C527是泛 DUB 酶的抑制剂，对 USP1/UAF1 复合物活性较高， IC50 值为0.88 μM。
| 生物活性 |
C527 is a is a pan DUB enzyme inhibitor, with a high potency for the USP1/UAF1 complex (IC50=0.88 μM). |
|---|---|
| 体外研究 |
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. |
| 分子式 |
C17H8NO3F
|
| 分子量 |
293.25
|
| CAS号 |
192718-06-2
|
| 运输条件 |
Room temperature in continental US; may vary elsewhere. |
| 储存方式 |
4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| 溶解性数据 |
In Vitro:
H2O : < 0.1 mg/mL (insoluble) DMSO : < 1 mg/mL (insoluble or slightly soluble) |
纯度： 98%
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