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GSK 2194069

Cat. No. 5303 4 Citations Submit a Review Datasheet / COA / SDS
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Description: Potent human fatty acid synthase (hFASN) inhibitor
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% (HPLC)
Datasheet
Citations (4)
Reviews
Literature (1)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for GSK 2194069

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.

Compound Libraries for GSK 2194069

GSK 2194069 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for GSK 2194069

M. Wt 428.48
Formula C25H24N4O3
Storage Store at +4°C
Purity ≥99% (HPLC)
CAS Number 1332331-08-4
PubChem ID 67376285
InChI Key AQTPWCUIYUOEMG-INIZCTEOSA-N
Smiles O=C1NN=C(C[C@@H]2CCN(C(C3CC3)=O)C2)N1C4=CC=C(C5=CC=C(OC=C6)C6=C5)C=C4

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.

Solubility Data for GSK 2194069

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 42.85 100
ethanol 8.57 20

Preparing Stock Solutions for GSK 2194069

The following data is based on the product molecular weight 428.48. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.33 mL 11.67 mL 23.34 mL
5 mM 0.47 mL 2.33 mL 4.67 mL
10 mM 0.23 mL 1.17 mL 2.33 mL
50 mM 0.05 mL 0.23 mL 0.47 mL

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References for GSK 2194069

References are publications that support the biological activity of the product.

Hardwicke et al (2014) A human fatty acid synthase inhibitor binds β-ketoacyl reductase in the keto-substrate site. Nat.Chem.Biol. 10 774 PMID: 25086508

Chu et al (2021) Pharmacological inhibition of fatty acid synthesis blocks SARS-CoV-2 replication. Nat.Metab. 3 1466 PMID: 34580494

If you know of a relevant reference for GSK 2194069, please let us know.

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Keywords: GSK 2194069, GSK 2194069 supplier, GSK2194069, fatty, acid, synthases, hFAS, beta-ketoacyl, reductases, b-ketoacyl, β-ketoacyl, lipid, synthesis, inhibitors, inhibits, Fatty, Acid, Synthase, Coronavirus, 5303, Tocris Bioscience

4 Citations for GSK 2194069

Citations are publications that use Tocris products. Selected citations for GSK 2194069 include:

Wu and Näär (2019) SREBP1-dependent de novo fatty acid synthesis gene expression is elevated in malignant melanoma and represents a cellular survival trait. Sci Rep 9 10369 PMID: 31316083

Evan C et al (2022) Cancer cells depend on environmental lipids for proliferation when electron acceptors are limited. Nat Metab 4 711-723 PMID: 35739397

Chu et al (2021) Pharmacological inhibition of fatty acid synthesis blocks SARS-CoV-2 replication. Nat.Metab. 3 1466 PMID: 34580494

Lien et al (2021) Low glycaemic diets alter lipid metabolism to influence tumour growth. Nature 599 302 PMID: 34671163

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Literature in this Area

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Cancer Metabolism Research Product Guide

Cancer Metabolism Research Product Guide

This product guide reviews some of the main areas in cancer metabolism research and lists around 150 products that can be used to investigate metabolic pathways in cancer including: