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GNE-140 racemate

Chemical Structure : GNE-140 racemate

CAS No.: 1802977-61-2

GNE-140 racemate (GNE 140 racemate;GNE140 racemate)

Catalog No.: PC-42245Not For Human Use, Lab Use Only.

GNE-140 racemate is the racemate of GNE-140, a novel potent, selective lactate dehydrogenase (LDH) inhibitor with IC50 of 3, 5, and 5 nM for LDHA, LDHB, and LDHC, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

GNE-140 racemate is the racemate of GNE-140, a novel potent, selective lactate dehydrogenase (LDH) inhibitor with IC50 of 3, 5, and 5 nM for LDHA, LDHB, and LDHC, respectively.
GNE-140 racemate displays no inhibition on malate MDH-1, MDH-2 (IC50>10 uM for both enzymes), and no appreciable inhibition against a panel of 301 kinases (<50% inhibition at 1 uM).
GNE-140 racemate perturbs glycolysis and inhibits proliferation in MIA PaCa-2 cells (IC50=0.43 uM), decreases glucose uptake (IC50=0.47 uM).
Pancreatic cell lines that utilize oxidative OXPHOS rather than glycolysis are inherently resistant to GNE-140, which can be resensitized to GNE-140 with the OXPHOS inhibitor phenformin.

Physicochemical Properties

M.Wt 499.0447
Formula C25H23ClN2O3S2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 34 mg/mL

Chemical Name/SMILES

2,4-Piperidinedione, 3-[(2-chlorophenyl)thio]-6-[4-(4-morpholinyl)phenyl]-6-(3-thienyl)-

References

1. Boudreau A, et al. Nat Chem Biol. 2016 Oct;12(10):779-86.

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