DM-01 是一种强效的选择性EZH2抑制剂,可用于弥漫性大 B 细胞淋巴瘤 (DLBCL),滤泡性淋巴瘤 (FL) 和 SNF5/INI-1/SMARCB1 基因相关实体瘤的研究。
产品描述
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].
体外活性
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 IC 50 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 IC 50 s 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.
Cas No.
2355280-00-9
分子式
C23H24F3N3O2
分子量
431.45
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years