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GNE-6640
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GNE-6640图片
CAS NO:2009273-67-8
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
1 mL*10 mM(in DMSO)电议

产品介绍
GNE 6640 是一种选择性泛素特异性肽酶 7(USP7)的非共价抑制剂,其对全长USP7、USP7 催化结构域、全长USP43 以及 Ub-Mdm2 的IC50值分别为 0.75 μM、0.43 μM、20.3 μM 和 0.23 μM。

产品描述

GNE-6640 is a non-covalent inhibitor of ubiquitin epecific peptidase 7 (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.

体外活性

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.

Cas No.

2009273-67-8

分子式

C20H18N4O

分子量

330.391

储存和溶解度

DMSO:5 mg/mL (15.13 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years