Home / Deubiquitinating Enzyme Inhibitors / HBX 41108

HBX 41108

Catalog #: 4285
6 Citations Datasheet / COA / SDS
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4285/10
HBX 41108 | CAS No. 924296-39-9 | Deubiquitinating Enzyme Inhibitors
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Description: Selective USP7 inhibitor

Chemical Name: 7-Chloro-9-oxo-9H-indeno[1,2-b]pyrazine-2,3-dicarbonitrile

Purity: ≥98%

Product Details
Citations (6)
Reviews
Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

HBX 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.

Technical Data

M.Wt:
266.64
Formula:
C13H3ClN4O
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
924296-39-9

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.

Additional Information

Licensing Caveats:
Sold for research use only under patent license from Hybrigenics S.A.

Background References

  1. Small-molecule inhibitor of USP7/HAUSP ubiquitin protease stabilizes and activates p53 in cells.
    CollF, Formstecher E, Jacq X et al.
    Mol Cancer Ther
  2. USP7 and TDP-43: Pleiotropic Regulation of Cryptochrome Protein Stability Paces the Oscillation of the Mammalian Circadian Clock

    PLoS ONE, 2016;11(4):e0154263.
  3. Synthesis and biological evaluation of 9-oxo-9H-indeno[1,2-b]pyrazine-2,3-dicarbonitrile analogues as potential inhibitors of deubiquitinating enzymes.
    Colombo et al.
    ChemMedChem, 2010;5:552
  4. A RUNX2 stabilization pathway mediates physiologic and pathologic bone formation
    JM Kim, YS Yang, KH Park, X Ge, R Xu, N Li, M Song, H Chun, S Bok, JF Charles, O Filhol-Coc, B Boldyreff, T Dinter, PB Yu, N Kon, W Gu, T Takarada, MB Greenblatt, JH Shim
    Nat Commun, 2020;11(1):2289.

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Citations for HBX 41108

The citations listed below are publications that use Tocris products. Selected citations for HBX 41108 include:

6 Citations: Showing 1 - 6

  1. Role of the DUB enzyme USP7 in dendritic arborization, neuronal migration, and autistic-like behaviors in mice.
    Authors: Yuda Et al.
    iScience  2022;25:104595
  2. ABPP-HT - High-Throughput Activity-Based Profiling of Deubiquitylating Enzyme Inhibitors in a Cellular Context.
    Authors: Benedikt M Et al.
    Front Chem  2021;9:640105
  3. TGF-β-driven downregulation of the transcription factor TCF7L2 affects Wnt/β-catenin signaling in PDGFRα+ fibroblasts.
    Authors: Hesham Et al.
    J Cell Sci  2020;133
  4. TGF-β-driven downregulation of the Wnt/β-Catenin transcription factor TCF7L2/TCF4 in PDGFRα+ fibroblasts.
    Authors: Hesham Et al.
    J Cell Sci  2020;
  5. USP7 inhibits Wnt/β-catenin signaling through promoting stabilization of Axin.
    Authors: Ji Et al.
    Nat Commun  2019;10:4184
  6. Targeting HAUSP in both p53 wildtype and p53-mutant tumors.
    Authors: Tavana Et al.
    Cell Cycle  2018;:1

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