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MS-1020 is a novel small molecule that selectively inhibits JAK3 activity
Kim, Byung-Hak,Oh, Sei-Ryang,Yin, Chang-Hong,Lee, Sangku,Kim, Eun-Ah,Kim, Min-Seok,Sandoval, Claudio,Jayabose, Somasundaram,Bach, Erika A.,Lee, Hyeong-Kyu,Baeg, Gyeong-Hun Blackwell Publishing Ltd 2010 British journal of haematology Vol.148 No.1
<P>Summary</P><P>In order to identify Janus kinase/signal transducer and activator of transcription (JAK/STAT) signalling inhibitors, a cell-based high throughput screening was performed using a plant extract library that identified <I>N</I>b-(&agr;-hydroxynaphthoyl)serotonin called MS-1020 as a novel JAK3 inhibitor. MS-1020 potently inhibited persistently-active STAT3 in a cell type-specific manner. Further examination showed that MS-1020 selectively blocked constitutively-active JAK3 and consistently suppressed interleukin-2-induced JAK3/STAT5 signalling but not prolactin-induced JAK2/STAT5 signalling. Furthermore, MS-1020 affected cell viability only in cancer cells harbouring persistently-active JAK3/STATs, and <I>in vitro</I> kinase assays showed MS-1020 binds directly with JAK3, blocking its catalytic activity. Therefore, the present study suggested that this reagent selectively inhibits JAK3 and subsequently leads to a block in STAT signalling. Finally, MS-1020 decreased cell survival by inducing apoptosis via down-regulation of anti-apoptotic gene expression. These results suggest that MS-1020 may have therapeutic potential in the treatment of cancers harbouring aberrant JAK3 signalling.</P>