1332331-08-4
Chemical Structure
GSK2194069
- CAS No.: 1332331-08-4
- Formula:C25H24N4O3
- Molecular Weight:428.48
IUPAC Name: (S)-4-(4-(benzofuran-5-yl)phenyl)-5-((1-(cyclopropanecarbonyl)pyrrolidin-3-yl)methyl)-2,4-dihydro-3H-1,2,4-triazol-3-one
InChIKey: AQTPWCUIYUOEMG-INIZCTEOSA-N
SMILES: O=C(N1C[C@H](CC2=NNC(N2C3=CC=C(C4=CC=C(OC=C5)C5=C4)C=C3)=O)CC1)C6CC6
Biological Activity: GSK2194069 is a potent inhibitor of β-ketoyl reductase (KR) of fatty acid synthase (FASN), with an IC50 value of 7.7 nM. GSK2194069 shows specifically inhibitory effect on FAS expressing cancer cells, by acting potent efficacy on acetoacetyl-CoA, NADPH with IC50 or Ki values of 4.8 nM and 5.6 nM, respectively[1][2][3].
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GSK2194069 | 99.80% | GSK2194069 is a potent inhibitor of β-ketoyl reductase (KR) of fatty acid synthase (FASN), with an IC50 value of 7.7 nM. GSK2194069 shows specifically inhibitory effect on FAS expressing cancer cells, by acting potent efficacy on acetoacetyl-CoA, NADPH with IC50 or Ki values of 4.8 nM and 5.6 nM, respectively. | ||||||||||||||||||||
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- [1]. Hardwicke MA, et al. A human fatty acid synthase inhibitor binds β-ketoacyl reductase in the keto-substrate site. Nat Chem Biol. 2014 Sep;10(9):774-9. [Content Brief]
- [2]. Kelly JM, et al. Synthesis and Evaluation of 11C-Labeled Triazolones as Probes for Imaging Fatty Acid Synthase Expression by Positron Emission Tomography. Molecules. 2022 Feb 25;27(5):1552. [Content Brief]
- [3]. Oh JE, et al. Deciphering Fatty Acid Synthase Inhibition-Triggered Metabolic Flexibility in Prostate Cancer Cells through Untargeted Metabolomics. Cells. 2020 Nov 10;9(11):2447. [Content Brief]
Keywords
