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MS-1020 Is a Novel Small Molecule That Selectively Inhibits JAK3 Activity

MS-1020 Is a Novel Small Molecule That Selectively Inhibits JAK3 Activity

Byung-Hak Kim, Sei-Ryang Oh, Chang-Hong Yin, Sangku Lee, Eun-Ah Kim, Min-Seok Kim, Claudio Sandoval, Somasundaram Jayabose, Erika A Bach, Hyeong-Kyu Lee, Gyeong-Hun Baeg

Br J Haematol. 2010 Jan;148(1):132-43.

PMID: 19793252

Abstract:

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 Nb-(alpha-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 in vitro 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.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP1255516869	MS-1020		1255516-86-9	Price

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