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Chemical Structure : (R)-GNE-140
CAS No.: 2003234-63-5
Catalog No.: PC-42246Not For Human Use, Lab Use Only.
(R)-GNE-140 (GNE-140) is a novel potent, selective lactate dehydrogenase (LDH) inhibitor with IC50 of 3, 5, and 5 nM for LDHA, LDHB, and LDHC, respectively.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $148 | In stock | |
| 10 mg | $238 | In stock | |
| 25 mg | $398 | In stock | |
| 50 mg | Get quote | ||
| 100 mg | Get quote |
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(R)-GNE-140 (GNE-140) is a novel potent, selective lactate dehydrogenase (LDH) inhibitor with IC50 of 3, 5, and 5 nM for LDHA, LDHB, and LDHC, respectively。
GNE-140 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 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.
| M.Wt | 499.0447 | |
| Formula | C25H23ClN2O3S2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
(R)-3-((2-Chlorophenyl)thio)-4-hydroxy-6-(4-morpholinophenyl)-6-(thiophen-3-yl)-5,6-dihydropyridin-2(1H)-one |
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1. Boudreau A, et al. Nat Chem Biol. 2016 Oct;12(10):779-86.
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