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GNE-6776
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-6776图片
CAS NO:2009273-71-4
包装与价格:
包装价格(元)
1 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

产品名称
GEN6776
产品介绍
GNE6776 是一种具有口服活性的选择性USP7抑制剂。

产品描述

GNE-6776 is a selective USP7 inhibitor.

体外活性

GNE-6776 non-covalently targets USP7 12?? distant from the catalytic cysteine. GNE-6776 attenuates ubiquitin binding and thus inhibits USP7 deubiquitinase activity. GNE-6776 interacts with acidic residues that mediate hydrogen-bond interactions with the ubiquitin Lys48 side chain. GNE-6776 targets cellular USP7, MDM2, and p53 signalling pathways.GNE-6776 selectively inhibits recombinant USP7 relative to 36 other deubiquitinases. GNE-6776 remains selective even at 100?μM, a more than sixfold higher concentration than used in cellular assays. GNE-6776 significantly inhibits USP7 while remaining selective against 44-47 other detected deubiquitinases.

体内活性

Although efficacious exposure is only transiently achieved, GNE-6776 causes modest, although significant, EOL-1 xenograft growth delay.

Cas No.

2009273-71-4

分子式

C20H20N4O2

分子量

348.406

别名

GEN6776

储存和溶解度

DMSO:310 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years