DM-01

DM-01 is a powerful and selective EZH2 inhibitor for the research of diffuse large B-cell lymphoma (DLBCL), follicular lymphoma (FL), and SNF5/INI-1/SMARCB1 genetically defined solid tumors[1].

Research Areas >> Cancer

Signaling Pathways >> Epigenetics >> Histone Methyltransferase

EZH2

Knockdown EZH2 in A549 cells results in the decrease of cell sensitivity to DM-01 at 50 and 100 μM concentrations. DM-01 also shows comparable inhibitory activity for K562 cells with an IC50 value of 58.706 μΜ[1]. DM-01 (5 and 10 μM; 24 hours) strongly inhibits the activity of EZH2 and results in abolished H3K27me expression in K562 cells[1]. DM-01 (5 and 10 μM) also increases the transcription expression of DIRAS3 in a dose dependent manner, a tumor suppressor in downstream of EZH2[1]. Cell Viability Assay[1] Cell Line: A549 sh-EV and A549 sh-EZH2 cells Concentration: 1, 5, 10, 50, 100 μM Incubation Time: 48 hours Result: The IC50s of 72.748 and 269.7 μΜ for A549 sh-EV and A549 sh-EZH2 cells, respectively. Western Blot Analysis[1] Cell Line: K562 cells Concentration: 5, 10 μM Incubation Time: 24 hours Result: Inhibited the activity of EZH2 and resulted in abolished H3K27me expression.

[1]. Qifan Zhou, et al. Design, synthesis and biological activities of pyrrole-3-carboxamide derivatives as EZH2 (enhancer of zeste homologue 2) inhibitors and anticancer agents. New Journal of Chemistry. 10 Jan 2020.