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Novobiocin sodium

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Chemical Structure| 1476-53-5 同义名 : 新生霉素钠 ;Albamycin sodium;Cathomycin sodium;Novobiocin (sodium salt);NSC 2382
CAS号 : 1476-53-5
货号 : A299620
分子式 : C31H35N2NaO11
纯度 : 95%
分子量 : 634.606
MDL号 : MFCD00066541
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(47.27 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 50 mg/mL(78.79 mM)，配合低频超声助溶
动物实验配方：
生物活性
靶点

  • Topo II
描述 Novobiocin is an orally active antibiotic that inhibits DNA gyrase by binding the ATP-binding site in the ATPase subunit[3]. Novobiocin not only inhibits DNA gyrase but also binds and stimulates LptB, the ATPase that powers LPS transport[4]. Novobiocin, an old antibiotic, was tested in vitro and in a murine sepsis model against one amoxicillin-susceptible and three amoxicillin-resistant strains (minimum inhibitory concentrations (MICs) 8-64 mg/L)[5]. Novobiocin is shown to inhibit melanoma B16 cell proliferation. Growth inhibition by novobiocin was accompanied by phenotypic alterations, that included morphological changes, lipid accumulation and marked increases in the activities of NADPH cytochrome c reductase and gamma glutamyl transpeptidase[6]. Novobiocin, a HSP90 inhibitor, could decrease the expression of SMYD3 (SET and MYND domain-containing protein 3) and dose dependently inhibit the proliferation and migration of MDA-MB-231 human breast cancer cells[7]. Novobiocin and cDDP (cisplatin) or BCNU (carmustine) markedly reduced in vivo growth of a murine fibrosarcoma without increased host toxicity[8].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02099240 Osteomyelitis Early Phase 1 Recruiting September 2019 United States, Kentucky ... 展开 >> University of Louisville Recruiting Louisville, Kentucky, United States, 40202 Contact: Julio A Ramirez, MD    502-852-1148    jarami01@louisville.edu    Contact: David Seligson, MD    502-852-0923    d0seli01@louisville.edu    Sub-Investigator: Forest Arnold, DO          Sub-Investigator: Timothy Wiemkwn, PhD          Sub-Investigator: Robert Kelley, PhD          Sub-Investigator: James Summersgill, PhD          Sub-Investigator: Ruth Carrico, PhD          Sub-Investigator: Julie Harting, PharmD          Sub-Investigator: Paula Peyrani, MD          Principal Investigator: David Seligson, MD          Sub-Investigator: Craig Roberts, MD          Principal Investigator: Julio Ramirez, MD 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.58mL

0.32mL

0.16mL

7.88mL

1.58mL

0.79mL

15.76mL

3.15mL

1.58mL
参考文献

[1]Yun BG, Huang W, et al. Novobiocin induces a distinct conformation of Hsp90 and alters Hsp90-cochaperone-client interactions. Biochemistry. 2004 Jun 29;43(25):8217-29.

[2]Marcu MG, Chadli A, 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.

[3]May JM, Owens TW, Mandler MD, Simpson BW, Lazarus MB, Sherman DJ, Davis RM, Okuda S, Massefski W, Ruiz N, Kahne D. The Antibiotic Novobiocin Binds and Activates the ATPase That Powers Lipopolysaccharide Transport. J Am Chem Soc. 2017 Dec 6;139(48):17221-17224

[4]Mandler MD, Baidin V, Lee J, Pahil KS, Owens TW, Kahne D. Novobiocin Enhances Polymyxin Activity by Stimulating Lipopolysaccharide Transport. J Am Chem Soc. 2018 Jun 6;140(22):6749-6753

[5]Rodríguez-Cerrato V, Del Prado G, Huelves L, Naves P, Ruiz V, García E, Ponte C, Soriano F. 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

[6]Nordenberg J, Albukrek D, Hadar T, Fux A, Wasserman L, Novogrodsky A, Sidi Y. Novobiocin-induced anti-proliferative and differentiating effects in melanoma B16. Br J Cancer. 1992 Feb;65(2):183-8

[7]Luo XG, Zou JN, Wang SZ, Zhang TC, Xi T. Novobiocin decreases SMYD3 expression and inhibits the migration of MDA-MB-231 human breast cancer cells. IUBMB Life. 2010 Mar;62(3):194-9

[8]Eder JP, Teicher BA, Holden SA, Cathcart KN, Schnipper LE. Novobiocin enhances alkylating agent cytotoxicity and DNA interstrand crosslinks in a murine model. J Clin Invest. 1987 May;79(5):1524-8