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Submit ReviewHBX 41108 is an inhibitor of ubiquitin-specific protease (USP) 7 activity (IC50 = 424 nM). Displays uncompetitive inhibition. Also inhibits USP7-mediated p53 deubiquitination (IC50 = 0.8 μM). Stabilizes p53 and inhibits cancer cell growth; induces p53-dependent apoptosis in p53 wild type and null isogenic cancer cell lines.
Sold for research use only under patent license from Hybrigenics S.A.
分子量 | 266.64 |
公式 | C13H3ClN4O |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 924296-39-9 |
PubChem ID | 16065773 |
InChI Key | BIGPXXAUSQLTQR-UHFFFAOYSA-N |
Smiles | O=C2C1=CC(Cl)=CC=C1C3=C2N=C(C#N)C(C#N)=N3 |
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 | 26.66 | 100 |
以下数据基于产品分子量 266.64。 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 | 3.75 mL | 18.75 mL | 37.5 mL |
5 mM | 0.75 mL | 3.75 mL | 7.5 mL |
10 mM | 0.38 mL | 1.88 mL | 3.75 mL |
50 mM | 0.08 mL | 0.38 mL | 0.75 mL |
参考文献是支持产品生物活性的出版物。
Colland et al (2009) Small-molecule inhibitor of USP7/HAUSP ubiquitin protease stabilizes and activates p53 in cells. Mol.Cancer Ther. 8 2286 PMID: 19671755
Colombo et al (2010) Synthesis and biological evaluation of 9-oxo-9H-indeno[1,2-b]pyrazine-2,3-dicarbonitrile analogues as potential inhibitors of deubiquitinating enzymes. ChemMedChem 5 552 PMID: 20186914
If you know of a relevant reference for HBX 41108, please let us know.
关键词: HBX 41108, HBX 41108 supplier, HBX41108, ubiquitin-specific, proteases, usp7, selective, inhibitors, inhibits, proteasome, ubiquitin, deubiquitination, hausp, herpesvirus-associated, Deubiquitinating, Enzymes, 4285, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 HBX 41108 的部分引用包括:
Hesham et al (2020) TGF-β-driven downregulation of the Wnt/β-Catenin transcription factor TCF7L2/TCF4 in PDGFRα+ fibroblasts. J Cell Sci PMID: 34005169
Hesham et al (2020) TGF-β-driven downregulation of the transcription factor TCF7L2 affects Wnt/β-catenin signaling in PDGFRα+ fibroblasts. J Cell Sci 133 PMID: 32434871
Benedikt M et al (2021) ABPP-HT - High-Throughput Activity-Based Profiling of Deubiquitylating Enzyme Inhibitors in a Cellular Context. Front Chem 9 640105 PMID: 33718328
Ji et al (2019) USP7 inhibits Wnt/β-catenin signaling through promoting stabilization of Axin. Nat Commun 10 4184 PMID: 31519875
Tavana et al (2018) Targeting HAUSP in both p53 wildtype and p53-mutant tumors. Cell Cycle 1 PMID: 29616860
Yuda et al (2022) Role of the DUB enzyme USP7 in dendritic arborization, neuronal migration, and autistic-like behaviors in mice. iScience 25 104595 PMID: 35800757
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HEK293T cells stably expressing the STF-Luc reporter were pretreated with increasing amounts of USP7 inhibitors HBX41108