An inhibitor of the USP1/UAF complex
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C527

Item No. 21771

Technical Information
Formal Name
2-(4-fluorophenyl)-naphth[2,3-d]oxazole-4,9-dione
CAS Number
192718-06-2
Molecular Formula
C17H8FNO3
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMF: 0.33 mg/mLDMSO: 0.16 mg/mL
λmax
277 nm
SMILES
O=C(C(OC(C1=CC=C(F)C=C1)=N2)=C2C3=O)C4=C3C=CC=C4
InChi Code
InChI=1S/C17H8FNO3/c18-10-7-5-9(6-8-10)17-19-13-14(20)11-3-1-2-4-12(11)15(21)16(13)22-17/h1-8H
InChi Key
ULJDFEYQOPCCPM-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    C527 is an inhibitor of USP1/UAF complex deubiquitinase activity (IC50 = 0.88 µM).1 It also inhibits USP5, UCL-H3, and USP12/46 but not UCL-H1 activity (IC50s = 1.65, 2.18, 5.97, and >10 µM, respectively). C527 increases ubiquinated Fanconi anemia complementation group D2 (FANCD2-Ub) and FANCI-Ub levels in a concentration-dependent manner. It inhibits homologous recombination repair, cell proliferation, and sensitizes HeLa cells to the DNA crosslinker mitomycin C (Item No. 11435). C527 also inhibits proliferation of PC3 and LNCap prostate cancer cells (IC50s = 0.24 and 0.03 µM, respectively, after 72 hours).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 alSmall-molecule inhibitors of USP1 target ID1 degradation in leukemic cells. Mol. Cancer Ther. 12(12), 2651-2662 (2013).

    2. Brandy, Y., Ononiwu, I., Adedeji, D., et alSynthesis and cytotoxic activities of some 2-arylnaphtho[2,3-d]oxazole-4,9-dione derivatives on androgen-dependent (LNCaP) and androgen-independent (PC3) human prostate cancer cell lines. Invest New Drugs 30(4), 1709-1714 (2012).

    Product Citations

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