| Size | Price | Stock | Qty |
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| 5mg |
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Novobiocin (Cathomycin, U6591, U-6591, Inabiocin, Albadry, Streptonivicin, Albamycin) is an orally bioactive and coumarin-based antibiotic isolated from Streptomyces niveus with the potential for highly beta-lactam-resistant pneumococcal infections and has anti-orthopoxvirus activity. It is a DNA gyrase inhibitor and a heat shock protein 90 (Hsp90) antagonist, acting by binding to DNA gyrase, and blocking adenosine triphosphatase (ATPase) activity.
| ln Vitro |
Novobiocin (1 mM) disrupts nucleotide binding by competitively inhibiting ATP binding to gyrase B. It also interferes with the co-chaperones' connection with Hsp90, namely Hsc70 and p23[1]. Novobiocin (200 µM; 24 h) reduces the clonogenic survival of human glioblastoma multiforme cells by inhibiting the rate of repair of both cis-DDP and BCNU-induced DNA interstrand cross-links[2]. Novobiocin (0.3 mM; 48 hours) causes an approximately three- to five-fold increase in apoptotic cells in K562, HL60, and Mutz-2 experiments that are dependent on the caspase-3/7 enzyme[5].
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| ln Vivo |
Anti-infection activity of Novobiocin (25, 50, 100, and 200 mg/kg; sc; four times at 1, 5, 24, and 48 hours after infection) has been shown in mice infected with Streptococcus pneumoniae that is resistant to amoxicillin[3].
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| Animal Protocol |
Animal/Disease Models: 30 g adult female Swiss mice (sepsis induced by the penicillin-susceptible strain (AR33118))[3]
Doses: 25, 50, 100, 200 mg/kg Route of Administration: Sc; given at 1, 5, 24 and 48 h after infection Experimental Results: demonstrated anti-infection activity in mice infected with amoxicillin-resistant S. pneumoniae. |
| References |
[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. [6]. Smee DF. Progress in the discovery of compounds inhibiting orthopoxviruses in animal models. Antivir Chem Chemother. 2008;19(3):115-24. |
| Molecular Formula |
C31H36N2O11
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|---|---|
| Molecular Weight |
612.63
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| Exact Mass |
612.2319
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| CAS # |
303-81-1
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| Related CAS # |
Novobiocin sodium;1476-53-5
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| SMILES |
C/C(=C/CC1C(O)=CC=C(C(NC2C(=O)OC3C(=C(O[C@@H]4OC(C)(C)[C@H](OC)[C@@H](OC(=O)N)[C@H]4O)C=CC=3C=2O)C)=O)C=1)/C
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| Synonyms |
U-6391 U 6391 NovobiocinCathomycin,U6591, U-6591, Inabiocin, Albadry, Streptonivicin, Albamycin
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6323 mL | 8.1615 mL | 16.3231 mL | |
| 5 mM | 0.3265 mL | 1.6323 mL | 3.2646 mL | |
| 10 mM | 0.1632 mL | 0.8162 mL | 1.6323 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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