CPI-455 hydrochloride

CPI-455 hydrochloride CAS号: 2095432-28-1分子式: C16H15ClN4O分子量: 314.77描述纯度储存/保存方法可溶性/溶解性靶点In vitro(体外研究)

产品描述
描述
CPI-455 hydrochloride is a specific, pan-KDM5 inhibitor with an IC50 of 10 nM for KDM5A. CPI-455 hydrochloride mediates KDM5 inhibition, elevates global levels of H3K4me3, and decreases the number of drug-tolerant persister cancer cells in multiple cancer cell line models treated with standard chemotherapy or targeted agents.
纯度
98%
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.
基本信息
可溶性/溶解性
DMSO : 63 mg/mL ( 200.14 mM)
生物活性
靶点
KDM5A (Cell-free assay)10 nM
In vitro(体外研究)
CPI-455 mediates KDM5 inhibition, elevates global levels of H3K4 trimethylation (H3K4me3) and decreases the number of DTPs in multiple cancer cell line models treated with standard chemotherapy or targeted agents[1]. CPI-455 has a high measured affinity for the target KDM5 proteins. Within 24 hours, CPI-455 and CPI-766 can dose-dependently increases in H3K4me3, but not H3K4me2. IC50 calculation for KDM5 Inhibitor CPI-455 in 3 luminal breast cancer cell lines MCF-7, T-47 and EFM-19 are 35.4, 26.19 and 16.13 μM, respectively.