Actinonin (Synonyms: (-)-Actinonin)
目录号: PC61716 纯度: 10mM*1mL in DMSO
CAS No. :13434-13-4
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中文名称
Actinonin
中文别名
放线酰胺素;(-)-放线酰胺素;(±)-6,6-二溴-1,1-二-2-萘酚
英文名称
Actinonin
英文别名
(R)-N4-Hydroxy-N1-((S)-1-((S)-2-(hydroxymethyl)pyrrolidin-1-yl)-3-methyl-1-oxobutan-2-yl)-2-pentylsuccinamide;(-)-Actinonin;ACTINONIN;Actinonin​;Butanediamide,N4-hydroxy-N1-[(1S)-1-[[(2S)-2-(hydroxymethyl)-1-pyrrolidinyl]carbonyl]-2-methyl...;Butanediamide,N4-hydroxy-N1-[(1S)-1-[[(2S)-2-(hydroxymethyl)-1-pyrrolidinyl]carbonyl]-2-methylpropyl]-2-pentyl-,(2R)-;Actinonine;3-[[1-[(2-(Hydroxymethyl)-1-pyrrolidinyl)carbonyl]-2-methylpropyl]carbamoyl]octanohydroxamic acid;octanohydroxamicacid,3-((1-((2-(hydroxymethyl)-1-pyrrolidinyl)carbonyl)-2-met;3-[[1-[[2-(HYDROXYMETHYL)-1-PYRROLIDINYL]CARBONYL]-2-METHYL-PROPYL]CARBAMOYL]OCTANOHYDROXAMIC ACID;N'-Hydroxy-N-[1-[[2-(hydroxymethyl)-1-pyrrolidinyl]carbonyl]-2-methylpropyl]-2-pentylbutanediamide;3-[[1-[[2-(HYDROXYMETHYL)-1-PYRROLIDINYL]-CARBONYL]-2-METHYLPROPYL]-CARBAMOYL]-OCTONOHYDROXAMIC ACID;N4-HYDROXY-N1-[(1S)-1[[(2S)-2-(HYDROXYMETHYL)-1-PYRROLDINYL]CARBONYL]-2-METHYLPROPYL]-2-PENTYL-,(2R)-(9CI);Butanediamide, N4-hydroxy-N1-(1S)-1-(2S)-2-(hydroxymethyl)-1-pyrrolidinylcarbonyl-2-methylpropyl-2-pentyl-, (2R)-;hylpropyl)carbamoyl)-
Cas No.
13434-13-4
分子式
C19H35N3O5
分子量
385.50
包装储存
Powder; -20°C; 3 years;In solvent; -80°C; 6 months;
生物活性
Actinonin ((-)-Actinonin) is a naturally occurring antibacterial agent produced by Actinomyces. Actinonin inhibits aminopeptidase M, aminopeptidase N and leucine aminopeptidase. Actinonin is a potent reversible peptide deformylase (PDF) inhibitor with a Ki of 0.28 nM. Actinonin also inhibits MMP-1, MMP-3, MMP-8, MMP-9, and hmeprin α with Ki values of 300 nM, 1,700 nM, 190 nM, 330 nM, and 20 nM, respectively. Actinonin is an apoptosis inducer. Actinonin has antiproliferative and antitumor activities.
性状
Solid
IC50 & Target[1][2]
Ki: 0.28 nM (Peptide deformylase (PDF)), 300 nM (MMP-1), 1,700 nM (MMP-3), 190 nM (MMP-8), 330 nM(MMP-9), and 20 nM (hmeprin α)
Apoptosis
Aminopeptidase M, Aminopeptidase N and Leucine aminopeptidase
体外研究(In Vitro)
Actinonin inhibits cell growth in various human tumor cell lines. The IC50 of 4, 6.9, 12.8, 16.6, 27.4, 15.7 and 49.3 μM for Raji cells, MDA-MB-468 cells,PC3 cells, SK-LC-19 cells, Hela cells, HT-1080 cells and AL67 cells, respectively.
HsPDF is a critical target of actinonin and that the inhibition of this protein in the mitochondria leads to cell death in tumor cells. Actinonin treatment of cells led to a tumor-specific mitochondrial membrane depolarization and ATP depletion in a time- and dose-dependent manner.
Actinonin is a potent inhibitor of all three forms (Zn-, Ni-, and Fe-) of peptide deformylases from both S. aureus and E. coli bacteria. Under the assay conditions, the IC50 values for Actinonin are 90, 3, 0.8, and 11 nM for Zn-PDF (E. coli), Ni-PDF (E. coli), Fe-PDF (E. coli), and Ni-PDF (S. aureu
体内研究(In Vivo)
Actinonin has been safely administered to mice as an antibiotic at doses up to 400 mg/kg. Actinonin does not appear to have significant toxicity to normal tissues, despite its antitumor activity in vitro. Remarkably, Actinonin exhibits significant antitumor activity when given i.p. or orally in a CWR22 human prostate tumor xenograft model in nude mice. During treatment, the animals show no signs of toxicity.Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature or refrigerated transport.
储存方式
Powder; -20°C; 3 years;In solvent; -80°C; 6 months;
结构分类
Others
来源
actinomycete
溶解度数据
体外研究:
DMSO : 50 mg/mL(129.70 mM;Need ultrasonic)
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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