GSK2194069

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

GSK2194069 是脂肪酸合成酶 (FASN) 的 β-酮基还原酶 (KR) 的有效抑制剂，IC50 为 7.7 nM。GSK2194069 通过作用乙酰乙酰辅酶 A、NADPH (IC50 或 Ki 分别为 4.8 nM 和 5.6 nM) ，抑制表达 FAS 的癌细胞。

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.

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.

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Membrane Transporter/Ion Channel

NADPH

NADPH | Fatty Acid Synthase

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1332331-08-4

428.48

C25H24N4O3

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : ≥ 100 mg/mL (233.38 mM )

O=C(C1CC1)N1CC[C@@H](Cc2n[nH]c(=O)n2-c2ccc(cc2)-c2ccc3occc3c2)C1

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(-20℃)

With Ice Pack

≥ 2 years