PknG Inhibitor

General description

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 PKCα, 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 (10µM or higher) that does not otherwise affect the growth of BCG outside its infected host.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Scherr, N., et al. 2007. Proc. Natl. Acad. Sci. USA104, 16388.Walburger, A., et al. 2004. Science304, 1800.

Packaging

Packaged under inert gas

10 mg in Plastic ampoule

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)