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GNE140

GNE140 Structure
GNE140
  • CAS No.2003234-63-5
  • Chemical Name:GNE140
  • 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 wordWarning
  • Hazard statements H302-H315-H319-H335
  • Precautionary statements P261-P305+P351+P338

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.
  • Uses (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.).
  • in vivo

    (R)-GNE-140 (5 mg/kg) has high bioavailability in mice. At higher oral doses, ranging from 50 to 200 mg/kg, (R)-GNE-140 displays greater exposure.

  • References [1] Purkey HE, et al. Cell Active Hydroxylactam Inhibitors of Human Lactate Dehydrogenase with Oral Bioavailability in Mice. ACS Med Chem Lett. 2016 Aug 26;7(10):896-901. DOI:10.1021/acsmedchemlett.6b00190
GNE140 Preparation Products And Raw materials
Raw materials
Preparation Products
GNE140 Suppliers
Global(87)Suppliers
  • Supplier：
    InvivoChem
  • Tel：+1-708-310-1919<br/>+1-13798911105
  • Email：sales@invivochem.cn
  • Country：United States
  • ProdList：6391
  • Advantage：58
  • Supplier：
    TargetMol Chemicals Inc.
  • Tel：
  • Email：support@targetmol.com
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  • Supplier：
    LEAPCHEM CO., LTD.
  • Tel：+86-852-30606658
  • Email：market18@leapchem.com
  • Country：China
  • ProdList：43340
  • Advantage：58
GNE140 Spectrum
2003234-63-5, GNE140Related Search:
  • 化学试剂
  • 药靶配体
  • 抑制剂
  • 其他生化试剂
  • 细胞生物学试剂
  • 化合物(R)-GNE-140,10 MM DMSO 溶液
  • (6R)-3-[(2-氯苯基)硫代]-5,6-二氢-4-羟基-6-[4-(4-吗啉基)苯基]-6-(3-噻吩基)-2(1H)-吡啶酮
  • 化合物(R)-GNE-140
  • (R)-3-((2-氯苯基)硫基)-4-羟基-6-(4-吗啉苯基)-6-(噻吩-3-基)-5,6-二氢吡啶-2(1H)-酮
  • LDHA抑制剂((R)-GNE-140)
  • 2003234-63-5
  • (R)-GNE-140, 10 mM in DMSO
  • Inhibitor,LDH,(R) GNE 140,inhibit,Lactate Dehydrogenase,(R)GNE140
  • 2(1H)-Pyridinone, 3-[(2-chlorophenyl)thio]-5,6-dihydro-4-hydroxy-6-[4-(4-morpholinyl)phenyl]-6-(3-thienyl)-, (6R)-
  • CS-2624
  • (R)-GNE-140
  • (R)-GNE-140 (GNE-140
  • (R)-3-((2-chlorophenyl)thio)-4-hydroxy-6-(4-morpholinophenyl)-6-(thiophen-3-yl)-5,6-dihydropyridin-2(1H)-one
  • GNE-140;GNE 140;GNE140
  • GNE140

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