Actinonin
Catalog No. T14121 CAS
13434-13-4
Synonyms:
(-)-Actinonin
Actinonin ((-)-Actinonin) is a naturally occurring antibacterial agent produced by Actinomyces and a potent reversible peptide deformylase (PDF) inhibitor with a Ki of 0.28 nM, it also is an apoptosis inducer. Actinonin inhibits aminopeptidase M, aminopeptidase N and leucine aminopeptidase, it 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 has antiproliferative and antitumor activities[1][2][3][4][5].
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Actinonin, CAS 13434-13-4
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Biological Description
Chemical Properties
Storage
& Solubility Information
Description |
Actinonin ((-)-Actinonin) is a naturally occurring antibacterial agent produced by Actinomyces and a potent reversible peptide deformylase (PDF) inhibitor with a Ki of 0.28 nM, it also is an apoptosis inducer. Actinonin inhibits aminopeptidase M, aminopeptidase N and leucine aminopeptidase, it 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 has antiproliferative and antitumor activities[1][2][3][4][5]. |
Targets&IC50 |
PDF:(ki)0.28 nM
|
In vitro |
Actinonin is a chemical compound that effectively inhibits the growth of various human tumor cells, displaying IC50 values ranging from 4 μM to 49.3 μM across multiple cell lines, including Raji, MDA-MB-468, PC3, SK-LC-19, Hela, HT-1080, and AL67[1]. It induces tumor-specific effects, such as mitochondrial membrane depolarization and ATP depletion, in a time- and dose-dependent manner[1]. Furthermore, Actinonin exhibits antimicrobial activity against both Gram-positive bacteria, like S. aureus (MIC 8-16 μg/mL), Streptococcus pyogenes (MIC 8 μg/mL), and Streptococcus epidermidis (MIC 2-4 μg/mL), and Gram-negative bacteria, including H. influenzae (MIC 1-2 μg/mL), Moraxella catarrhalis (MIC 0.5 μg/mL), and Neisseria gonorrheae (MIC 1-4 μg/mL), with notable effectiveness against efflux pump mutants of H. influenzae and E. coli (MIC values of 0.13 μg/mL and 0.25 μg/mL, respectively)[2]. Actinonin targets HsPDF within mitochondria, leading to cell death in tumors, and is a potent inhibitor of peptide deformylases (PDF) from both S. aureus and E. coli, with IC50 values as low as 0.8 nM for Fe-PDF (E. coli) under assay conditions[2].
|
In vivo |
Actinonin, administered safely to mice at doses up to 400 mg/kg as an antibiotic, exhibits remarkable antitumor activity in both intraperitoneal (i.p.) and oral forms in a CWR22 human prostate tumor xenograft model in nude mice, with no observed toxicity[1]. Furthermore, despite its in vitro antitumor efficacy, Actinonin demonstrates no significant toxicity to normal tissues.
|
Synonyms |
(-)-Actinonin
|
Molecular Weight |
385.5
|
Formula |
C19H35N3O5 |
CAS No. |
13434-13-4 |
Storage
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
References and Literature
1.
Lee MD, et al. Human mitochondrial peptide deformylase, a new anticancer target of actinonin-based antibiotics. J Clin Invest. 2004 Oct;114(8):1107-16.
2.
Chen DZ, et al. Actinonin, a naturally occurring antibacterial agent, is a potent deformylase inhibitor. Biochemistry. 2000 Feb 15;39(6):1256-62.
3.
Wahl, R.C., et al. Hydroxamate inhibitors of human gelatinase B (92 kDa). Bioorganic & Medicinal Chemistry Letters 5(4), 349-352 (1995).
4.
Duke SO, et al. Modes of action of microbially-produced phytotoxins. Toxins (Basel). 2011 Aug;3(8):1038-64.
5.
Kruse MN, et al. Human meprin alpha and beta homo-oligomers: cleavage of basement membrane proteins and sensitivity to metalloprotease inhibitors. Biochem J. 2004 Mar 1;378(Pt 2):383-9.
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Keywords
Actinonin
13434-13-4
Metabolism
Aminopeptidase
(-)-Actinonin
inhibitor
inhibit