GNE-6640,2009273-67-8

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GNE-6640

CAS No. : 2009273-67-8

MCE 国际站：GNE-6640

产品活性：GNE-6640 是泛素特异性肽酶 7 (USP7) 选择性的、非共价结合的抑制剂，其对USP7 全长，USP7 催化结构域，USP43 全长以及 Ub-MDM2 的 IC₅₀ 值分别为 0.75 μM，0.43 μM，20.3 μM 和 0.23 μM。

研究领域：Cell Cycle/DNA Damage

作用靶点：Deubiquitinase

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 IC₅₀ ≤ 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.

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