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13434-13-4

中文名称 放线酰胺素
英文名称 ACTINONIN
CAS 13434-13-4
分子式 C19H35N3O5
MDL 编号 MFCD00080257
分子量 385.5
MOL 文件 13434-13-4.mol
更新日期 2023/03/20 15:41:27
13434-13-4 结构式 13434-13-4 结构式

基本信息

中文别名
放线酰胺素
(-)-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
英文别名
ACTINONIN

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
BRN1555250
稳定性可在-20°下的DMSO或乙醇溶液保存长达2个月。

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
安全说明22-24/25
安全说明S22-S24/25
WGK Germany3
WGK Germany3
RTECS号RG9900700

知名试剂公司产品信息

常见问题列表

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.

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