GSK2194069

SKU: orb1707243

Description

GSK2194069 is a potent and selective β-keto reductase (KR) domain inhibitor of fatty acid synthase (FASN), exhibiting an IC50 of 7.7 nM. It suppresses cancer cell proliferation by disrupting the FASN-catalyzed reduction of acetoacetyl-CoA with NADPH, making it a valuable tool for studying lipid metabolism and oncogenesis in vitro.

Research Area

Metabolism Research

Key Properties

• CAS Number: 1332331-08-4
• MW: 428.48
• Purity: 99.84% (May vary between batches)
• Formula: C₂₅H₂₄N₄O₃
• SMILES: O=C(C1CC1)N1CC[C@@H](Cc2n[nH]c(=O)n2-c2ccc(cc2)-c2ccc3occc3c2)C1
• Target: NADPH,Fatty Acid Synthase
• Solubility: DMSO:90 mg/mL (210.04 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (7.7 mM)

Bioactivity

• Target IC50:
  Phosphatidylcholine:15.5 ± 9 nM(EC50)|β-ketoyl reductase:7.7 nM
• In Vitro:
  GSK2194069 (100 nM; 24 h) suppresses fatty acid synthase (FAS) activity in cancer cell lines (KATO-III, MKN45, A549, SNU-1) while maintaining FAS protein production levels. GSK2194069 (5 μM and 20 μM) demonstrates higher efficacy in FASN-positive LNCaP cells compared to FASN-negative PC3 cells, correlating with higher FASN expression in LNCaP cells. GSK2194069 (50 μM; 24 h) inhibits the growth of LNCaP-LN3 human prostate cancer cells. GSK2194069 (60.4 nM; 24 h) exhibits metabolomic alterations, including decreases in L-acetyl carnitine, stearoyl carnitine, vaccenyl carnitine, and palmitoyl-L-carnitine in LNCaP-LN3 cells.
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Storage & Handling

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

Alternative Names

NADPH, Fatty Acid Synthase, Fatty Acid Synthase (FASN), FattyAcidSynthase, GSK2194069, GSK-2194069, GSK 2194069

Compound Identifiers

PubChem CID

67376285