]-5,6-dihydro-4-hydroxy-6-[4-(4-morpholinyl)phenyl]-6-(3-thienyl)-2(1H)-pyridinone, (R)-3-(2-Chlorophenyl)sulfanyl-6-(4-morpholinophenyl)-6-(3-thienyl)piperidine-2,4-dione, GNE 140, GNE140

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About This Item

Empirical Formula (Hill Notation):
C25H23ClN2O3S2
CAS Number:
2003234-63-5
Molecular Weight:
499.04
MDL number:
MFCD31560470
UNSPSC Code:
12352200
NACRES:
NA.77

Key Documents

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Product Name

GNE-140, ≥98% (HPLC)

Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

−20°C

InChI key

SUFXXEIVBZJOAP-RUZDIDTESA-N

Related Categories

Biochem/physiol Actions

Active site-targeting, potent and selective lactate dehydrogenase (LDH) inhibitor that affects glycolysis-dependent cancer proliferation & survival.
GNE-140 is an active site-targeting, potent and selective lactate dehydrogenase (LDH) inhibitor (LDH-A/B/C IC50 = 3/5/5 nM; LDH-A IC50 = 22 nM with mixed GNE-140 diastereomers; malate dehydrogenases MDH1/2 IC50 >10 μM; 301 kinases IC50 >1 μM) that reduces cellular lactate (IC50 = 670 nM; MIA PaCa-2) and upregulates pyruvate levels. GNE-140 affects glycolysis-dependent cancer proliferation (IC50 = 430 nM; MIA PaCa-2 & KP-2) & survival, but not oxidative phosphorylation (OXPHOS)-dependent growth. Due to rapid clearance, GNE-140 is ineffective against MIA PaCa-2 tumor growth with only transient lactate-reducing efficacy in tumor tissue in mice in vivo (100-400 mg/kg b.i.d. p.o.).

Storage Class Code

13 - Non Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Regulatory Information

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Certificates of Analysis (COA)

Lot/Batch Number
0000403328
0000403328
0000326122
0000326123
0000326123

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Raju V Pusapati et al.
Cancer cell, 29(4), 548-562 (2016-04-08)
Although glycolysis is substantially elevated in many tumors, therapeutic targeting of glycolysis in cancer patients has not yet been successful, potentially reflecting the metabolic plasticity of tumor cells. In various cancer cells exposed to a continuous glycolytic block, we identified
Aaron Boudreau et al.
Nature chemical biology, 12(10), 779-786 (2016-08-02)
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
Anneleen Daemen et al.
Proceedings of the National Academy of Sciences of the United States of America, 112(32), E4410-E4417 (2015-07-29)
Although targeting cancer metabolism is a promising therapeutic strategy, clinical success will depend on an accurate diagnostic identification of tumor subtypes with specific metabolic requirements. Through broad metabolite profiling, we successfully identified three highly distinct metabolic subtypes in pancreatic ductal
John Smestad et al.
Oncotarget, 9(5), 6109-6127 (2018-02-22)
Succinate dehydrogenase (SDH)-loss pheochromocytoma and paraganglioma (PPGL) are tumors driven by metabolic derangement. SDH loss leads to accumulation of intracellular succinate, which competitively inhibits dioxygenase enzymes, causing activation of pseudohypoxic signaling and hypermethylation of histones and DNA. The mechanisms by
Aerobic glycolysis is important for zebrafish larval wound closure and tail regeneration.
Scott, et al.
Wound Repair and Regeneration, 30, 665-680 (2023)

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