| 产品描述： | 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 |
| 靶点： |
Fatty Acid Synthase (FASN);Others; NADPH; FattyAcidSynthase |
| 体外研究： |
GSK2194069 (100 nM; 24 h) inhibits fatty acid synthase (FAS) in cancer cell lines (KATO-III, MKN45, A549, SNU-1) without reducing FAS production protein level. GSK2194069 decreases phosphatidylcholine levels in A549 cells with a half-maximum effective concentration (EC50) value of 15.5 ± 9 nM (n = 78), correlating with the decreased palmitate synthesis. 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. GSK2194069 (50 μM; 24 h) inhibits the growth of LNCaP-LN3 human prostate cancer cells. 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. Western Blot Analysis Cell Line: A549 Concentration: 0, 10, 100, 1000 nM Incubation Time: 48 hours or 120 hours Result: Didn’t decrease FAS protein level. Western Blot Analysis Cell Line: FASN-positive LNCaP cells, and FASN-negative PC3 cells Concentration: 1 nM-0.1 mM Incubation Time: 48 hours Result: Inhibited tumor cells growth significantly, and reduced LNCaP cells much better. |
| 参考文献： |
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. |
| 溶解性： |
soluble in DMSO |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.334 ml |
11.669 ml |
23.338 ml |
| 5 mM |
0.467 ml |
2.334 ml |
4.668 ml |
| 10 mM |
0.233 ml |
1.167 ml |
2.334 ml |
| 50 mM |
0.047 ml |
0.233 ml |
0.467 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京