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)
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GNE-6640
CAS number：2009273-67-8 molecular formula：C20H18N4O
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| Chinese alias | - | ||
| English alias | - | ||
| CAS number | 2009273-67-8 | molecular formula | C20H18N4O |
| molecular weight | 330.4 g/mol | Exact mass | ≥99% |
| PSA | 87.800 Ų | logp | 3.800 |
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