Novobiocin [303-81-1]

Referência T20510-5mg

Tamanho : 5mg

Marca : TargetMol

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Novobiocin

Catalog No. T20510   CAS 303-81-1
Synonyms: U-6391, U 6391, U6391, Cathomycin, Albamycin

Novobiocin is an orally active and potent antibiotic.Novobiocin is a DNA gyrase inhibitor and heat shock protein 90 (Hsp90) antagonist with inhibitory effects on gyrase and Hsp90. Novobiocin has anti-positive activity and can be used to study highly resistant pneumococcal infections.

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Novobiocin Chemical Structure
Novobiocin, CAS 303-81-1
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Purity: 98.72%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Novobiocin is an orally active and potent antibiotic.Novobiocin is a DNA gyrase inhibitor and heat shock protein 90 (Hsp90) antagonist with inhibitory effects on gyrase and Hsp90. Novobiocin has anti-positive activity and can be used to study highly resistant pneumococcal infections.
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.[1]
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.[2]
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.[5]
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)) shows anti-infection activity in mice infected with amoxicillin-resistant Streptococcus pneumoniae.[3]
Synonyms U-6391, U 6391, U6391, Cathomycin, Albamycin
Molecular Weight 612.62
Formula C31H36N2O11
CAS No. 303-81-1

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 55 mg/mL (89.78 mM)

TargetMolReferences and Literature

1. Marcu MG, et al. The heat shock protein 90 antagonist novobiocin interacts with a previously unrecognized ATP-binding domain in the carboxyl terminus of the chaperone. J Biol Chem. 2000 Nov 24;275(47):37181-6. 2. Ali-Osman F, et al. Topoisomerase II inhibition and altered kinetics of formation and repair of nitrosourea and cisplatin-induced DNA interstrand cross-links and cytotoxicity in human glioblastoma cells. Cancer Res. 1993 Dec 1;53(23):5663-8. 3. Rodríguez-Cerrato V, et al. Comparative efficacy of novobiocin and amoxicillin in experimental sepsis caused by beta-lactam-susceptible and highly resistant pneumococci. Int J Antimicrob Agents. 2010 Jun;35(6):544-9. 4. Eder JP, et al. A phase I clinical trial of novobiocin, a modulator of alkylating agent cytotoxicity. Cancer Res. 1991 Jan 15;51(2):510-3. 5. Bhatia S, et al. Targeting HSP90 dimerization via the C terminus is effective in imatinib-resistant CML and lacks the heat shock response.Blood. 2018 Jul 19;132(3):307-320.

Related compound libraries

This product is contained In the following compound libraries:
Natural Product Library Drug Repurposing Compound Library Natural Product Library for HTS Inhibitor Library Bioactive Compounds Library Max Bioactive Compound Library

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Keywords

Novobiocin 303-81-1 Apoptosis Cytoskeletal Signaling DNA Damage/DNA Repair Metabolism Microbiology/Virology Antibacterial Antibiotic DNA gyrase HSP Virus Protease U-6391 U 6391 U6391 Cathomycin Albamycin inhibitor inhibit