Puromycin 2HCl

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Chemical Structure| 58-58-2 同义名 : 嘌呤霉素二盐酸盐水合物 ;CL13900 dihydrochloride; Puromycin(hydrochloride); PDH; NSC 3055; CL13900 2HCl; Puromycin 2HCl; Puromycin(dihydrochloride)
CAS号 : 58-58-2
货号 : A547954
分子式 : C22H31Cl2N7O5
纯度 : 99%+
分子量 : 544.43
MDL号 : MFCD00012691
存储条件：

Pure form Inert atmosphere, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(45.92 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 50 mg/mL(91.84 mM)

无水乙醇: 5 mg/mL(9.18 mM)，配合低频超声，并水浴加热至45℃助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇
生物活性
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
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
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
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

[1]Watanabe S, Iwamoto M, et al. A novel method for the production of transgenic cloned pigs: electroporation-mediated gene transfer to non-cultured cells and subsequent selection with puromycin. Biol Reprod. 2005 Feb;72(2):309-15.

[2]DARKEN MA. PUROMYCIN INHIBITION OF PROTEIN SYNTHESIS. Pharmacol Rev. 1964 Sep;16:223-43.

[3]Miyamoto-Sato E, Nemoto N, Kobayashi K, Yanagawa H. Specific bonding of puromycin to full-length protein at the C-terminus. Nucleic Acids Res. 2000;28(5):1176‐1182

[4]Carter J, Weaver BA, Chiacchio MA, et al. Synthesis, stereochemical characterization, and antimicrobial evaluation of a potentially nonnephrotoxic 3'-C-acethydrazide puromycin analog. Nucleosides Nucleotides Nucleic Acids. 2017;36(3):224‐241

[5]Citterio B, Albertini MC, Ghibelli L, et al. Multiparameter analysis of apoptosis in puromycin-treated Saccharomyces cerevisiae. Arch Microbiol. 2015;197(6):773‐780

[6]Vince R, Daluge S, Brownell J. Carbocyclic puromycin: synthesis and inhibition of protein biosynthesis. J Med Chem. 1986;29(11):2400‐2403