Actinonin ((-)-Actinonin) is a naturally occurring antibacterial agent produced byActinomyces. Actinonin inhibitsaminopeptidaseM,aminopeptidaseNandleucineaminopeptidase. Actinonin is a potent reversiblepeptide deformylase (PDF)inhibitor with aK_iof 0.28 nM. Actinonin also inhibitsMMP-1,MMP-3,MMP-8,MMP-9, andhmeprin αwithK_ivalues of 300 nM, 1,700 nM, 190 nM, 330 nM, and 20 nM, respectively. Actinonin is anapoptosisinducer. Actinonin has antiproliferative and antitumor activities^{[1][2][3][4][5]}.

Ki: 0.28 nM (Peptide deformylase (PDF))^[2], 300 nM (MMP-1), 1,700 nM (MMP-3), 190 nM (MMP-8), 330 nM (MMP-9)^[3], and 20 nM (hmeprin α)^[5]
Apoptosis^[1]
Aminopeptidase M, Aminopeptidase N and Leucine aminopeptidase^[1]

Actinonin inhibits cell growth in various human tumor cell lines. The IC₅₀of 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^[1].
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^[1].
Actinonin is a potent inhibitor of all three forms (Zn-, Ni-, and Fe-) of peptide deformylases from bothS. aureusandE. colibacteria. Under the assay conditions, the IC₅₀values 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. aureus), respectively^[2].
Actinonin is active against Gram-positive bacteria, includingS. aureus(MIC value of 8-16 μg/mL),Streptococcus pyogenes(MIC value of 8 μg/mL) andStreptococcus epidermidis(MIC value of 2-4 μg/mL). Actinonin is also active against fastidious Gramne-gative bacteria, such asH. influenzae(MIC value of 1-2 μg/mL),Moraxella catarrhalis(MIC value of 0.5 μg/mL), andNeisseria gonorrheae(MIC value of 1-4 μg/mL). Actinonin is very active against theH. influenzae acr(MIC value of 0.13 μg/mL) andE. coli acr(MIC value of 0.25 μg/mL) efflux pump mutants^[2].

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^[1].

385.50

Solid

C₁₉H₃₅N₃O₅

13434-13-4

• Others

actinomycete

Room temperature in continental US; may vary elsewhere.

DMSO : 50 mg/mL(129.70 mM;Need ultrasonic)

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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40%PEG300   5%Tween-80   45% saline

  Solubility: ≥ 5 mg/mL (12.97 mM); Clear solution

  此方案可获得 ≥ 5 mg/mL (12.97 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液
• 2.

  请依序添加每种溶剂： 10% DMSO    90% (20%SBE-β-CDin saline)

  Solubility: 5 mg/mL (12.97 mM); Suspended solution; Need ultrasonic

  此方案可获得 5 mg/mL (12.97 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

  以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
• 3.

  请依序添加每种溶剂： 10% DMSO    90%corn oil

  Solubility: ≥ 5 mg/mL (12.97 mM); Clear solution

  此方案可获得 ≥ 5 mg/mL (12.97 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。