GNE-6776
产品说明书
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同义名 : | GEN-6776 |
| CAS号 : | 2009273-71-4 | |
| 货号 : | A955293 | |
| 分子式 : | C20H20N4O2 | |
| 纯度 : | 99%+ | |
| 分子量 : | 348.4 | |
| MDL号 : | MFCD31657364 | |
| 存储条件： |
Pure form Keep in dark place, inert atmosphere, 2-8°C In solvent -20°C:1个月-80°C:12个月 |
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| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
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| 描述 | Deubiquitinase enzymes cleave ubiquitin from substrates and are implicated in disease; for example, ubiquitin-specific protease-7 (USP7) regulates stability of the p53 tumour suppressor and other proteins critical for tumour cell survival[2]. GNE-6776 is a selective USP7 inhibitor. It non-covalently targets USP7 12 Å distant from the catalytic cysteine and attenuates ubiquitin binding and thus inhibits USP7 deubiquitinase activity. GNE-6776 targets cellular USP7, MDM2, and p53 signaling pathways but selectively inhibits recombinant USP7 relative to 36 other deubiquitinases. Notably, GNE-6776 remains selective even at 100 μM, a more than sixfold higher concentration than used in cellular assays[2]. Although efficacious exposure is only transiently achieved, GNE-6776 causes modest, although significant, EOL-1 xenograft growth delay[2]. | ||
| 作用机制 | GNE-6776 interacts with acidic residues that mediate hydrogen-bond interactions with the ubiquitin Lys48 side chain. | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.87mL 0.57mL 0.29mL |
14.35mL 2.87mL 1.44mL |
28.70mL 5.74mL 2.87mL |
| 参考文献 |
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