Novobiocin

SKU: orb1705597

Description

Novobiocin is an orally active antibiotic that functions as a dual DNA gyrase inhibitor and Hsp90 antagonist. It is utilized in research to study highly resistant bacterial infections, such as those caused by Streptococcus pneumoniae, in both in vitro and in vivo experimental models.

Research Area

Cell Biology, Infectious Disease & Virology, Metabolism Research, Molecular Biology, Pharmacology & Drug Discovery, Signal Transduction

Key Properties

• CAS Number: 303-81-1
• MW: 612.62
• Purity: 98.72% (May vary between batches)
• Formula: C₃₁H₃₆N₂O₁₁
• SMILES: CO[C@@H]1[C@@H](OC(N)=O)[C@@H](O)[C@H](Oc2ccc3c(O)c(NC(=O)c4ccc(O)c(CC=C(C)C)c4)c(=O)oc3c2C)OC1(C)C
• Target: DNA gyrase|||Antibacterial|||HSP|||Apoptosis|||Virus Protease|||Antibiotic
• Solubility: 10% DMSO+40% PEG300+5% Tween-80+45% Saline:5 mg/mL (8.16 mM);DMSO:237.5 mg/mL (387.68 mM)

Bioactivity

• In Vivo:
  Novobiocin (25, 50, 100, 200 mg/kg; s.c.; 4 times at 1, 5, 24, and 48 h after infection; Adult female Swiss mice (30g) with sepsis induced by the penicillin-susceptible strain (AR33118)) exhibits anti-infection activity in mice infected with amoxicillin-resistant Streptococcus pneumoniae.
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• In Vitro:
  Novobiocin (1 mM) competitively hinders the binding of ATP to gyrase B, disrupting nucleotide binding, and impairs the interaction between the co-chaperones Hsc70 and p23 with Hsp90. Novobiocin (200 µM; 24 h) results in the inhibition of the repair rate of DNA interstrand cross-links induced by both cisplatin (cis-DDP) and BCNU. This is accompanied by a corresponding reduction in the clonogenic survival of human glioblastoma multiforme cells. Novobiocin (0.3 mM; 48 hours) triggers caspase-3/7 enzyme-dependent apoptosis assays, resulting in an approximate three- to fivefold increase in the number of apoptotic cells in K562, HL60, and Mutz-2.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

U 6391, U6391, U-6391, VirusProtease, Virus Protease, HSP90, Orthopoxvirus, Novobiocin, Bacterial, Apoptosis, Antibiotic, Albamycin, DNAgyrase, DNA gyrase, Cathomycin

Compound Identifiers

PubChem CID

54675769