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Submit ReviewP 22077 is an inhibitor of ubiquitin-specific protease (USP) 7 (EC50 = 8.6 μM); also inhibits the closely related deubiquitinase (DUB) USP47. Demonstrates downstream inhibition of HDM2 and claspin in vitro. Inhibits USP7-mediated p53 deubiquitination. Blocks deubiquitination of Tip60 (KAT5) histone lysine acetyltransferase.
P 22077 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. 了解 Tocris 化合物库的更多信息。
分子量 | 315.32 |
公式 | C12H7F2NO3S2 |
储存 | Store at +4°C |
纯度 | ≥99% (HPLC) |
CAS Number | 1247819-59-5 |
PubChem ID | 46931953 |
InChI Key | RMAMGGNACJHXHO-UHFFFAOYSA-N |
Smiles | CC(C1=CC([N+]([O-])=O)=C(SC2=CC=C(F)C=C2F)S1)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 31.53 | 100 |
以下数据基于产品分子量 315.32。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 3.17 mL | 15.86 mL | 31.71 mL |
5 mM | 0.63 mL | 3.17 mL | 6.34 mL |
10 mM | 0.32 mL | 1.59 mL | 3.17 mL |
50 mM | 0.06 mL | 0.32 mL | 0.63 mL |
参考文献是支持产品生物活性的出版物。
Loch et al (2011) Deubiquitylase, deSUMOylase, and deISGylase activity microarrays for assay of substrate preference and functional modifiers. Mol.Cell.Proteomics 10 M100.002402 PMID: 20956615
Tian et al (2011) Characterization of selective ubiquitin and ubiquitin-like protease inhibitors using a fluorescence-based multiplex assay format. Assay Drug Dev.Technol. 9 165 PMID: 21133675
Altun et al (2011) Activity-based chemical proteomics accelerates inhibitor development for deubiquitylating enzymes. Chem.Biol. 18 1401 PMID: 22118674
Dar et al (2013) Deubiquitination of Tip60 by USP7 determines the activity of the p53-dependent apoptotic pathway. Mol.Cell Biol. 33 3309 PMID: 23775119
If you know of a relevant reference for P 22077, please let us know.
关键词: P 22077, P 22077 supplier, P22077, inhibitors, inhibits, ubiquitin-specific, proteases, USP7, DUB, HDM2, claspin, ubiquitin, deubiquitination, anticancer, hausp, Deubiquitinating, Enzymes, 4485, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 P 22077 的部分引用包括:
Lecona et al (2015) USP7 cooperates with SCML2 to regulate the activity of PRC1. Pharmacol Res Perspect 35 1157 PMID: 25605328
Ting-Xin et al (2021) Global feather orientations changed by electric current. iScience 24 102671 PMID: 34179734
Oscar et al (2021) USP7 and VCPFAF1 define the SUMO/Ubiquitin landscape at the DNA replication fork. Cell Rep 37 109819 PMID: 34644576
Ji et al (2019) USP7 inhibits Wnt/β-catenin signaling through promoting stabilization of Axin. Nat Commun 10 4184 PMID: 31519875
Lecona et al (2016) USP7 is a SUMO deubiquitinase essential for DNA replication. Nat Struct Mol Biol 23 270 PMID: 26950370
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平均评分: 4 (基于 2 条评论。)
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P22077 was seen to induce (tumor) cell death with EC50 values in the low micromolar range. P22077 inhibition exhibited changes in ubiquitylated protein levels that are distinct from the broad specificity inhibitor.
HEK293T cells stably expressing the STF-Luc reporter were pretreated with increasing amounts of USP7 inhibitors P22077