DC-BPi-11

• 常用名: DC-BPi-11
• 英文名: DC-BPi-11
• CAS号: 2758411-61-7
• 分子量: 397.49
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₀H₂₃N₅O₂S
• 熔点: N/A
• 闪点: N/A

DC-BPi-11用途

DC-BPi-11是溴结构域PHD指转录因子(BPTF)的抑制剂,IC50值为698nM。DC-BPi-11显示出对白血病细胞增殖的显著抑制[1]。

DC-BPi-11名称

• 英文名: DC-BPi-11

DC-BPi-11生物活性

• 描述: DC-BPi-11是溴结构域PHD指转录因子(BPTF)的抑制剂,IC50值为698nM。DC-BPi-11显示出对白血病细胞增殖的显著抑制[1]。
• 相关类别:
  研究领域 >> 癌症
  信号通路 >> 表观遗传学 >> 表观遗传读者域
• 靶点实验:

  698 nM (BPTF)[1]

• 体外研究: DC-BPi-11(0.1 nM-1μM；24小时)抑制人白血病MV-4-11细胞中的BPTF,EC50值为120 nM[1]。DC-BPi-11(0.01μM-100μM；24小时)显著抑制人白血病MV-4-11细胞的增殖(IC50=0.89μM),并且(2.5-20μM；24h)降低下游癌基因的表达[1]。DC-BPi-11(0.6-50μM；24小时)剂量依赖性地降低c-Myc蛋白水平[1]。DC-BPi-11是安全的,对正常细胞的影响最小[1]。Western印迹分析[1]细胞系：人白血病MV-4-11细胞浓度：0.6μM、1.8μM、5.6μM、16.6μM和50μM培养时间：24小时结果：c-Myc以剂量依赖性方式耗尽。细胞凋亡分析[1]细胞系：人白血病MV-4-11细胞浓度：5μM、10μM、20μM培养时间：24小时结果：通过阻滞G1期细胞周期诱导细胞凋亡。
• 参考文献:

  [1]. Lu T, et al. Discovery of High-Affinity Inhibitors of the BPTF Bromodomain. J Med Chem. 2021 Aug 26;64(16):12075-12088.

DC-BPi-11物理化学性质

• 分子式: C₂₀H₂₃N₅O₂S
• 分子量: 397.49

DC-BPi-11靶点实验

查看更多实验

实验名称：Induction of apoptosis in human MV4-11 cells at 5 to 20 uM after 24 hrs by Annexin V-... 来源：ChEMBL 靶标：MV4-11 External Id：CHEMBL4830000

实验名称：Induction of cell cycle arrest in human MV4-11 cells assessed as accumulation at S ph... 来源：ChEMBL 靶标：MV4-11 External Id：CHEMBL4829999

实验名称：Downregulation of c-Myc protein expression in human MV4-11 cells after 24 hrs by West... 来源：ChEMBL 靶标：N/A External Id：CHEMBL4829994

实验名称：Cytotoxicity against human MRC5 assessed as reduction in cell viability at 100 uM aft... 来源：ChEMBL 靶标：MRC5 External Id：CHEMBL4829993

实验名称：Cytotoxicity against HUVEC assessed as reduction in cell viability at 100 uM after 3 ... 来源：ChEMBL 靶标：HUVEC External Id：CHEMBL4829992

实验名称：Induction of cell cycle arrest in human MV4-11 cells assessed as accumulation at G1 p... 来源：ChEMBL 靶标：MV4-11 External Id：CHEMBL4829998

实验名称：Inhibition of BPTF in human MV4-11 cells assessed as reduction in CDK6 mRNA level inc... 来源：ChEMBL 靶标：Nucleosome-remodeling factor subunit BPTF External Id：CHEMBL4829997

实验名称：Inhibition of BPTF in human MV4-11 cells assessed as reduction in bcl2 mRNA level inc... 来源：ChEMBL 靶标：Nucleosome-remodeling factor subunit BPTF External Id：CHEMBL4829996

实验名称：Inhibition of BPTF in human MV4-11 cells assessed as reduction in c-Myc mRNA level in... 来源：ChEMBL 靶标：Nucleosome-remodeling factor subunit BPTF External Id：CHEMBL4829995

实验名称：Binding affinity to BRD2-BD2 (unknown origin) assessed as change in melting temperatu... 来源：ChEMBL 靶标：Bromodomain-containing protein 2 External Id：CHEMBL4829986

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