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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.
M. Wt | 266.64 |
Formula | C13H3ClN4O |
Storage | Store at -20°C |
Purity | ≥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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 26.66 | 100 |
The following data is based on the product molecular weight 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.
Concentration / Solvent Volume / Mass | 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 |
References are publications that support the biological activity of the product.
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.
Keywords: HBX 41108, HBX 41108 supplier, HBX41108, ubiquitin-specific, proteases, usp7, selective, inhibitors, inhibits, proteasome, ubiquitin, deubiquitination, hausp, herpesvirus-associated, Deubiquitinating, Enzymes, 4285, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for HBX 41108 include:
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
Do you know of a great paper that uses HBX 41108 from Tocris? Please let us know.
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HEK293T cells stably expressing the STF-Luc reporter were pretreated with increasing amounts of USP7 inhibitors HBX41108