Name | C527 |
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Synonyms |
2-(4-Fluorophenyl)naphtho[2,3-d][1,3]oxazole-4,9-dione
MFCD01033540 Naphth[2,3-d]oxazole-4,9-dione, 2-(4-fluorophenyl)- |
Description | C527 is a is a pan DUB enzyme inhibitor, with a high potency for the USP1/UAF1 complex (IC50=0.88 μM). |
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Related Catalog | |
Target |
0.88 μM (USP1)[1] |
In Vitro | Pretreatment of USP1/UAF1 with C527 resulted in inhibition of its enzyme activity with an IC50 of 0.88±0.03 μM. C527 inhibits the DUB activity of the USP12/USP46 complex and other DUB enzymes in vitro. However, the IC50 of C527 for these DUB enzymes was higher in comparison with USP1/UAF1 complex. C527 has considerably less inhibitory effect on UCH-L1 and UCH-L3, a different subclass of DUB enzymes. C527 treatments causes an increase in the levels of Ub-FANCD2 and Ub-FANCI. Pretreatment of cells with the C527 causes an enhancement in the cytoxicity of mitomycin C and camptothecin. C527 treatments lead to an increase in ubiquitinated forms of FANCD2 and FANCI, cause a decrease in homologous recombination activity, and sensitize cells to DNA damaging agents[1]. |
Cell Assay | HeLa cells are treated with DMSO or C527 (0.5, 1, 5 μM) in appropriate medium for 24 to 72 hours. The viable cell counts are determined using Trypan Blue staining, CellTiter-Glo reagent or MTT assay[1]. |
References |
Density | 1.4±0.1 g/cm3 |
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Boiling Point | 488.6±47.0 °C at 760 mmHg |
Molecular Formula | C17H8FNO3 |
Molecular Weight | 293.249 |
Flash Point | 249.3±29.3 °C |
Exact Mass | 293.048828 |
LogP | 4.82 |
Vapour Pressure | 0.0±1.2 mmHg at 25°C |
Index of Refraction | 1.639 |
Storage condition | 2-8℃ |