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GSK2194069

Chemical Structure : GSK2194069

CAS No.: 1332331-08-4

GSK2194069 (GSK 2194069;GSK-2194069)

Catalog No.: PC-42976Not For Human Use, Lab Use Only.

GSK2194069 is a potent and specific inhibitor of the β-ketoacyl reductase (KR) activity of human fatty acid synthase (hFAS) with IC50 of 7.7 nM (CoA release).

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Biological Activity

GSK2194069 is a potent and specific inhibitor of the β-ketoacyl reductase (KR) activity of human fatty acid synthase (hFAS) with IC50 of 7.7 nM (CoA release).
GSK2194069 shows an IC50 of 29 nM versus hFAS with acetoacetyl-CoA as the substrate, but shows little or no inhibition with β-hydroxybutyrylCoA and crotonyl-CoA (IC50 >1,000 nM), also does not inhibit the partial activities of the KS domain.
GSK2194069 decreases phosphatidylcholine levels in A549 cells with IC50 of 15.5 nM without effect on FAS protein levels, reduced A549 cell growth with EC50 of 15 nM.

Physicochemical Properties

M.Wt 428.4831
Formula C25H24N4O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3H-1,2,4-Triazol-3-one, 4-[4-(5-benzofuranyl)phenyl]-5-[[(3S)-1-(cyclopropylcarbonyl)-3-pyrrolidinyl]methyl]-2,4-dihydro-

References

1. Hardwicke MA, et al. Nat Chem Biol. 2014 Sep;10(9):774-9.

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