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DUB 抑制剂 VI,P22077-Calbiochem

DUB Inhibitor VI, P22077-Calbiochem
产品编号:4156681
规格:The DUB Inhibitor VI, P22077 controls the biological activity of DUB. This small molecule/inhibitor is primarily used for Protease Inhibitors applications.
包装规格:25 MG
产品类别:进口试剂
品牌:Sigma-Aldrich
优惠价:立即咨询
产品价格
产品编号包装单位单价(元)国内现货国外库存询价单
415668125 MG3120
产品别名

DUB 抑制剂 VI,P22077-Calbiochem

DUB Inhibitor VI, P22077-Calbiochem

P022077, 1-(5-(2,4-Difluorophenylthio)-4-nitrothiophen-2-yl)ethanone, USP7 Inhibitor II, USP47 Inhibitor II

USP7 Inhibitor II, USP47 Inhibitor II, P022077, 1-(5-(2,4-Difluorophenylthio)-4-nitrothiophen-2-yl)ethanone

结构式
基本信息
Empirical Formula【经验(实验)分子式】
C12H7F2NO3S2
Molecular weight
315.32
MDL number
MFCD22580421
General description【一般描述】
A cell-permeable thiophenylethanone that is shown to inhibit USP7 and USP47 deubiquitinase activity (IC50 = 8.01 & 8.74 µM, respectively), while exhibiting much reduced affinity toward ATXN3, BAP1, and USP1, and displaying no inhibitory activity toward other known PR-619 (Cat. No. 662141) targets (IC50 >50 µM). Both P22077 and PR-619 are shown to increase overall protein polyubiquitination in HEK293T cells in a dose- and time-dependent manner (20 to 150 µM; 0.5 to 20 h), however PR619 treatment results in upregulation of both K48- and K63-linked, while P22077 exposure results in mainly enrichment of K48-linked polyUb chains.
A cell-permeable thiophenylethanone compound that acts a direct, reversible, and selective inhibitor of deubiquitylating enzymes (DUBs) USP7 and USP47 (IC50 = 8.01 & 8.74 µM, respectively). Exhibits only a minimal effect on other DUBs and proteases (>25 µM). Also shown to block UCH-L5 activity in HEK293T cell extracts, but not in intact cells. Stabilizes p53, HDM2, and p21 levels in HEK293T and HCT-116 cells and induces growth arrest (50% cytotoxicity concentration; CC50 = 16.6 and 7.83 µM).

Note: A pan-DUB selective inhibitor PR-619 (Cat. No. 662141) is also available.
Warning【警告】
Toxicity: Standard Handling (A)
Reconstitution【重悬】
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes【其他说明】
Altun, M., et al. 2011. Chem. Biol.18, 1401.
Tian, X., et al. 2011. Assay Drug Dev. Technol.9, 165.
Legal Information【法律信息】
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
产品性质
Quality Level【质量水平】
100
Assay【测定】
≥98% (HPLC)
form【形式】
solid
manufacturer/tradename
Calbiochem®
storage condition【储存条件】
OK to freeze
protect from light
color【颜色】
off-white
solubility【溶解性】
DMSO: 50 mg/mL
shipped in【运输】
ambient
storage temp.【储存温度】
2-8℃
SMILES string
CC(C1=CC([N+]([O-])=O)=C(SC2=CC=C(F)C=C2F)S1)=O
packaging【包装】
25 mg in Glass bottle
Packaged under inert gas
安全信息
Storage Class Code【储存分类代码】
11 - Combustible Solids
WGK
WGK 3
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