DB1976,1557397-51-9

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DB1976

CAS No. : 1557397-51-9

MCE 国际站：DB1976

产品活性：DB1976 是一种 DB270 的硒烯类似物，是一种高效且可渗透细胞的转录因子 PU.1 的抑制剂。在体外，DB1976 有效抑制 PU.1 结合 (IC₅₀ 为 10 nM)，可强烈抑制 PU.1/DNA 复合物 (具有高 DB1976-λB 亲和力，K_D 为 12 nM)。DB1976 具有诱导细胞凋亡的作用。

研究领域：Apoptosis

作用靶点：Apoptosis

In Vitro: DB1976 is a classic heterocyclic dication (a single heteroatom) with strong affinity and selectivity for AT-rich sequences commonly found in cognate DNA binding sites for PU.1.
DB1976 inhibits PU.1-dependent transactivation of the reporter in a dose-dependent manner with an IC₅₀ value of 2.4 μM in PU.1-negative HEK293 cells.
DB1976 treatment leads to a profound decrease in the growth of PU.1 URE^–/– AML cells (IC₅₀ of 105 μM), while showing little effect on normal hematopoietic cells at similar concentrations (IC₅₀ of 334 μM).
DB1976 treatment leads to a 1.6-fold increase in apoptotic cells in murine PU.1 URE^–/– AML cells, and observed similar effects in human MOLM13 cells.
DB1976 treatment leads to a significant decrease in the number of viable cells (primary human AML cells) (mean decrease of 81%) and clonogenic capacity (mean decrease of 36%) compared with vehicle-treated cells. The apoptotic cell fraction increased on average by 1.5-fold with DB1976.

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