LFM-A13 is a selective inhibitor of Bruton’s tyrosine kinase (BTK) – IC50’s = 2.5 µM (recombinant BTK) and 17.2 µM (human BTK). It has also been shown to inhibit Polo-ilke kinase (PLK) – IC50 = 61 µM for human PLK3. It displayed no activity (concentrations up to 278 µM) at JAK1, JAK3, HCK, EGFRK...
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LFM-A13 is a selective inhibitor of Bruton’s tyrosine kinase (BTK) – IC50’s = 2.5 µM (recombinant BTK) and 17.2 µM (human BTK). It has also been shown to inhibit Polo-ilke kinase (PLK) – IC50 = 61 µM for human PLK3. It displayed no activity (concentrations up to 278 µM) at JAK1, JAK3, HCK, EGFRK and IRK2 or CDK1-3, CHK1, IKK, MAPK1, SAPK2a and ten tyrosine kinases
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BTK (Bruton tyrosine kinase), also known as tyrosine-protein kinase BTK, is a TEC-family non-receptor tyrosine kinase central to B-cell receptor signalling and B-lymphocyte development.
Biological function: Following B-cell receptor engagement, BTK is activated at the plasma membrane and phosphorylates PLCG2, promoting calcium mobilization and downstream protein kinase C signalling. This kinase activity is central to B-cell activation, differentiation and immune signalling.
