5.30729

AAA-ATPase Drg1 Inhibitor, Diazaborine

• Synonym(s): AAA-ATPase Drg1 Inhibitor, Diazaborine, 2-tosylbenzo[d][1,2,3]diazaborinin-1(2H)-ol, Ribosome Biogenesis Inhibitor, Diazaborine, Drg1 inhibitor
• Empirical Formula (Hill Notation): C₁₄H₁₃BN₂O₃S
• CAS Number: 22959-81-5
• Molecular Weight: 300.14
• UNSPSC Code: 51111800
• NACRES: NA.77

Properties

• Assay: ≥98% (HPLC)
• Quality Level: 100
• form: powder
• potency: 26 μM K_i
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: white
• solubility: DMSO: 100 mg/mL
• storage temp.: 2-8°C

Description

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 (K_i = 26 µM) resulting in reduced ATP hydrolysis and release of Rip24 from pre-60S particles.

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 (K_i = 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

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable