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GSK2194069 is a fatty acid synthase (FAS) inhibitor. GSK2194069 is a potent and specific inhibitor of the β-ketoacyl reductase (KR) activity of hFAS with an IC50 of 7.7 ± 4.1 nM for the overall hFAS reaction. FAS is upregulated in some cancers, including prostate cancer. GSK2194069 was found to inhibit tumour growth in prostate cancer C42b cell xenografts generated in Nod-SCID-gamma mice. Cellular FAS inhibition reduced cell growth were also demonstrated in non-small-cell lung (A549) cancer cell lines with an average EC50 of 15 ± 0.5 nM.
| Molecular Weight | 428.48 |
| Formula | C25H24N4O3 |
| CAS Number | 1332331-08-4 |
| Solubility (25°C) | DMSO: 5 mg/mL (warmed) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[5] Suzanne F Jones, et al. Molecular Pathways: Fatty Acid Synthase
| Related FAS Products |
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| C75
C75 is a novel, potent synthetic inhibitor of fatty acid synthase (FAS). C75 inhibits prostate cancer cells PC3 with an IC50 of 35 μM. C75 is a potent CPT1A activator. |
| Orlistat
Orlistat is an irreversible inhibitor of pancreatic and gastric lipases with IC50 of 122 ng/ml for PL from human duodenal juice. |
| Betulin
Betulin is a specific, small molecule inhibitor of SREBP (Sterol Regulatory Element-Binding Proteins). |
| Pseudoprotodioscin
Pseudoprotodioscin, a furan glucoside, inhibits sREBP1/2 and microRNA 33A/B levels and reduces the expression of genes associated with cholesterol and triglyceride synthesis. |
| Albaspidin-AP
Albaspidin AP inhibited fatty acid synthase (FAS) with IC50 value of 71.7 μM. Fatty acid synthase is emerging as a potential therapeutic target for cancer and obesity. |
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