C527 是一种泛 DUB 酶抑制剂，对 USP1/UAF1 复合物具有高效力，IC50值为0.88 μM。

C527 is a is a pan DUB enzyme inhibitor. Which has a high potency for the USP1/UAF1 complex (IC50=0.88 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 and it also 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]. Pretreatment of USP1/UAF1 with C527 resulted in inhibition of its enzyme activity with an IC50 of 0.88±0.03 μM. Pretreatment of cells with the C527 causes an enhancement in the cytoxicity of mitomycin C and camptothecin.

192718-06-2

C17H8FNO3

293.25

DMSO:65 mg/ml (221.65 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years