product name Novobiocin Sodium
Description: Novobiocin Sodium is an antibiotic of the aminocoumarin class that targets bacterial DNA gyrase (TopoIV), it is used to treat susceptible gram positive bacteria. 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.
References: J Biol Chem. 2000 Nov 24;275(47):37181-6; Biochemistry. 2004 Jun 29;43(25):8217-29.
634.61
Formula
C31H35N2O11.Na
CAS No.
1476-53-5
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 127 mg/mL (200.1 mM)
Water: 127 mg/mL (200.1 mM)
Ethanol: 127 mg/mL (200.1 mM)
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: 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 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. Kinase Assay: Cell Assay: |
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| In Vivo | |
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| Formulation & Dosage | |
| References | J Biol Chem. 2000 Nov 24;275(47):37181-6; Biochemistry. 2004 Jun 29;43(25):8217-29. |
