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，KD 为 12 nM)。DB1976 具有诱导细胞凋亡的作用。
DB1976 is a selenophene analog of DB270 and a potent and cell-permeable fully efficacious transcription factor PU.1 inhibitor. DB1976 potently inhibits PU.1 binding (IC50 of 10 nM) and strongly inhibits the PU.1/DNA complex (with high DB1976-ΛB affinity, KD of 12 nM) in vitro. DB1976 has apoptosis-inducing effect[1][2][3].
[1]. Munde M, et al. Structure-dependent inhibition of the ETS-family transcription factor PU.1 by novel heterocyclic diamidines. Nucleic Acids Res. 2014 Jan;42(2):1379-90. [2]. Stephens DC, et al. Pharmacologic efficacy of PU.1 inhibition by heterocyclic dications: a mechanistic analysis. Nucleic Acids Res. 2016 May 19;44(9):4005-13. [3]. Antony-Debré I, et al. Pharmacological inhibition of the transcription factor PU.1 in leukemia. J Clin Invest. 2017 Dec 1;127(12):4297-4313.
动态评分
0.0