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。

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.

Solid

IC50: 0.75 μM(full length USP7), 0.43 μM(USP7 catalytic domain), 20.3 μM(full length USP43), 0.23 μM(Ub-MDM2).

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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Kategaya L, et al. USP7 small-molecule inhibitors interfere with ubiquitin binding. Nature. 2017 Oct 26;550(7677):534-538.

In Vitro: DMSO : 5 mg/mL (15.13 mM; Need ultrasonic)配制储备液