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Beschreibung

A cell-permeable tetrahydrobenzothiophene compound that acts as a highly specific and ATP-binding site-targeting inhibitor against mycobacterial protein kinase G (PknG, IC50 = 390 nM), while exhibiting much reduced or no activity against 8 other mycobacterial and 25 other human kinases, including PKCalpha, the mammalian kinase most closely related to PknG. AX20017 is shown to completely inactivate PknG-mediated blockage of lysosomal transfer and degradation of M. bovis BCG in macrophages at concentrations (10µ,M or higher) that does not otherwise affect the growth of BCG outside its infected host.