Home Metabolism HSP Remmer Novobiocin Sodium (Cathomycin, Albamycin)

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Novobiocin Sodium (Cathomycin, Albamycin) Hsp90 C-terminale remmer

Cat.nr.: S2492

Novobiocin Sodium (NSC 2382, Albamycin, Cathomycin) is een aminocoumarine-antibioticum dat bacteriële DNA-gyrase (TopoIV) aanvalt en wordt gebruikt om gevoelige grampositieve bacteriën te behandelen.
Novobiocin Sodium (Cathomycin, Albamycin) HSP Remmer Chemical Structure

Chemische structuur

Molecuulgewicht: 634.61

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Kwaliteitscontrole (Quality Control)

Batch: Zuiverheid: 99.91%
99.91

Celkweek, behandeling & werkzame concentratie
(Cell Culture, Treatment & Working Concentration)

Cellijnen Assaytype Concentratie Incubatietijd Formulering Activiteitsbeschrijving 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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Chemische informatie, opslag en stabiliteit (Chemical Information, Storage & Stability)

Molecuulgewicht 634.61 Formule

C31H35N2O11.Na

 Opslag (vanaf de datum van ontvangst)
CAS-nr. 1476-53-5 SDF downloaden Opslag van stamoplossingen

Synoniemen Albamycin,Cathomycin,NSC 2382 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+]

Oplosbaarheid (Solubility)

In vitro
Batch:

DMSO : 100 mg/mL (157.57 mM)
(Met vocht verontreinigd DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Water : 100 mg/mL

Ethanol : 100 mg/mL

Molariteitscalculator

Massa Concentratie Volume Molecuulgewicht
Verdunningscalculator Molecuulgewichtcalculator

In vivo
Batch:

In vivo formulatiecalculator (heldere oplossing)

Stap 1: Voer onderstaande informatie in (Aanbevolen: een extra dier om rekening te houden met verlies tijdens het experiment)

mg/kg g μL

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in de sectie oplosbaarheid.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-moedervloeistof: mg geneesmiddel vooropgelost in μL DMSO ( Concentratie moedervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de batch van het geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toeμL PEG300, mengen en verhelderen, daarna toevoegenμL Tween 80, mengen en verhelderen, daarna toevoegen μL ddH2O, mengen en verhelderen.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toe μL Maïsolie, mengen en verhelderen.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysieke methoden zoals vortexen, ultrasoon of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme (Mechanism of Action)

Targets/IC50/Ki
Topoisomerase II
Topoisomerase IV
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.

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.

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

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.

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.

In vivo

Novobiocin sodium shows anti-infection activity in mice infected with amoxicillin-resistant Streptococcus pneumoniae.
Referenties
  • [4] https://pubmed.ncbi.nlm.nih.gov/20039369/
  • [5] https://pubmed.ncbi.nlm.nih.gov/24643001/
  • [6] https://pubmed.ncbi.nlm.nih.gov/20303716/