GSK2194069

GSK2194069 is an inhibitor of fatty acid synthase (FASN) with an IC50 value of 7.7 nM in an assay detecting released CoA. 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.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: DMF: 30 mg/ml, DMSO: 20 mg/ml, Ethanol: 1 mg/ml. lambdamax: 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.