JAK3

Technology

Janus kinase 3 (JAK3) is a cytoplasmic protein tyrosine kinase that associates with the common gamma-c chain of various cytokine receptors. JAK3 plays a key role in the response of immune cells to cytokines, especially in mast cells, lymphocytes and macrophages. Inhibition of JAK3 has shown beneficial clinical effects in rheumatoid arthritis and transplant rejection.

Even though some JAK3 inhibitors have been reported to be selective in vitro over the closely related kinases JAK1, JAK2 and Tyk2, this selectivity only poorly translated into the cellular setting.

With » Kinobeads™ we screened native JAK3 directly in cell lysate and identified several hit series with sub-micromolar potencies. These hits are being optimised for their potency and selectivity over the other members of the JAK kinase family.

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