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GSK2194069

Catalog No. T15429 CAS 1332331-08-4

GSK2194069 is an active β-keto reductase (KR)-specific inhibitor of fatty acid synthase (FASN) with an IC50 of 7.7 nM in an assay for the detection of released CoA.GSK2194069 inhibits the proliferation of FAS in cancer cells through the action of acetoacetyl-coenzyme A and NADPH.

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GSK2194069, CAS 1332331-08-4

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Description	GSK2194069 is an active β-keto reductase (KR)-specific inhibitor of fatty acid synthase (FASN) with an IC50 of 7.7 nM in an assay for the detection of released CoA.GSK2194069 inhibits the proliferation of FAS in cancer cells through the action of acetoacetyl-coenzyme A and NADPH.
Targets&IC50	Phosphatidylcholine:15.5 ± 9 nM(EC50), β-ketoyl reductase:7.7 nM
In vitro	GSK2194069 (100 nM; 24 h) suppresses fatty acid synthase (FAS) activity in cancer cell lines (KATO-III, MKN45, A549, SNU-1) while maintaining FAS protein production levels.[1] GSK2194069 (5 μM and 20 μM) shows higher efficacy in FASN-positive LNCaP cells rather than FASN-negative PC3 cells, with the higher FASN Expression level in LNCaP cells.[2] GSK2194069 (50 μM; 24 h) inhibits the growth of LNCaP-LN3 human prostate cancer cells.[3] GSK2194069 (60.4 nM; 24 h) displays properties of metabolomics, including L-acetyl carnitine, stearoyl carnitine, vaccenyl carnitine, and palmitoyl-L-carnitine decrease in LNCaP-LN3 cells.[3]

Molecular Weight	428.48
Formula	C25H24N4O3
CAS No.	1332331-08-4

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 90.0 mg/mL (210.0 mM)

References and Literature

1. Hardwicke MA, et al. A human fatty acid synthase inhibitor binds β-ketoacyl reductase in the keto-substrate site. Nat Chem Biol. 2014;10(9):774-779. 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;27(5):1552. 3. Oh JE, et al. Deciphering Fatty Acid Synthase Inhibition-Triggered Metabolic Flexibility in Prostate Cancer Cells through Untargeted Metabolomics. Cells. 2020;9(11):2447.

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Keywords

GSK2194069 1332331-08-4 Metabolism Others Fatty Acid Synthase NADPH GSK 2194069 GSK-2194069 inhibitor inhibit

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