GSK 2194069
Chemical Name: 4-[4-(5-Benzofuranyl)phenyl]-5-[[(3S)-1-(cyclopropylcarbonyl)-3-pyrrolidinyl]methyl]-2,4-dihydro-3H-1,2,4-triazol-3-one
Purity: ≥99%
Biological Activity
GSK 2194069 is a potent human fatty acid synthase (hFASN) inhibitor (IC50 = 7.7 nM); inhibits hFAS β-ketoacyl reductase activity. Inhibits lipid synthesis and attenuates proliferation of A549 non-small-cell lung cancer cells (EC50 = 15 nM) in vitro. GSK 2194069 also inhibits infection by SARS-CoV-2 (EC50 = 0.9 nM) in vitro.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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A human fatty acid synthase inhibitor binds β-ketoacyl reductase in the keto-substrate site.
Hardwicke et al.
Nat.Chem.Biol., 2014;10:774
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Citations for GSK 2194069
The citations listed below are publications that use Tocris products. Selected citations for GSK 2194069 include:
4 Citations: Showing 1 - 4
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Cancer cells depend on environmental lipids for proliferation when electron acceptors are limited.
Authors: Evan C Et al.
Nat Metab 2022;4:711-723
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Low glycaemic diets alter lipid metabolism to influence tumour growth.
Authors: Lien Et al.
Nature 2021;599:302
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Pharmacological inhibition of fatty acid synthesis blocks SARS-CoV-2 replication.
Authors: Chu Et al.
Nat.Metab. 2021;3:1466
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SREBP1-dependent de novo fatty acid synthesis gene expression is elevated in malignant melanoma and represents a cellular survival trait.
Authors: Wu and Näär
Sci Rep 2019;9:10369
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