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192718-06-2

192718-06-2 structure
192718-06-2 structure

Name C527
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).
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

[1]. Mistry H, et al. Small-molecule inhibitors of USP1 target ID1 degradation in leukemic cells. Mol Cancer Ther. 2013 Dec;12(12):2651-62.

Density 1.4±0.1 g/cm3
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℃
Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H302
RIDADR NONH for all modes of transport
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