GNE140
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
- CAS NO.：2003234-63-5
- Empirical Formula: C25H23ClN2O3S2
- Molecular Weight: 499.04
- Update Date: 2024-07-02 08:55:09
What is GNE140?
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.).
Properties of GNE140
| 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 |
Safety information for GNE140
| Signal word | Warning |
| Pictogram(s) |
 Exclamation Mark Irritant GHS07 |
| GHS Hazard Statements |
H302:Acute toxicity,oral H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation |
| Precautionary Statement Codes |
P261:Avoid breathing dust/fume/gas/mist/vapours/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. |
Computed Descriptors for GNE140
| InChIKey | SUFXXEIVBZJOAP-RUZDIDTESA-N |
| SMILES | C1(=O)N[C@](C2=CC=C(N3CCOCC3)C=C2)(C2C=CSC=2)CC(O)=C1SC1=CC=CC=C1Cl |
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