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JAK Inhibitor

No.165(April 2015)
Tyrphostin AG490   (1)
The Janus kinase (JAK) family is one non-receptor tyrosine kinase. Each protein has a kinase domain and a catalytically inactive pseudo-kinase domain, and each binds the cytokine receptor through FERM domains.1) JAKs are activated on the binding of cytokines to their receptors.1,2) The activated JAKs phosphorylate the receptors, creating docking sites for signaling molecules, STAT (signal transducer and activator of transcription) family.2)
Tyrphostin AG490 (1) is an inhibitor of EGFR (epidermal growth factor receptor) tyrosine kinase.3) 1 has been shown to inhibit activation of JAK2 in pre-B ALL (acute lymphoblastic leukemia) cells.4) 1 also inhibits JAK3/STAT, JAK3/AP-1, and JAK3/MAPK signaling pathways and blocks JAK3 autophosphorylation.5-7)
FERM domain: domains found in molecules such as Band 4.1, ezrin, radaxin, and moesin.


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