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Novobiocin Sodium (NSC 2382)

Name: Novobiocin Sodium (NSC 2382)
Brand: Selleck Chemicals
SKU: S2492
Rating: 5 (13 reviews)

Synonyms: Albamycin,Cathomycin,NSC 2382

Catalog No.S2492 Purity: 99.91%

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

Novobiocin Sodium (NSC 2382) Chemical Structure

CAS: 1476-53-5

Selleck's Novobiocin Sodium (NSC 2382) has been cited by 13 Publications

1 Customer Review

Purity & Quality Control

Batch: Purity: 99.91%

99.91

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Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
MCF7-MX	Function assay			TP_TRANSPORTER: inhibition of mitoxantrone efflux in BCRP-expressing MCF7-MX cells, IC50=25μM	16460798
MELN	Function assay	200 uM	18 hrs	Inhibition of estradiol-induced ER-mediated transcription in MELN cells by measuring luciferase activity at 200 uM after 18 hrs	17979263
SH-SY5Y	Neuroprotection assay			Neuroprotection against beta-amyloid peptide 1-42-induced toxicity in human SH-SY5Y cells assessed as lactate dehydrogenase release, EC50=0.04839μM	19138859
SH-SY5Y	Neuroprotection assay	10 nM		Neuroprotection against beta-amyloid peptide 1-42-induced toxicity in retinoic acid-differentiated human SH-SY5Y cells assessed as lactate dehydrogenase release at 10 nM	19138859
SH-SY5Y	Neuroprotection assay			Neuroprotection against beta-amyloid peptide 1-42-induced toxicity in retinoic acid-differentiated human SH-SY5Y cells assessed as lactate dehydrogenase release	19138859
LNCaP-LN3	Antiproliferative assay			Antiproliferative activity against human LNCaP-LN3 cells, IC50=1.05μM	21129982
yeast PP30	Function assay	100 uM	3 hrs	Inhibition of human HSP90alpha expressed in yeast PP30 cells co-expressing HSF-lacZ reporter assessed as inhibition of heat stress-induced response at 100 uM after 3 hrs	21129982
Sf9	Function assay			Inhibition of Escherichia coli His6-tagged ParC/ParE expressed in baculovirus-infected Sf9 cells by gel electrophoresis, IC50=0.21μM	21235241
SKBR3	Function assay	1000 uM	18 hrs	Inhibition of HSP90 in human SKBR3 cells assessed as aggregation of intracellular HER2 at 1000 uM after 18 hrs by DAPI staining-based immunofluorescence microscopic analysis	23859777
BL21 (DE3) pLysS	Function assay		100 mins	Inhibition of 6-His-tagged Mycobacterium smegmatis GyrB expressed in Escherichia coli BL21 (DE3) pLysS cells incubated for 100 mins in presence of ATP by malachite green dye based ATP assay, IC50=0.18μM	25129171
BL21 (DE3) pLysS	Function assay		100 mins	Inhibition of Mycobacterium smegmatis GyrB ATPase activity expressed in Escherichia coli BL21 (DE3) pLysS cells after 100 mins by inorganic phosphate release detection based malachite green reagent assay, IC50=0.18μM	25801151
BL21 (DE3) pLysS	Function assay		100 mins	Inhibition of Mycobacterium smegmatis DNA gyrase B expressed in Escherichia coli BL21 (DE3) pLysS cells assessed as reduction in ATPase activity incubated for 100 mins by inorganic phosphate detection assay, IC50=0.18μM	26318054
BL21 (DE3) pLysS	Function assay		120 mins	Inhibition of Mycobacterium smegmatis 155 6His-tagged DNA gyrase B catalytic domain ATPase activity expressed in Escherichia coli BL21 (DE3) pLysS cells assessed as inorganic phosphate release after 120 mins in presence of ATP by malachite green dye based, IC50=0.046μM	27371925
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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
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]
Cell Research	Cell lines	Cell-free assays
	Concentrations	1 mM
	Incubation Time	1 h
	Method	Reticulocyte lysate was treated with novobiocin for 1 h.

In Vivo
In vivo	Novobiocin sodium shows anti-infection activity in mice infected with amoxicillin-resistant Streptococcus pneumoniae.
Animal Research	Animal Models	Female Swiss mice
	Dosages	100 or 200 mg/kg
	Administration	s.c.

References

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Chemical lnformation & Solubility

Molecular Weight	634.61	Formula	C₃₁H₃₅N₂O₁₁.Na
CAS No.	1476-53-5	SDF	Download Novobiocin Sodium (NSC 2382) SDF
Smiles	CC1=C(C=CC2=C1OC(=O)C(=C2O)NC(=O)C3=CC(=C(C=C3)[O-])CC=C(C)C)OC4C(C(C(C(O4)(C)C)OC)OC(=O)N)O.[Na+]
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 100 mg/mL ( (157.57 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 100 mg/mL

Ethanol : 100 mg/mL

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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