Dithiolo-thione 계열 유도체 SWU-20009의 Akt 활성 저해 효과

Inhibitory Effects of Dithiolo-thione Derivative SWU-20009 on Akt Activity

Akt (or Protein Kinase B; PKB) is a serine/threonine kinase and is activated by phosphoinositide 3-kinase (PI3K) pathway: Recent evidence indicates that the abnormal activities or expression of Akt is closely associated with cancers diabetes and neuro- degenerative diseases. These findings mean that Akt is likely to be a new therapeutic target for the treatment of disease. Here, we screened the effects of dithiolo- dithione derivatives such as SWU-20004, SWU-20709 and SWU-20025 on Akt activities. Among these compounds, only SWU-20009 (2-Thioxo - [1,3]dithiolo[4,5- β][1,4] dithiine-5,6-dicarboxylic acid dimethyl ester) inhibited the growth of KATOIII cell at micromolar range of concentration. Further investigation also revealed that SWU- 20009 inhibited cellular Akt activity and induced apoptotic cell death.