A selective inhibitor of ubiquitin-specific protease 7
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P005091

Item No. 15224

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[5-[(2,3-dichlorophenyl)thio]-4-nitro-2-thienyl]-ethanone
CAS Number
882257-11-6
Synonyms
  • P5091
Molecular Formula
C12H7Cl2NO3S2
Formula Weight
348.2
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 3 mg/mlDMF:PBS(pH7.2) (1:2): 0.3 mg/mlDMSO: 0.2 mg/ml
λmax
268, 318 nm
SMILES
ClC1=C(Cl)C(SC2=C([N+]([O-])=O)C=C(C(C)=O)S2)=CC=C1
InChi Code
InChI=1S/C12H7Cl2NO3S2/c1-6(16)10-5-8(15(17)18)12(20-10)19-9-4-2-3-7(13)11(9)14/h2-5H,1H3
InChi Key
LKZLGMAAKNEGCH-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $73

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    10 mg

    $117

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    25 mg

    $251

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    50 mg

    $426

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    Cayman Chemical
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    Product Description

    P005091 is a trisubstituted thiophene that inhibits USP7 and the closely related USP47 (EC50s = 4.2 and 4.3 μM, respectively) with little activity against other classes of proteases, including caspases, cathepsins, calpain, metalloproteases, and serine proteases (EC50s = > 100 μM).1,2 P005091 has been shown to accelerate the degradation of the USP7 substrate HDM2 in several multiple myeloma cell lines (EC50 = 11 μM) and to inhibit the growth of HCT116 human colorectal cancer cells (EC50 = 11 μM) synergistically with doxorubicin, etoposide, or mechlorethamine.1 In vivo, 10 mg/kg P005091 prolongs survival and reduces tumor growth in mice bearing human multiple myeloma and B cell leukemia xenografts.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Chauhan, D., Tian, Z., Nicholson, B., et al. A small molecule inhibitor of ubiquitin-specific protease-7 induces apoptosis in multiple myeloma cells and overcomes bortezomib resistance. Cancer Cell 22(3), 345-358 (2012).

    2. Weinstock, J., Wu, J., Cao, P., et al. Selective dual inhibitors of the cancer-related deubiquitylating proteases USP7 and USP47. ACS Med. Chem. Lett. 3, 789-792 (2012).