GNE140
- Product Name
- GNE140
- CAS No.
- 2003234-63-5
- Chemical Name
- GNE140
- Synonyms
- GNE140;CS-2624;(R)-GNE-140;(R)-GNE-140 (GNE-140;GNE-140;GNE 140;GNE140;Inhibitor,LDH,(R) GNE 140,inhibit,Lactate Dehydrogenase,(R)GNE140;(R)-3-((2-chlorophenyl)thio)-4-hydroxy-6-(4-morpholinophenyl)-6-(thiophen-3-yl)-5,6-dihydropyridin-2(1H)-one;2(1H)-Pyridinone, 3-[(2-chlorophenyl)thio]-5,6-dihydro-4-hydroxy-6-[4-(4-morpholinyl)phenyl]-6-(3-thienyl)-, (6R)-
- CBNumber
- CB43353026
- Molecular Formula
- C25H23ClN2O3S2
- Formula Weight
- 499.04
- MOL File
- 2003234-63-5.mol
GNE140 Property
- 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
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- SML2580
- Product name
- GNE-140
- Purity
- ≥98% (HPLC)
- Packaging
- 5MG
- Price
- $160
- Updated
- 2024/03/01
- Product number
- SML2580
- Product name
- GNE-140
- Purity
- ≥98% (HPLC)
- Packaging
- 25MG
- Price
- $617
- Updated
- 2024/03/01
- Product number
- orb611623
- Product name
- (R)-GNE-140
- Packaging
- 100mg
- Price
- $912.9
- Updated
- 2021/12/16
- Product number
- CS-7646
- Product name
- (R)-GNE-140
- Purity
- 99.20%
- Packaging
- 10mg
- Price
- $370
- Updated
- 2021/12/16
- Product number
- CS-7646
- Product name
- (R)-GNE-140
- Purity
- 99.20%
- Packaging
- 50mg
- Price
- $1100
- Updated
- 2021/12/16
GNE140 Chemical Properties,Usage,Production
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.).