产品
编 号:F190091
分子式:C17H28N4O3
分子量:336.43
产品类型
结构图
CAS No: 1596348-32-1
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产品详情
生物活性:
KDM5-C70 is an ethyl ester derivative of KDM5-C49 and a potent, cell-permeable and pan-KDM5 histone demethylase inhibitor. KDM5-C70 has an antiproliferative effect in myeloma cells, leading to genome-wide elevation of H3K4me3 levels.
体外研究:
KDM5-C70 (10-9-10-5 M; 7 days; MM.1S myeloma cells) treatment shows antiproliferative effects after 7 days of treatment at elevated concentrations (estimated 50% reduction of viability/proliferation for KDM5-C70 at ~20 μM).KDM5-C70 (50 μM; 7 days; MM.1S myeloma cells)treatment decreases the level of phosphorylation of retinoblastoma protein (Rb), while leaving the total level of phosphorylated Rb (pRb) unchanged, indicating impairment of cell cycle progression.Chromatin immunoprecipitation followed by next-generation sequencing shows an increase in H3K4me3 levels around transcription start sites with KDM5-C70 but little change with GSK467A at 50 μM inhibitor concentrations.