KDM5-C70

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 In Vitro 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: MM.1S myeloma cells Concentration: 10 -9 -10 -5 M Incubation Time: 7 days Result: Showed antiproliferative effects after 7 days of treatment at elevated concentrations. Western Blot AnalysisCell Line: MM.1S myeloma cells Concentration: 50 μM Incubation Time: 7 days Result: Decreased the level of phosphorylation of retinoblastoma protein (Rb). IC50& Target:KDM5 histone demethylase

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