An inhibitor of the USP1-UAF1 complex and SARS-CoV-2 PLpro
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SJB2-043

Item No. 36605

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-phenyl-naphth[2,3-d]oxazole-4,9-dione
CAS Number
63388-44-3
Molecular Formula
C17H9NO3
Formula Weight
275.3
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMF: 2 mg/mlDMSO: 1 mg/mlEthanol: insolPBS (pH 7.2): insol
λmax
277 nm
SMILES
O=C1C2=C(C(C3=C1C=CC=C3)=O)OC(C4=CC=CC=C4)=N2
InChi Code
InChI=1S/C17H9NO3/c19-14-11-8-4-5-9-12(11)15(20)16-13(14)18-17(21-16)10-6-2-1-3-7-10/h1-9H
InChi Key
CMYQQADDUUDCCA-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $70

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    10 mg

    $124

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    25 mg

    $256

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    50 mg

    $409

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    Cayman Chemical
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    Product Description

    SJB2-043 is an inhibitor of the ubiquitin-specific peptidase 1 (USP1) and USP1-associated factor 1 (UAF1) complex (USP1-UAF1 complex; IC50 = 0.544 µM for its deubiquitinase activity) and severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) papain-like protease (PLpro).1,2 It reduces the levels of USP1, DNA-binding protein inhibitor 1 (ID-1), ID-2, and ID-3 in K562 chronic myelogenous leukemia (CML) cells when used at concentrations ranging from 0.5 to 10 µM, an effect that can be partially blocked by the proteasome inhibitor MG132.1 SJB2-043 decreases the viability of K562 cells (EC50 = 1.07 µM) and induces apoptosis in K562 cells in a concentration-dependent manner. It also inhibits SARS-CoV-2 PLpro with IC50 values of 0.56 and 0.091 µM using the fluorogenic substrates Z-LRGG-AMC (Item No. 26641) or ubiquitin-AMC (Ub-AMC), respectively, as PLpro substrates.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Mistry, H., Hsieh, G., Buhrlage, S.J., et al. Small-molecule inhibitors of USP1 target ID1 degradation in leukemic cells. Mol. Cancer Ther. 12(12), 2651-2662 (2013).

    2. Cho, C.-C., Li, S.G., Lalonde, T.J., et al. Drug repurposing for the SARS-CoV-2 papain-like protease. ChemMedChem 17(1), e202100455 (2022).