| MDL | MFCD01033540 |
|---|---|
| Molecular Weight | 293.25 |
| Molecular Formula | C17H8FNO3 |
| SMILES | O=C1C2=C(N=C(C3=CC=C(F)C=C3)O2)C(C4=CC=CC=C41)=O |
C527 is a is a pan DUB enzyme inhibitor, with a high potency for the USP1/UAF1 complex ( IC 50 =0.88 μM).
0.88 μM (USP1) [1]
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 [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Solid
Room temperature in continental US; may vary elsewhere.
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
H 2 O : < 0.1 mg/mL (insoluble)
DMSO : < 1 mg/mL (insoluble or slightly soluble)