Molecular Formula | C17H8FNO3 |
Molar Mass | 293.25 |
Density | 1.433±0.06 g/cm3(Predicted) |
Boling Point | 488.6±47.0 °C(Predicted) |
Solubility | DMSO: soluble0.3mg/mL, clear (warmed) |
Appearance | powder |
Color | faint yellow to dark yellow |
pKa | -4.21±0.20(Predicted) |
Storage Condition | Sealed in dry,Room Temperature |
In vitro study | 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. |
Hazard Symbols | Xn - Harmful |
Risk Codes | 22 - Harmful if swallowed |
Safety Description | 46 - If swallowed, seek medical advice immediately and show this container or label. |
WGK Germany | 3 |
biological activity | C527 is a pan-DUB enzyme inhibitor with high activity for USP1/UAF1 complex, the IC50 value was 0.88 μm. |
Target | 0.88 μm (USP1) |