SML2580

GNE-140

≥98% (HPLC)

• Synonym(e): (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
• Empirische Formel (Hill-System): C₂₅H₂₃ClN₂O₃S₂
• CAS-Nummer: 2003234-63-5
• Molekulargewicht: 499.04
• MDL-Nummer: MFCD31560470
• UNSPSC-Code: 12352200
• NACRES: NA.77

Eigenschaften

• Assay: ≥98% (HPLC)
• Form: powder
• Farbe: white to beige
• Löslichkeit: DMSO: 2 mg/mL, clear
• Lagertemp.: −20°C
• InChIKey: SUFXXEIVBZJOAP-RUZDIDTESA-N

Beschreibung

Biochem./physiol. Wirkung

Active site-targeting, potent and selective lactate dehydrogenase (LDH) inhibitor that affects glycolysis-dependent cancer proliferation & survival.

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.).

Sicherheitshinweise

• Lagerklassenschlüssel: 13 - Non Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable