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Novobiocin sodium/新生霉素(钠盐) {[allProObj[0].p_purity_real_show]}

货号:A299620 同义名: 新生霉素钠 / Albamycin sodium; Cathomycin sodium

Novobiocin sodium是一种来源于Streptomyces niveus的抗生素。

Novobiocin sodium/新生霉素(钠盐) 化学结构 CAS号:1476-53-5
Novobiocin sodium/新生霉素(钠盐) 化学结构
CAS号:1476-53-5
Novobiocin sodium/新生霉素(钠盐) 3D分子结构
CAS号:1476-53-5
Novobiocin sodium/新生霉素(钠盐) 化学结构 CAS号:1476-53-5
Novobiocin sodium/新生霉素(钠盐) 3D分子结构 CAS号:1476-53-5
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Novobiocin sodium/新生霉素(钠盐) 纯度/质量文件 产品仅供科研

货号:A299620 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Topo I Topo II Topo IV Topoisomerase 其他靶点 纯度
Ellagic acid 98%
β-Lapachone 99%+
(s)-10-hydroxycamptothecin 98+%
Camptothecin ++

Topo I, IC50: 0.68 μM

98%
Betulinic acid ++

Eukaryotic topoisomerase I, IC50: 5 μM

98%
Topotecan ++++

Topo I (DU-145 Luc cells), IC50: 2 nM

Topo I (MCF-7 Luc cells), IC50: 13 nM

98%
Irinotecan HCl Trihydrate 98%
SN-38 98%
Levofloxacin hydrate 98%
Dexrazoxane 99%+
Ofloxacin 98+%
Enoxacin 99%+
Flumequine +

Topo II, IC50: 15 μM

98%
Levofloxacin 97%
Etoposide 98%
Pefloxacin mesylate dihydrate 99+%
Marbofloxacin 98+%
Voreloxin HCl 98%
Mitoxantrone 2HCl PKC 98%
Nalidixic acid 98%
Doxorubicin 97%
Novobiocin sodium 95%
Amonafide 99%+
Pirarubicin 98%+
Idarubicin HCl +++

Topo II (MCF-7 cells), IC50: 3.3 ng/mL

99%+
Genistein EGFR 98%
Teniposide 98%
Moxifloxacin 98%
Ciprofloxacin 98%
Clinafloxacin 99%
Gatifloxacin 98%
Daunorubicin HCl +++

DNA synthesis, Ki: 20 nM

98%
Epirubicin HCl 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Novobiocin sodium/新生霉素(钠盐) 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].

Novobiocin sodium/新生霉素(钠盐) 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 <<

Novobiocin sodium/新生霉素(钠盐) 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

Novobiocin sodium/新生霉素(钠盐) 实验方案

计算器
存储液制备 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

Novobiocin sodium/新生霉素(钠盐) 技术信息

CAS号1476-53-5
分子式C31H35N2NaO11
分子量 634.61
SMILES Code CC1=C(OC2=O)C(C(O)=C2NC(C3=CC(C/C=C(C)/C)=C([O-])C=C3)=O)=CC=C1O[C@H](OC(C)(C)[C@H](OC)[C@H]4OC(N)=O)[C@@H]4O.[Na+]
MDL No. MFCD00066541
别名 新生霉素钠 ;Albamycin sodium; Cathomycin sodium; Novobiocin (sodium salt); NSC 2382
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Keep in dark place, inert atmosphere, 2-8°C

溶解方案

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

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