An inhibitor of USP7
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GNE-6640

Item No. 33751

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[2-amino-4-ethyl-5-(1H-indazol-5-yl)-3-pyridinyl]-phenol
CAS Number
2009273-67-8
Molecular Formula
C20H18N4O
Formula Weight
330.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 1 mg/mlDMSO: 1 mg/mlDMSO:PBS (pH 7.2) (1:2): 0.33 mg/mlEthanol: slightly soluble
SMILES
OC1=CC=C(C2=C(N)N=CC(C3=CC=C4NN=CC4=C3)=C2CC)C=C1
InChi Code
InChI=1S/C20H18N4O/c1-2-16-17(13-5-8-18-14(9-13)10-23-24-18)11-22-20(21)19(16)12-3-6-15(25)7-4-12/h3-11,25H,2H2,1H3,(H2,21,22)(H,23,24)
InChi Key
ZHYXJQQBKROZDX-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $134

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    10 mg

    $213

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    25 mg

    $301

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    50 mg

    $530

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    Cayman Chemical
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    Product Description

    GNE-6640 is an inhibitor of ubiquitin-specific protease 7 (USP7; IC50 = 0.75 µM).1 It is selective for USP7 over USP47 and USP5 (IC50s = 20.3 and >200 µM, respectively). GNE-6640 enhances ubiquitination of the USP7 substrate MDM2 in HCT116 colon cancer cells (IC50 = 0.23 µM) and reduces cell viability in a panel of 108 cell lines (IC50s = <10 µM for all). GNE-6640 (10-70 µM) enhances apoptosis induced by doxorubicin (Item No. 15007) or cisplatin (Item No. 13119) in MCF-7 and U2OS cancer cells, respectively.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kategaya, L., Di Lello, P., Rouge, L., et al. USP7 small-molecule inhibitors interfere with ubiquitin binding. Nature 550(7677), 534-538 (2017).