GNE-6640
产品说明书
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同义名 : | - |
| CAS号 : | 2009273-67-8 | |
| 货号 : | A858171 | |
| 分子式 : | C20H18N4O | |
| 纯度 : | 99%+ | |
| 分子量 : | 330.38 | |
| MDL号 : | MFCD31807618 | |
| 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-6640 is a selective and non-covalent inhibitor of USP7, with IC50 values of 0.75 μM, 0.43 μM, 20.3 μM and 0.23 μM for full length USP7, USP7 catalytic domain, full length USP43 and Ub-MDM2, respectively[2]. GNE-6640 promoted endogenous MDM2 ubiquitination with Lys48 (K48)-linked polyubiquitin chains, which direct proteasomal degradation and it targeted cellular USP7, MDM2, and p53 signalling pathways[2]. GNE-6640 decreased viability of 54 cell lines with IC50 ≤ 10 μM. Acute myeloid leukaemia (AML) cell lines had increased sensitivity to GNE-6640[2]. Combining GNE-6640 with doxorubicin or cisplatin (DNA-damaging agents) could activate the p53 response and enhance USP7 inhibitory efficacy. GNE-6640 could also induce tumor cell death and enhance cytotoxicity with chemotherapeutic agents and targeted compounds, including PIM kinase inhibitors[2]. | ||
| 作用机制 | GNE-6640 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 |
3.03mL 0.61mL 0.30mL |
15.13mL 3.03mL 1.51mL |
30.27mL 6.05mL 3.03mL |
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