Novobiocin (sodium)

Novobiocin (Albamycin) sodium is a potent and orally active antibiotic. Novobiocin sodium also is a DNA gyrase inhibitor and a heat shock protein 90 (Hsp90) antagonist. Novobiocin sodium has the potential for the research of highly beta-lactam-resistant pneumococcal infections. Novobiocin sodium shows anti-orthopoxvirus activity^[1][2][3][4]. IC50 & Target: IC50: 700 μM (HSP90)^[2] In Vitro: Novobiocin sodium (1 mM) competitively inhibits ATP binding to gyrase B to interfere with nucleotide binding and interferes with the association of the co-chaperones Hsc70 and p23 with Hsp90^[1].
Novobiocin sodium (200 µM; 24 h) inhibits the rate of repair of both cis-DDP and BCNU induced DNA interstrand cross-links and with a corresponding decrease in the clonogenic survival of the human glioblastoma multiforme cells^[2].
Novobiocin sodium (0.3 mM; 48 hours) induces a caspase-3/7 enzyme–dependent apoptosis assays with an induction of approximately three- to fivefold of apoptotic cells in K562, HL60, Mutz-2^[5].
In Vivo: Novobiocin sodium (25, 50, 100, 200 mg/kg; s.c.; 4 times at 1, 5, 24 and 48 h after infection) shows anti-infection activity in mice infected with amoxicillin-resistant Streptococcus pneumoniae^[3].