Novobiocin Sodium (NSC 2382)

製品コードS2492 バッチS249213

印刷

化学情報

 Chemical Structure Synonyms Albamycin,Cathomycin,NSC 2382 Storage
(From the date of receipt)
3 years -20°C powder
1 years -80°C in solvent
化学式

C31H35N2O11.Na

分子量 634.61 CAS No. 1476-53-5
Solubility (25°C)* 体外 DMSO 100 mg/mL (157.57 mM)
Water 100 mg/mL (157.57 mM)
Ethanol 100 mg/mL (157.57 mM)
体内 (毎回新しく調製した物を用意してください)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液(一定の濃度)を調合する

生物活性

製品説明 Novobiocin Sodium (NSC 2382, Albamycin, Cathomycin) is an aminocoumarin antibiotic that targets bacterial DNA gyrase (TopoIV), used to treat susceptible gram positive bacteria.
in vitro

Novobiocin also interacts with Hsp90, altering the affinity of the chaperone for geldanamycin and radicicol and causing in vitro and in vivo depletion of key regulatory Hsp90-dependent kinases including v-Src, Raf-1, and p185(ErbB2). Novobiocin interferes with association of the co-chaperones Hsc70 and p23 with Hsp90. [1]

Novobiocin specifically inhibits the maturation of the heme-regulated eIF2alpha kinase (HRI) in a concentration-dependent manner. Novobiocin induces the dissociation of Hsp90 and Cdc37 from immature HRI, while the Hsp90 cochaperones p23, FKBP52, and protein phosphatase 5 remained associated with immature HRI. [2]

Novobiocin causes morphological and biochemical changes which lead to induction of cell death exhibiting characteristic features of metazoan apoptosis. [3]

Novobiocin, a HSP90 inhibitor, could decrease the expression of SMYD3 and dose dependently inhibit the proliferation and migration of MDA-MB-231 human breast cancer cells. Novobiocin can inhibit the migration of breast cancer cells and such event may involve the downregulation of SMYD3. [4]

Novobiocin, an aminocoumarin antibiotic, interferes with heat shock protein 90 and hypoxia inducible factor dependent gene expression and thus compromises cell survival. Novobiocin (500 礛) results in a significant increase of [Ca(2+)]i, decrease of forward scatter, increase of annexin-V-binding and enhances ceramide formation. Novobiocin stimulates eryptosis, an effect at least in part due to entry of extracellular Ca(2+) and formation of ceramide. [5]

in vivo

Novobiocin sodium shows anti-infection activity in mice infected with amoxicillin-resistant Streptococcus pneumoniae.

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Cell-free assays
濃度 1 mM
反応時間 1 h
実験の流れ

Reticulocyte lysate was treated with novobiocin for 1 h.

動物実験 動物モデル Female Swiss mice
投薬量 100 or 200 mg/kg
投与方法 s.c.

参考

  • https://pubmed.ncbi.nlm.nih.gov/10945979/
  • https://pubmed.ncbi.nlm.nih.gov/15209518/
  • https://pubmed.ncbi.nlm.nih.gov/15811527/
  • https://pubmed.ncbi.nlm.nih.gov/20039369/
  • https://pubmed.ncbi.nlm.nih.gov/24643001/
  • https://pubmed.ncbi.nlm.nih.gov/20303716/

カスタマーフィードバック

, , Mol Cancer, 2014, 13(1):265.

Selleckの高級品が、幾つかの出版された研究調査結果(以下を含む)で使われた:

Hsp90 C-terminal domain inhibition enhances ferroptosis by disrupting GPX4-VDAC1 interaction to increase HMOX1 release from oligomerized VDAC1 channels [ Redox Biol, 2025, 85:103672] PubMed: 40472773
Polymerase theta inhibition impairs tumor growth and amplifies melphalan-induced DNA damage in multiple myeloma [ J Transl Med, 2025, 23(1):1079] PubMed: 41074018
Repurposing amiodarone for bladder cancer treatment [ Cancer Res Commun, 2025, 10.1158/2767-9764.CRC-24-0433] PubMed: 40353763
Propafenone facilitates mitochondrial-associated ferroptosis and synergizes with immunotherapy in melanoma [ J Immunother Cancer, 2024, 12(11)e009805] PubMed: 39581704
Loss of POLE3-POLE4 unleashes replicative gap accumulation upon treatment with PARP inhibitors [ Cell Rep, 2024, 43(5):114205] PubMed: 38753485
Hsp90α promotes lipogenesis by stabilizing FASN and promoting FASN transcription via LXRα in hepatocellular carcinoma [ J Lipid Res, 2024, 66(1):100721] PubMed: 39645039
The Proteogenomics of Prostate Cancer Radioresistance [ Cancer Res Commun, 2024, 10.1158/2767-9764.CRC-24-0292] PubMed: 39166898
Polymerase θ inhibition activates the cGAS-STING pathway and cooperates with immune checkpoint blockade in models of BRCA-deficient cancer [ Nat Commun, 2023, 14(1):1390] PubMed: 36914658
Polymerase θ inhibition activates the cGAS-STING pathway and cooperates with immune checkpoint blockade in models of BRCA-deficient cancer [ Nat Commun, 2023, 14(1):1390] PubMed: 36914658
POLQ inhibition elicits an immune response in homologous recombination-deficient pancreatic adenocarcinoma via cGAS/STING signaling [ J Clin Invest, 2023, 133(11)e165934] PubMed: 36976649

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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