DB1976

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

DB1976 

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

DB1976 Chemical Structure

CAS No. : 1557397-51-9

规格 价格 是否有货
5 mg ￥4500 询问价格 & 货期
10 mg ￥7500 询问价格 & 货期
50 mg ￥21000 询问价格 & 货期
100 mg ￥29500 询问价格 & 货期

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DB1976 的其他形式现货产品:

DB1976 dihydrochloride

生物活性

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].

IC50 & Target

IC50: 10 nM (Transcription factor PU.1)[1]
体外研究
(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[2].
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[3].
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)[3].
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[3].
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[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

447.35

Formula

C20H16N8Se
CAS 号

1557397-51-9
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [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.

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