(R)-GNE-140

SKU: orb1302977

Description

GNE-140 is a potent dual inhibitor of LDHA and LDHB, exhibiting IC50 values of 3 nM and 5 nM, respectively. The R-enantiomer demonstrates 18-fold greater inhibitory activity than its S-enantiomer counterpart. This inhibitor is a valuable research tool for studying cancer metabolism and has shown antitumor efficacy in preclinical in vivo models.

Research Area

Metabolism Research

Key Properties

• CAS Number: 2003234-63-5
• MW: 499.04
• Purity: 97.32% (May vary between batches)
• Formula: C₂₅H₂₃ClN₂O₃S₂
• SMILES: OC1=C(Sc2ccccc2Cl)C(=O)N[C@@](C1)(c1ccsc1)c1ccc(cc1)N1CCOCC1
• Target: Dehydrogenase
• Solubility: DMSO:21.43 mg/mL (42.94 mM);DMF:25mg/mL (50.09 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2 mM);H2O:< 0.1 mg/mL (insoluble)

Bioactivity

• Target IC50:
  LDHA:3 nM|LDHB:5 nM
• In Vivo:
  (R)-GNE-140 demonstrates high bioavailability in mice at 5 mg/kg and achieves greater exposure at oral doses of 50-200 mg/kg.
• In Vitro:
  (R)-GNE-140 (5 μM) inhibits proliferation in 37 of 347 cancer cell lines. (R)-GNE-140 has an inhibitory effect on two chondrosarcomas (bone) cancer cell lines that harbor IDH1 mutations (IC50: 0.8 mΜ).
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, Inhibitor, Lactate Dehydrogenase, LDH, GNE 140, GNE140, GNE-140, (R)GNE140, (R) GNE 140

Compound Identifiers

PubChem CID

121225870