370653

PknG Inhibitor

The PknG Inhibitor, also referenced under CAS 329221-38-7, controls the biological activity of PknG. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Synonym(s): PknG Inhibitor, Mycobacterial Protein Kinase G Inhibitor, 2-(Cyclopropanecarbonylamino)-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide, AX20017
• Empirical Formula (Hill Notation): C₁₃H₁₆N₂O₂S
• CAS Number: 329221-38-7
• Molecular Weight: 264.34
• MDL number: MFCD00785286
• UNSPSC Code: 12352200
• NACRES: NA.77
• Assay: ≥95% (HPLC)
• Form: solid
• Quality level: 100
• Storage condition: OK to freeze, protect from light

Properties

• Quality Level: 100
• assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, protect from light
• color: light brown
• solubility: DMSO: 5 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• SMILES string: [s]1c2c(c(c1NC(=O)C3CC3)C(=O)N)CCCC2
• InChI: 1S/C13H16N2O2S/c14-11(16)10-8-3-1-2-4-9(8)18-13(10)15-12(17)7-5-6-7/h7H,1-6H2,(H2,14,16)(H,15,17)
• InChI key: VATFNEMGBRWLHI-UHFFFAOYSA-N

Description

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.

Packaging

Packaged under inert gas

Preparation Note

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

Other Notes

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

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable