Novobiocin Sodium (NSC 2382)

Catalog No.S2492 Batch:S249216

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Technical Data

Formula

C31H35N2O11.Na
Molecular Weight 634.61 CAS No. 1476-53-5
Solubility (25°C)* In vitro DMSO 100 mg/mL (157.57 mM)
Water 100 mg/mL (157.57 mM)
Ethanol 100 mg/mL (157.57 mM)
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Novobiocin Sodium (NSC 2382, Albamycin, Cathomycin) is an aminocoumarin antibiotic that targets bacterial DNA gyrase (TopoIV), used to treat susceptible gram positive bacteria.
Targets
Topoisomerase II [1] Topoisomerase IV [1]
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.

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    Cell-free assays

  • Concentrations

    1 mM

  • Incubation Time

    1 h

  • Method

    Reticulocyte lysate was treated with novobiocin for 1 h.
Animal Study:

[6]
  • Animal Models

    Female Swiss mice

  • Dosages

    100 or 200 mg/kg

  • Administration

    s.c.

Customer Product Validation

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

Selleck's Novobiocin Sodium (NSC 2382) has been cited by 15 publications

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
Novobiocin blocks nucleic acid binding to Polθ and inhibits stimulation of its ATPase activity [ Nucleic Acids Res, 2023, 51(18):9920-9937] PubMed: 37665033
Targeting polymerase θ impairs tumorigenesis and enhances radiosensitivity in lung adenocarcinoma [ Cancer Sci, 2023, 114(5):1943-1957] PubMed: 36642785
HSP90 C-terminal domain inhibition promotes VDAC1 oligomerization via decreasing K274 mono-ubiquitination in Hepatocellular Carcinoma [ Neoplasia, 2023, 44:100935] PubMed: 37717471
HSP90 C-terminal domain inhibition promotes VDAC1 oligomerization via decreasing K274 mono-ubiquitination in Hepatocellular Carcinoma [ Neoplasia, 2023, 44:100935] PubMed: 37717471
Exploring pharmacokinetics of talazoparib in ABCB1/ABCG2-deficient mice using a novel UHPLC-MS/MS method [ Heliyon, 2023, 9(11):e20972] PubMed: 37908705
Exploring pharmacokinetics of talazoparib in ABCB1/ABCG2-deficient mice using a novel UHPLC-MS/MS method [ Heliyon, 2023, 9(11):e20972] PubMed: 37908705
Hsp90 Inhibitor STA9090 induced VPS35 related extracellular vesicle release and metastasis in hepatocellular carcinoma [ Transl Oncol, 2022, 26:101502] PubMed: 36137350
POLQ suppresses genome instability and alterations in DNA repeat tract lengths [ NAR Cancer, 2022, 4(3):zcac020] PubMed: 35774233

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.