生物活性 | |||
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描述 | Puromycin (2HCl), an aminonucleoside antibiotic, inhibits protein synthesis. Puromycin (2HCl), an analog of the 3' end of aminoacyl-tRNA, causes premature termination of translation by being linked non-specifically to growing polypeptide chains. Puromycin acting as a non-inhibitor at very low concentration (e.g. 0.04 microM) can bond only to full-length protein at the C-terminus. Puromycin and its derivatives at concentrations lower than those able to compete effectively with aminoacyl-tRNA can bond specifically to full-length protein at a stop codon[3]. Puromycin is a peptidyl nucleoside endowed with significant antibiotic and anticancer properties, but also with an unfortunate nephrotoxic character that has hampered its use as a chemotherapeutic agent[4]. Moreover, puromycin is a damaging agent known to induce apoptosis in mammalian cells. Puromycin-induced apoptosis in S. cerevisiae[5]. Carbocyclic puromycin was equal to puromycin when evaluated for cytotoxicity using P-388 mouse lymphoid leukemia cells in culture[6]. |
细胞研究 | |||||
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细胞系 | 浓度 | 检测类型 | 检测时间 | 活性说明 | 数据源 |
HEK239 cells | Cytotoxic assay | 72 h | Cytotoxicity against HEK239 cells after 72 hrs by Alamar blue assay, IC50=0.42 μM. | 20558060 | |
human hepatocellular carcinoma cell line (Huh7) | Cytotoxic assay | NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7), CC50=6.63 μM. | 18579783 | ||
human HepG2 cells | Growth inhibition assay | 72 h | Growth inhibition of human HepG2 cells after 72 hrs by SRB assay, IC50=0.21 μM. | 18512984 |
临床研究 | |||||
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NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT01132183 | Healthy | Phase 1 | Completed | - | India ... 展开 >> Bioserve Clinical Research Pvt. Ltd. Hyd, Andhra Pradesh, India, 500 037 收起 << |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.84mL 0.37mL 0.18mL |
9.18mL 1.84mL 0.92mL |
18.37mL 3.67mL 1.84mL |
参考文献 |
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[2]DARKEN MA. PUROMYCIN INHIBITION OF PROTEIN SYNTHESIS. Pharmacol Rev. 1964 Sep;16:223-43. |