C527CAS号: 192718-06-2分子式: C17H8FNO3分子量: 293.25描述纯度储存/保存方法外观可溶性/溶解性靶点In vitro(体外研究)
产品描述 | |
描述 |
C527 is a is a pan DUB enzyme inhibitor, with a high potency for the USP1/UAF1 complex (IC50=0.88 μM).
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纯度 |
98%
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储存/保存方法 |
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
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基本信息 | |
外观 |
Faint yellow to dark yellow powder
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可溶性/溶解性 |
H2O : 1 mg/mL (3.41 mM)
DMSO : 1 mg/mL (3.41 mM) |
生物活性 | |
靶点 |
USP1
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In vitro(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.
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分子结构图