370653
PknG Inhibitor
Mycobacterial Protein Kinase G Inhibitor, 2-(Cyclopropanecarbonylamino)-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide, AX20017
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Merck KGaA
Frankfurter Str. 250
64293 Darmstadt
Germany
Phone: +49 6151 72-0
Fax: +49 6151 72 2000
01 June 2012
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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.
| Product information | |||
|---|---|---|---|
| Form | Light brown solid | ||
| Molar mass | 264.3 | ||
| Protect from Light | Yes | ||
| Packaged under inert gas | Yes | ||
| Purity | ≥95% by HPLC | ||
| Solubility | DMSO | ||
| Chemical formula | C13H16N2O2S | ||
| CAS number | 329221-38-7 | ||
| Store and ship information | |||
|---|---|---|---|
| Storage | +2°C to +8°C | ||
| Ship |
Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Standard Handling |
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