GSK2194069
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].
Product Specifications
CAS Number
1332331-08-4
UNSPSC
12352005
Hazard Statement
H301
Target
Fatty Acid Synthase (FASN)
Type
Reference compound
Related Pathways
Metabolic Enzyme/Protease
Applications
Cancer-programmed cell death
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/GSK2194069.html
Purity
99.80
Solubility
DMSO : ≥ 100 mg/mL
Smiles
O=C(N1C[C@H](CC2=NNC(N2C3=CC=C(C4=CC=C(OC=C5)C5=C4)C=C3)=O)CC1)C6CC6
Molecular Formula
C25H24N4O3
Molecular Weight
428.48
Precautions
H301
References & Citations
[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.|[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. |[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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Available Sizes
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