An inhibitor of fatty acid synthase
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GSK2194069

Item No. 20022

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[4-(5-benzofuranyl)phenyl]-5-[[(3S)-1-(cyclopropylcarbonyl)-3-pyrrolidinyl]methyl]-2,4-dihydro-3H-1,2,4-triazol-3-one
CAS Number
1332331-08-4
Molecular Formula
C25H24N4O3
Formula Weight
428.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 20 mg/mlEthanol: 1 mg/ml
λmax
239 nm
SMILES
O=C(N(C1)CC[C@H]1CC2=NNC(N2C3=CC=C(C4=CC=C(OC=C5)C5=C4)C=C3)=O)C6CC6
InChi Code
InChI=1S/C25H24N4O3/c30-24(18-1-2-18)28-11-9-16(15-28)13-23-26-27-25(31)29(23)21-6-3-17(4-7-21)19-5-8-22-20(14-19)10-12-32-22/h3-8,10,12,14,16,18H,1-2,9,11,13,15H2,(H,27,31)/t16-/m0/s1
InChi Key
AQTPWCUIYUOEMG-INIZCTEOSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $36

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    1 mg

    $53

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    5 mg

    $186

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    Product Description

    GSK2194069 is an inhibitor of fatty acid synthase (FASN) with an IC50 value of 7.7 nM in an assay detecting released CoA.1 It is a competitive inhibitor that is selective for the KR domain over the KS domain of FASN, with IC50 values of 29 and >10,000 nM, respectively, in vitro. GSK2194069 decreases incorporation of 13C-labeled acetate into cellular lipids in a dose-dependent manner in KATO-III, MKN-45, and SNU-1 gastric, and A549 non-small cell lung cancer cell lines. It also reduces cell growth of A549 cells (EC50 = 15 nM) and inhibits lipid synthesis without decreasing FASN protein expression.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hardwicke, M.A., Rendina, A.R., Williams, S.P., et al. The uptake and subcellular distribution of radio-labeled metabolites of digoxin in the isolated perfused guinea-pig heart. Naunyn Schmiedebergs Arch. Pharmacol. 292(3), 251-254 (1976).