Molecular structure of PknG Inhibitor, CAS Number: 329221-38-7
PknG Inhibitor (CAS 329221-38-7)
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Alternate Names:
Mycobacterial Protein Kinase G Inhibitor
Application:
PknG Inhibitor is a cell-permeable tetrahydrobenzothiophene compound
CAS Number:
329221-38-7
Molecular Weight:
264.3
Molecular Formula:
C13H16N2O2S
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
PknG Inhibitor is 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.
PknG Inhibitor (CAS 329221-38-7) References
- Protein kinase G from pathogenic mycobacteria promotes survival within macrophages. | Walburger, A., et al. 2004. Science. 304: 1800-4. PMID: 15155913
- Structural basis for the specific inhibition of protein kinase G, a virulence factor of Mycobacterium tuberculosis. | Scherr, N., et al. 2007. Proc Natl Acad Sci U S A. 104: 12151-6. PMID: 17616581
- A novel drug discovery concept for tuberculosis: inhibition of bacterial and host cell signalling. | Székely, R., et al. 2008. Immunol Lett. 116: 225-31. PMID: 18258308
- Protein kinases as antibacterial targets. | Schreiber, M., et al. 2009. Curr Opin Cell Biol. 21: 325-30. PMID: 19246185
- Sclerotiorin inhibits protein kinase G from Mycobacterium tuberculosis and impairs mycobacterial growth in macrophages. | Chen, D., et al. 2017. Tuberculosis (Edinb). 103: 37-43. PMID: 28237032
- Identification of Novel Mycobacterial Inhibitors Against Mycobacterial Protein Kinase G. | Kanehiro, Y., et al. 2018. Front Microbiol. 9: 1517. PMID: 30050511
- An Aspartate-Specific Solute-Binding Protein Regulates Protein Kinase G Activity To Control Glutamate Metabolism in Mycobacteria. | Bhattacharyya, N., et al. 2018. mBio. 9: PMID: 30065086
- An Overview on the Potential Antimycobacterial Agents Targeting Serine/Threonine Protein Kinases from Mycobacterium tuberculosis. | Mori, M., et al. 2019. Curr Top Med Chem. 19: 646-661. PMID: 30827246
- Deletion of pknG Abates Reactivation of Latent Mycobacterium tuberculosis in Mice. | Khan, MZ. and Nandicoori, VK. 2021. Antimicrob Agents Chemother. 65: PMID: 33468473
- Identifying RO9021 as a Potential Inhibitor of PknG from Mycobacterium tuberculosis: Combinative Computational and In Vitro Studies. | Arica-Sosa, A., et al. 2022. ACS Omega. 7: 20204-20218. PMID: 35721990
Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
PknG Inhibitor, 10 mg | sc-222180 | 10 mg | $198.00 |