| Identification | Back Directory | [Name]
2-(4-Fluorophenyl)naphtho[2,3-d]oxazole-4,9-dione | [CAS]
192718-06-2 | [Synonyms]
C527
C527 >=98% (HPLC)
2-(4-Fluorophenyl)naphtho[2,3-d]oxazole-4,9-dione
2-(4-Fluorophenyl)-naphth[2,3-d]oxazole-4,9-dione
Naphth[2,3-d]oxazole-4,9-dione, 2-(4-fluorophenyl)- | [Molecular Formula]
C17H8FNO3 | [MDL Number]
MFCD01033540 | [MOL File]
192718-06-2.mol | [Molecular Weight]
293.25 |
| Chemical Properties | Back Directory | [Boiling point ]
488.6±47.0 °C(Predicted) | [density ]
1.433±0.06 g/cm3(Predicted) | [storage temp. ]
Sealed in dry,Room Temperature | [solubility ]
DMSO: soluble0.3mg/mL, clear (warmed) | [form ]
powder | [pka]
-4.21±0.20(Predicted) | [color ]
faint yellow to dark yellow |
| Hazard Information | Back Directory | [Uses]
C527 is a is a pan DUB enzyme inhibitor, with a high potency for the USP1/UAF1 complex (IC50=0.88 μM). | [Biological Activity]
C527 is a pan-DUB enzyme inhibitor with high activity against USP1/UAF1 complex with IC50 value of 0.88 μM. | [in vitro]
Pretreatment of USP1/UAF1 with C527 resulted in inhibition of its enzyme activity with an IC 50 of 0.88±0.03 μM. C527 inhibits the DUB activity of the USP12/USP46 complex and other DUB enzymes in vitro . However, the IC 50 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. | [target]
| [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. DOI:10.1158/1535-7163.MCT-13-0103-T |
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