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Potent and selective ubiquitin specific peptidase USP8 deubiquitinase (DUB) inhibitor.
DUBs-IN-2 is a potent and selective ubiquitin specific peptidase USP8 deubiquitinase (DUB) inhibitor (IC50 = 280 nM/USP8, >100 µM/USP7). DUBs-IN-2 inhibits the proliferation of gastric cancer (GC) cell NCI-N87 in cultures (IC50 = 480 nM post 3-day incubation) and NCI-N87-derived tumor growth in mice in vivo (2 mg/kg/d 5x per wk) by promoting HER-2 degradation.
DUBs-IN-2 is a potent and selective ubiquitin specific peptidase USP8 deubiquitinase (DUB) inhibitor (IC50 = 280 nM/USP8, >100 µM/USP7). DUBs-IN-2 inhibits the proliferation of gastric cancer (GC) cell NCI-N87 in cultures (IC50 = 480 nM post 3-day incubation) and NCI-N87-derived tumor growth in mice in vivo (2 mg/kg/d 5x per wk) by promoting HER-2 degradation.
訊號詞
Warning
危險聲明
危險分類
Acute Tox. 4 Oral
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
Jiangang Sun et al.
OncoTargets and therapy, 13, 9941-9952 (2020-10-30)
Referring to global cancer statistics, the incidence of gastric cancer (GC) was ranked sixth; however, detailed mechanisms underlying its development were not thoroughly investigated. Previous studies have reported that inhibition of ubiquitin-specific peptidase 8 (USP8) induced degradation of several receptor
Matteo Colombo et al.
ChemMedChem, 5(4), 552-558 (2010-02-27)
High-throughput screening highlighted 9-oxo-9H-indeno[1,2-b]pyrazine-2,3-dicarbonitrile (1) as an active inhibitor of ubiquitin-specific proteases (USPs), a family of hydrolytic enzymes involved in the removal of ubiquitin from protein substrates. The chemical behavior of compound 1 was examined. Moreover, the synthesis and in
Wenjun Xiong et al.
Nature communications, 13(1), 1700-1700 (2022-04-02)
Anti-PD-1/PD-L1 immunotherapy has achieved impressive therapeutic outcomes in patients with multiple cancer types. However, the underlined molecular mechanism(s) for moderate response rate (15-25%) or resistance to PD-1/PD-L1 blockade remains not completely understood. Here, we report that inhibiting the deubiquitinase, USP8
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