| Actinoninpeptidomimetic antibiotic that inhibits aminopeptidases |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
- View current batch:
- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
Actinonin Dilution Calculator
calculate
Actinonin Molarity Calculator
calculate
| Cas No. | 13434-13-4 | SDF | Download SDF |
| Synonyms | (-)-Actinonin,Ro 06-1467 | ||
| Chemical Name | (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 | ||
| Formula | C19H35N3O5 | M.Wt | 385.5 |
| Solubility | ≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
Actinonin is an antibiotic and CD13/aminopeptidase N (APN) inhibitor. Actinonin is a naturally occuring antibacterial agent produced by antinomycete with potent deformylase inhibitory effect [1].
In vitro: Actinonin showed an inhibitory effect in cell growth. The in vitro IC50 values of actinonin against NB4, HL6O human cell lines, AKR mouse leukemia cells CD13-negative cell lines RA.JI and DAUDI human lymphoma were about 2-5 μg/ml. Cell cycle analysis indicated that actinonin induced a G1 arrest in NB4 and HL6O cells. Intracellular flow cytometry showed that actinonin could induce cell apoptosis in 20-35% of the cells [2]. Actinonin dose-dependently inhibited the three forms (Zn-, Ni-, and Fe-) of peptide deformylases from both S. aureus and E. coli bacteria. The IC50 values of actinonin were 90, 3, 0.8, and 11 nM for Zn-PDF (E. coli), Ni-PDF (E. coli), Fe-PDF (E. coli), and Ni-PDF (S. aureus), respectively [2]. Actinonin is a tight binding inhibitor of E. coli Ni-PDF with a Ki of 0.3 nM [3].
In vivo: Actinonin showed dose-dependent antitumor effects on AKR leukemia, resulting in a survival advantage. In the syngeneic AKR mouse leukemia model, treatment with 100 p.g actinonin daily for 3 days beginning at day 3 after transplantation showed significant antitumor effects [2].
References:[1]. Gordon J J, Kelly B K, Miller G A. Actinonin: an antibiotic substance produced by an actinomycete[J]. Nature, 1962, 195: 701-702.[2]. Xu Y, Lai L T, Gabrilove J L, et al. Antitumor activity of actinonin in vitro and in vivo[J]. Clinical cancer research, 1998, 4(1): 171-176.[3]. Chen D Z, Patel D V, Hackbarth C J, et al. Actinonin, a naturally occurring antibacterial agent, is a potent deformylase inhibitor[J]. Biochemistry, 2000, 39(6): 1256-1262.
