放线酰胺素

生物活性靶点体外研究体内研究放线酰胺素试剂级价格

放线酰胺素

CAS号:13434-13-4
英文名:ACTINONIN
中文名:放线酰胺素
CBNumber:CB3273405
分子式:C19H35N3O5
分子量:385.5
MOL File:13434-13-4.mol

放线酰胺素化学性质

熔点 :137-139°C
密度 :1.139±0.06 g/cm3(Predicted)
储存条件 :-20°C
溶解度 :Soluble in DMSO (up to 25 mg/ml) or in Ethanol (up to 20 mg/ml).
酸度系数(pKa) :9.19±0.20(Predicted)
形态 :White to off-white powder.
颜色 :White
BRN :1555250
稳定性 :Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 2 months.
CAS 数据库 :13434-13-4(CAS DataBase Reference)

安全信息

安全说明 :22-24/25
WGK Germany :3
RTECS号 :RG9900700

放线酰胺素性质、用途与生产工艺

生物活性 Actinonin ((-)-Actinonin) 是一种由放线菌产生的天然抗菌剂。Actinonin 抑制氨肽酶 M，氨肽酶 N 和亮氨酸氨肽酶。Actinonin 是一种有效的可逆肽去甲酰基酶 (PDF) 抑制剂，Ki 为 0.28 nM。Actinonin 还抑制 MMP-1，MMP-3，MMP-8，MMP-9 和 hmeprin α 的 Ki 值分别为 300 nM，1,700 nM，190 nM，330 nM 和 20 nM。Actinonin 是一种凋亡诱导剂，具有抗增殖和抗肿瘤活性。
靶点

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
体外研究

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.
体内研究

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.