CAS:1628208-23-0CPI-455

CPI-455 is a selective inhibitor of KDM5 demethylases and can reduce survival of drug-tolerant cancer cells.

规格	价格	促销价格	库存

18817579266

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咨询

18817579266

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实验数据

技术信息

CAS号

1628208-23-0

储存条件

分子式

C16H14N4O

运输

蓝冰

分子量

278.31

别名

溶解度

DMSO	34.0 mg/mL (122.2 mM)

动物实验配方

生物活性

描述CPI-455 is a specific KDM5 inhibitor with IC50 value of 10nM for inhibition of full-length KDM5A in enzymatic assays. CPI-455-mediated KDM5 inhibition resulted in a dose-dependent increase in global H3K4me3 in HeLa cells. Also it induced a time-dependent increase in H3K4me3 that was detected only after 2 or more days of treatment. The elevation of H3K4 trimethylation mediated by this inhibition of KDM5 by CPI-455 decreased the number of drug-tolerant state in multiple cancer cell line models treated with standard chemotherapy or targeted agents.
作用机制The nitrile of CPI-455 makes a single interaction with the active-site metal ion of KDM5. The position occupied by CPI-455 completely overlaps the binding site of 2-OG, demonstrating a competitive mode of action.^[1]