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Sigma-Aldrich

AAA-ATPase Drg1 Inhibitor, Diazaborine

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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:
12352200
NACRES:
NA.77

Assay

≥98% (HPLC)

Quality Level

100

form

powder

potency

26 μM Ki

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

white

solubility

DMSO: 100 mg/mL

storage temp.

2-8°C

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.
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

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

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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