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Submit ReviewGSK 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.
GSK 2194069 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
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.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 42.85 | 100 | |
ethanol | 8.57 | 20 |
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.
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 |
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.
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
Citations are publications that use Tocris products. Selected citations for GSK 2194069 include:
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
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
Do you know of a great paper that uses GSK 2194069 from Tocris? Please let us know.
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