货号 | 2978/50 |
别名 | 4-[4-[(5-Nitro-2-furanyl)methylene] |
供应商 | Tocris |
生物活性 | Cell-permeable, irreversible ubiquitin-activating enzyme (E1) inhibitor (IC50 < 10 μM). Blocks ubiquitylation and prevents ubiquitin-mediated proteasomal degradation. Inhibits NF-κB activation, blocks degradation of p53, increases p21 levels and induces apoptosis in vitro. Also causes an increase in sumoylation of proteins. |
运输条件 | Blue Ice |
存放说明 | -20℃ |
纯度 | >98 % |
计算分子量 | 371.3 |
分子式 | C17H13N3O7 |
可溶性/溶解性 | Soluble to 100 mM in DMSO |
参考文献 | Brahemiet al (2010) Homology modelling of human E1 ubiquitin activating enzyme. Lett.Drug Des.Discov. 7 57. PMID: 20396627. Miet al (2009) Cancer preventative isothiocyanates induce selective degradation of cellular α- and β-tubulins by proteasomes. J.Biol.Chem. 284 17039. PMID: 19339240. Yanget al (2007) Inhibitors of ubiquitin-activating enzyme (E1), a new class of potential cancer therapeutics. Cancer Res. 67 9472. PMID: 17909057. |