GNE-6640
规格
| Cas Number | 2009273-67-8 |
| 规格或纯度 | ≥99% |
| 纯度 | ≥99% |
| 包装 | 50mg 或 10mg 或 5mg 或 25mg |
产品信息
| 品牌 | 阿拉丁 |
| 溶解性 | DMSO : 5 mg/mL (15.13 mM; Need ultrasonic) |
| 过滤标签 | Deubiquitinase,Cell Cycle/DNA Damage |
| 储存温度 | -20°C储存 |
| 运输条件 | 超低温冰袋运输 |
| 生化和生理学机理 | GNE-6640 是泛素表特异性肽酶 7 (USP7) 的一种选择性非共价抑制剂，对全长 USP7、USP7 催化域、全长 USP43 和 Ub-MDM2 的 IC 50 值分别为 0.75 μM、0.43 μM、20.3 μM 和 0.23 μM。 |
| 英文描述 |
GNE-6640 is a selective and non-covalent inhibitor of ubiquitin epecific peptidase 7 (USP7) , with IC 50 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 In Vitro GNE-6640 promotes endogenous MDM2 ubiquitination with Lys48 (K48)-linked polyubiquitin chains, which directs proteasomal degradation13. GNE-6640 targets cellular USP7, MDM2, and p53 signalling pathways. GNE-6640 decreases viability of 108 cell lines with IC 50 ≤ 10 μM. Combining GNE-6640 with doxorubicin or cisplatin (DNA-damaging agents), which could activate the p53 response and enhance USP7 inhibitor efficacy. GNE-6640 could induce tumor cell death. GNE-6640 enhances cytotoxicity with chemotherapeutic agents and targeted compounds, including PIM kinase inhibitors. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:IC50: 0.75 μM(full length USP7), 0.43 μM(USP7 catalytic domain), 20.3 μM(full length USP43), 0.23 μM(Ub-MDM2) |