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13434-13-4

中文名稱 放線酰胺素
英文名稱 ACTINONIN
CAS 13434-13-4
分子式 C19H35N3O5
MDL 編號(hào) MFCD00080257
分子量 385.5
MOL 文件 13434-13-4.mol
更新日期 2024/12/23 10:32:15
13434-13-4 結(jié)構(gòu)式 13434-13-4 結(jié)構(gòu)式

基本信息

中文別名
放線酰胺素
(-)-ACTINONIN
(R)-N4- 羥基-N1-((S)-1-((S)-2-(羥甲基)吡咯烷-1-基)-3-甲基-1-氧代丁-2-基)-2-戊基琥珀酰胺
英文別名
ACTINONIN

物理化學(xué)性質(zhì)

熔點(diǎn)137-139°C
密度1.139±0.06 g/cm3(Predicted)
儲(chǔ)存條件−20°C
儲(chǔ)存條件-20°C
溶解度可溶于DMSO(高達(dá)25mg/ml)或乙醇(高達(dá)20mg/ml)。
酸度系數(shù)(pKa)9.19±0.20(Predicted)
形態(tài)白色至類白色粉末。
顏色白色
BRN1555250
穩(wěn)定性可在-20°下的DMSO或乙醇溶液保存長(zhǎng)達(dá)2個(gè)月。
CAS 數(shù)據(jù)庫(kù)13434-13-4(CAS DataBase Reference)

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險(xiǎn)性描述H302-H315-H319-H335
安全說(shuō)明22-24/25
安全說(shuō)明S22-S24/25
WGK Germany3
WGK Germany3
RTECS號(hào)RG9900700

知名試劑公司產(chǎn)品信息

常見(jiàn)問(wèn)題列表

生物活性
Actinonin ((-)-Actinonin) 是一種由放線菌產(chǎn)生的天然抗菌劑。Actinonin 抑制氨肽酶 M,氨肽酶 N 和亮氨酸氨肽酶。Actinonin 是一種有效的可逆肽去甲酰基酶 (PDF) 抑制劑,Ki 為 0.28 nM。Actinonin 還抑制 MMP-1,MMP-3,MMP-8,MMP-9 和 hmeprin α 的 Ki 值分別為 300 nM,1,700 nM,190 nM,330 nM 和 20 nM。Actinonin 是一種凋亡誘導(dǎo)劑,具有抗增殖和抗腫瘤活性。
靶點(diǎn)

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

體外研究

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.

體內(nèi)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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