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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Fatty Acid Synthase-GSK2194069
GSK2194069

Chemical Structure : GSK2194069

CAS No.: 1332331-08-4

GSK2194069 (GSK 2194069;GSK-2194069)

货号: PC-42976Not For Human Use, Lab Use Only.

GSK2194069 is a potent and specific inhibitor of the β-ketoacyl reductase (KR) activity of human fatty acid synthase (hFAS) with IC50 of 7.7 nM (CoA release).

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5 mg ¥1280 In stock
10 mg ¥1980 In stock
25 mg ¥3280 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

GSK2194069 is a potent and specific inhibitor of the β-ketoacyl reductase (KR) activity of human fatty acid synthase (hFAS, FASN) with IC50 of 7.7 nM (CoA release).
GSK2194069 shows an IC50 of 29 nM versus hFAS with acetoacetyl-CoA as the substrate, but shows little or no inhibition with β-hydroxybutyrylCoA and crotonyl-CoA (IC50 >1,000 nM), also does not inhibit the partial activities of the KS domain.
GSK2194069 decreases phosphatidylcholine levels in A549 cells with IC50 of 15.5 nM without effect on FAS protein levels, reduced A549 cell growth with EC50 of 15 nM.

物理化学性质&存储条件

分子量 428.4831
分子式 C25H24N4O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3H-1,2,4-Triazol-3-one, 4-[4-(5-benzofuranyl)phenyl]-5-[[(3S)-1-(cyclopropylcarbonyl)-3-pyrrolidinyl]methyl]-2,4-dihydro-

参考文献

1. Hardwicke MA, et al. Nat Chem Biol. 2014 Sep;10(9):774-9.

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