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| Product Name: | GNE140 | | Synonyms: | GNE140;GNE-140;GNE 140;GNE140;(R)-3-((2-chlorophenyl)thio)-4-hydroxy-6-(4-morpholinophenyl)-6-(thiophen-3-yl)-5,6-dihydropyridin-2(1H)-one;(R)-GNE-140
(GNE-140;(R)-GNE-140;CS-2624;2(1H)-Pyridinone, 3-[(2-chlorophenyl)thio]-5,6-dihydro-4-hydroxy-6-[4-(4-morpholinyl)phenyl]-6-(3-thienyl)-, (6R)-;Inhibitor,LDH,(R) GNE 140,inhibit,Lactate Dehydrogenase,(R)GNE140 | | CAS: | 2003234-63-5 | | MF: | C25H23ClN2O3S2 | | MW: | 499.04 | | EINECS: | | | Product Categories: | | | Mol File: | 2003234-63-5.mol |  |
| | GNE140 Chemical Properties |
| Boiling point | 695.4±55.0 °C(Predicted) | | density | 1.46±0.1 g/cm3(Predicted) | | storage temp. | 2-8°C(protect from light) | | solubility | DMSO:14.4(Max Conc. mg/mL);28.9(Max Conc. mM) | | pka | 4.50±1.00(Predicted) | | form | Solid | | color | Light yellow to yellow | | InChIKey | SUFXXEIVBZJOAP-RUZDIDTESA-N | | SMILES | C1(=O)N[C@](C2=CC=C(N3CCOCC3)C=C2)(C2C=CSC=2)CC(O)=C1SC1=CC=CC=C1Cl |
| | GNE140 Usage And Synthesis |
| Description | GNE140 ((R)-GNE-140) is a potent lactate dehydrogenase A (LDHA) inhibitor, with IC50s of 3 nM and 5 nM for LDHA and LDHB, respectively; (R)-GNE-140 is 18-fold more potent than S enantiomer. | | Biochem/physiol Actions | 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.). |
| | GNE140 Preparation Products And Raw materials |
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