Actinonin
(Synonyms: 放线酰胺素,(-)-Actinonin,Ro 06-1467) 目录号 : GC16350An aminopeptidase inhibitor
Cas No.:13434-13-4
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Actinonin is a peptidomimetic antibiotic produced by Actinomyces that inhibits aminopeptidases. It inhibits the following matrix metalloproteinases (MMPs): MMP-1 (Ki = 300 nM), MMP-3 (Ki = 1,700 nM), MMP-8 (Ki = 130 nM), and MMP-9 (Ki = 330 nM).[1] Actinonin acts as an herbicide by targeting plastid peptide deformylase, an enzyme required for N-terminal processing of plastid-encoded proteins.[2] Actinonin has also been identified as an effective inhibitor of human meprin α (Ki = 20 nM), a zinc endopeptidase that cleaves matrix proteins.[3] More recently actinonin has been shown to inhibit tumor cell invasion and matrix degradation and to induce apoptosis in animal models by targeting human mitochondrial peptide deformylase.[4]
Reference:
[1]. Wahl, R.C., Pulvino, T.A., Mathiowetz, A.M., et al. Hydroxamate inhibitors of human gelatinase B (92 kDa). Bioorganic & Medicinal Chemistry Letters 5(4), 349-352 (1995).
[2]. Duke, S.O., and Dayan, F.E. Modes of action of microbially-produced phytotoxins. Toxins (Basel) 3(8), 1038-1064 (2011).
[3]. Kruse, M.N., Becker, C., Lottaz, D., et al. Human meprin α and β homo-oligomers: Cleavage of basement membrane proteins and sensitivity to metalloprotease inhibitors. Biochemistry Journal 378(1), 383-389 (2004).
[4]. Lee, M.D., She, Y., Soskis, M.J., et al. Human mitochondrial peptide deformylase, a new anticancer target of actinonin-based antibiotics. Journal of Clinical Investigation 114(8), 1107-1116 (2004).
Cas No. | 13434-13-4 | SDF | |
别名 | 放线酰胺素,(-)-Actinonin,Ro 06-1467 | ||
化学名 | (2R)-N4-hydroxy-N1-[(1S)-1-[[(2S)-2-(hydroxymethyl)-1-pyrrolidinyl]carbonyl]-2-methylpropyl]-2-pentyl-butanediamide | ||
Canonical SMILES | O=C([C@H](C(C)C)NC([C@H](CCCCC)CC(NO)=O)=O)N1CCC[C@H]1CO | ||
分子式 | C19H35N3O5 | 分子量 | 385.5 |
溶解度 | 30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide | 储存条件 | Store at -20°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.594 mL | 12.9702 mL | 25.9403 mL |
5 mM | 0.5188 mL | 2.594 mL | 5.1881 mL |
10 mM | 0.2594 mL | 1.297 mL | 2.594 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。