Novobiocin Sodium (NSC 2382)

製品コードS2492 バッチS249212

化学情報

	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)
* <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.

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

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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：

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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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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