13434-13-4
基本信息
(-)-ACTINONIN
(R)-N4- 羟基-N1-((S)-1-((S)-2-(羟甲基)吡咯烷-1-基)-3-甲基-1-氧代丁-2-基)-2-戊基琥珀酰胺
物理化学性质
| 熔点 | 137-139°C |
| 密度 | 1.139±0.06 g/cm3(Predicted) |
| 储存条件 | −20°C |
| 储存条件 | -20°C |
| 溶解度 | 可溶于DMSO（高达25mg/ml）或乙醇（高达20mg/ml）。 |
| 酸度系数(pKa) | 9.19±0.20(Predicted) |
| 形态 | 白色至类白色粉末。 |
| 颜色 | 白色 |
| BRN | 1555250 |
| 稳定性 | 可在-20°下的DMSO或乙醇溶液保存长达2个月。 |
| CAS 数据库 | 13434-13-4(CAS DataBase Reference) |
安全数据
| 危险性符号(GHS) |  GHS07 |
| 警示词 | 警告 |
| 危险性描述 | H302-H315-H319-H335 |
| 防范说明 | P261-P280-P301+P312-P302+P352-P305+P351+P338 |
| 安全说明 | 22-24/25 |
| 安全说明 | S22-S24/25 |
| WGK Germany | 3 |
| WGK Germany | 3 |
| RTECS号 | RG9900700 |
知名试剂公司产品信息
常见问题列表
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
Actinonin inhibits cell growth in various human tumor cell lines. The IC
50
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 IC
50
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. aureus
), respectively.
Actinonin is active against Gram-positive bacteria, including
S. aureus
(MIC value of 8-16 µg/mL),
Streptococcus pyogenes
(MIC value of 8 µg/mL) and
Streptococcus epidermidis
(MIC value of 2-4 µg/mL). Actinonin is also active against fastidious Gramne-gative bacteria, such as
H. influenzae
(MIC value of 1-2 µg/mL),
Moraxella catarrhalis
(MIC value of 0.5 µg/mL), and
Neisseria gonorrheae
(MIC value of 1-4 µg/mL). Actinonin is very active against the
H. influenzae acr
(MIC value of 0.13 µg/mL) and
E. coli acr
(MIC value of 0.25 µg/mL) efflux pump mutants.
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.