HDAC8/BRPF1-IN-1

• 常用名: HDAC8/BRPF1-IN-1
• 英文名: HDAC8/BRPF1-IN-1
• CAS号: 2484255-85-6
• 分子量: 417.44
• 密度: N/A
• 沸点: N/A
• 分子式: C₁₉H₁₉N₃O₆S
• 熔点: N/A
• 闪点: N/A

HDAC8/BRPF1-IN-1用途

HDAC8/BRPF1-IN-1(化合物23a)是HDAC8和BRPF1的双重抑制剂,其对人类HDAC8的IC50为443nM,对人类BRPF1为67nM。HDAC8/BR PF1-IN-2在体外对HDAC1和6的活性较低[1]。

HDAC8/BRPF1-IN-1名称

• 英文名: HDAC8/BRPF1-IN-1

HDAC8/BRPF1-IN-1生物活性

• 描述: HDAC8/BRPF1-IN-1(化合物23a)是HDAC8和BRPF1的双重抑制剂,其对人类HDAC8的IC50为443nM,对人类BRPF1为67nM。HDAC8/BR PF1-IN-2在体外对HDAC1和6的活性较低[1]。
• 相关类别:
  研究领域 >> 癌症
  信号通路 >> 细胞周期/DNA损伤 >> HDAC
  信号通路 >> 表观遗传学 >> HDAC
  信号通路 >> 表观遗传学 >> 表观遗传读者域
• 靶点实验:

  hHDAC8:443 nM (IC50)

  hBRPF1:67 nM (Ki)

• 体外研究: HDAC8/BRPF1-IN-1(化合物23a)(4-100μM；24 h)对急性髓系白血病细胞具有抗增殖活性[1]。细胞增殖测定[1]细胞系：急性髓系白血病细胞THP-1和HL60浓度：4、20和100μM培养时间：24小时结果：抑制THP-1、HL60细胞生长。
• 参考文献:

  [1]. Ghazy E, et al. Design, synthesis, and biological evaluation of dual targeting inhibitors of histone deacetylase 6/8 and bromodomain BRPF1. Eur J Med Chem. 2020 Aug 15;200:112338.

HDAC8/BRPF1-IN-1物理化学性质

• 分子式: C₁₉H₁₉N₃O₆S
• 分子量: 417.44

HDAC8/BRPF1-IN-1靶点实验

查看更多实验

实验名称：Antiproliferative activity against human HL60 assessed as reduction in cell growth at... 来源：ChEMBL 靶标：HL-60 External Id：CHEMBL4770970

实验名称：Antiproliferative activity against human HL60 assessed as reduction in cell growth at... 来源：ChEMBL 靶标：HL-60 External Id：CHEMBL4770968

实验名称：Antiproliferative activity against human HL60 assessed as reduction in cell growth at... 来源：ChEMBL 靶标：HL-60 External Id：CHEMBL4770969

实验名称：Inhibition of human recombinant HDAC8 using H2N-Arg-His-Lys(Ac)-Lys(Ac)-AMC as substr... 来源：ChEMBL 靶标：Histone deacetylase 8 External Id：CHEMBL4770962

实验名称：Binding affinity to BRPF1 (unknown origin) by Isothermal titration calorimetry 来源：ChEMBL 靶标：Peregrin External Id：CHEMBL4770963

实验名称：Inhibition of recombinant human HDAC6 at 1 uM using Z-(Ac)Lys-AMC as substrate after ... 来源：ChEMBL 靶标：Histone deacetylase 6 External Id：CHEMBL4770960

实验名称：Inhibition of recombinant human HDAC6 at 10 uM using Z-(Ac)Lys-AMC as substrate after... 来源：ChEMBL 靶标：Histone deacetylase 6 External Id：CHEMBL4770961

实验名称：Antiproliferative activity against human THP-1 assessed as reduction in cell growth a... 来源：ChEMBL 靶标：THP-1 External Id：CHEMBL4770966

实验名称：Antiproliferative activity against human THP-1 assessed as reduction in cell growth a... 来源：ChEMBL 靶标：THP-1 External Id：CHEMBL4770967

实验名称：Cytotoxicity against against human HEK293 assessed as reduction in cell viability inc... 来源：ChEMBL 靶标：HEK293 External Id：CHEMBL4770964

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