Merck, 5307290001, AAA-ATPase Drg1 Inhibitor, Diazaborine

General description
A diazaborine derivative with anti-bacterial properties against a wide range of Gram-negative bacteria. Shown to target NAD(P)H-dependent enoyl acyl carrier protein reductase (ENR), which results in the inhibition of bacterial fatty acid synthase. Blocks the maturation of ribosomal RNA for the large 60S ribosomal subunit in yeast cells by binding to the D2 domain of AAA-ATPase Drg1 (Ki = 26 µM) resulting in reduced ATP hydrolysis and release of Rip24 from pre-60S particles.

Please note that the molecular weight for this compound is batch-specific due to variable water content.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Drg1 AAA-ATPase
Reversible: yes
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
Loibl, M., et al. 2014. J. Biol. Chem. 289, 3913.
Pertschy B., et al. 2004. Mol. Cell. Biol. 24, 6476.
Baldock, C. et al. 1998. Biochem. Pharmacol. 55, 1541.
Grassberger M., et al. 1984. J Med Chem.27, 947.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)