An inhibitor of USP7
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HBX 41108

Item No. 23759

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
7-chloro-9-oxo-9H-indeno[1,2-b]pyrazine-2,3-dicarbonitrile
CAS Number
924296-39-9
Molecular Formula
C13H3ClN4O
Formula Weight
266.6
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMSO: 33 mg/mlDMSO:PBS (pH 7.2) (1:40): 0.2 mg/ml
λmax
312 nm
SMILES
O=C1C2=NC(C#N)=C(C#N)N=C2C3=C1C=C(Cl)C=C3
InChi Code
InChI=1S/C13H3ClN4O/c14-6-1-2-7-8(3-6)13(19)12-11(7)17-9(4-15)10(5-16)18-12/h1-3H
InChi Key
BIGPXXAUSQLTQR-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $41

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    5 mg

    $178

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    10 mg

    $293

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    25 mg

    $680

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    Cayman Chemical
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    Product Description

    HBX 41108 is an uncompetitive, reversible inhibitor of ubiquitin-specific protease 7 (USP7) activity (IC50 = 424 nM).1 It dose-dependently inhibits USP7-mediated p53 deubiquitination in a cell-free assay, with an IC50 value of approximately 0.8 µM, as well as in HEK293 cells. It is selective for USP7 over a panel of proteases including aspartic, serine, and metalloproteases (IC50s = >10 µM), several cysteine proteases (IC50s = >1 and >10 µM), and the deubiquitinating enzymes UCH-L1 (IC50 = >1 µM) and SENP1 (IC50 = >10 µM). HBX 41108 increases the levels of p53 and p21/WAF1, a p53 target gene. It also dose-dependently inhibits proliferation of HCT116 cells with an IC50 value of approximately 1 µM and induces apoptosis.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Colland, F., Formstecher, E., Jacq, X., et al. Small-molecule inhibitor of USP7/HAUSP ubiquitin protease stabilizes and activates p53 in cells. Mol. Cancer Ther. 8(8), 2286-2295 (2009).