HDAC6-IN-10

• 常用名: HDAC6-IN-10
• 英文名: HDAC6-IN-10
• CAS号: 2408286-73-5
• 分子量: 392.41
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₁H₂₀N₄O₄
• 熔点: N/A
• 闪点: N/A

HDAC6-IN-10用途

HDAC6-IN-10是一种高选择性HDAC6抑制剂,IC50为0.73 nM。HDAC6-IN-10的选择性是其他HDAC亚型的144～10941倍。HDAC6-IN-10对多发性骨髓瘤细胞具有抗增殖活性[1]。

HDAC6-IN-10名称

• 英文名: HDAC6-IN-10

HDAC6-IN-10生物活性

• 描述: HDAC6-IN-10是一种高选择性HDAC6抑制剂,IC50为0.73 nM。HDAC6-IN-10的选择性是其他HDAC亚型的144～10941倍。HDAC6-IN-10对多发性骨髓瘤细胞具有抗增殖活性[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
• 靶点实验:

  HDAC1:8020 nM (IC50)

  HDAC4:5620 nM (IC50)

  HDAC5:4370 nM (IC50)

  HDAC6:0.73 nM (IC50)

  HDAC7:752 nM (IC50)

  HDAC8:513 nM (IC50)

  HDAC9:2560 nM (IC50)

  HDAC10:105 nM (IC50)

  HDAC11:1800 nM (IC50)

• 体外研究: HDAC6-IN-10(化合物21b)(0.1-10μM；24小时)处理显示出对HDAC6的高度选择性抑制[1]。HDAC6-IN-10(化合物21b)(0-100μM；72小时)治疗显示对两种多发性骨髓瘤细胞RPMI-8226和U266具有抗增殖活性[1]。Western Blot分析[1]细胞系：HCT-116浓度：0.1、1和10μM培养时间：24小时结果：Ac微管蛋白水平呈剂量依赖性增加。细胞增殖试验[1]细胞系：RPMI-8226和U266细胞浓度：0-100μM孵育时间：72小时结果：对RPMI-82 26和U66具有抗增殖活性,IC50分别为33.183μM和43.233μM。
• 参考文献:

  [1]. Xin Chen, et al. Novel 2, 5-diketopiperazine derivatives as potent selective histone deacetylase 6 inhibitors: Rational design, synthesis and antiproliferative activity. Eur J Med Chem. 2020 Feb 1;187:111950.

HDAC6-IN-10物理化学性质

• 分子式: C₂₁H₂₀N₄O₄
• 分子量: 392.41

HDAC6-IN-10靶点实验

查看更多实验

实验名称：Inhibition of HDAC1/HDAC2/HDAC3 in human HCT-116 cells assessed as increase in Ac-H3 ... 来源：ChEMBL 靶标：Histone deacetylase 3 External Id：CHEMBL5230360

实验名称：Antiproliferative activity against human U-266 cells assessed as inhibition of cell g... 来源：ChEMBL 靶标：U-266 External Id：CHEMBL5230353

实验名称：Antiproliferative activity against human RPMI-8226 cells assessed as inhibition of ce... 来源：ChEMBL 靶标：RPMI-8226 External Id：CHEMBL5230352

实验名称：Cytotoxicity against human HS5 cells assessed as inhibition of cell growth incubated ... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5230354

实验名称：Selectivity index, ratio of IC50 for inhibition of HDAC4 (unknown origin) to IC50 for... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5230285

实验名称：Selectivity index, ratio of IC50 for inhibition of HDAC3 (unknown origin) to IC50 for... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5230284

实验名称：Selectivity index, ratio of IC50 for inhibition of HDAC7 (unknown origin) to IC50 for... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5230287

实验名称：Selectivity index, ratio of IC50 for inhibition of HDAC5 (unknown origin) to IC50 for... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5230286

实验名称：Selectivity index, ratio of IC50 for inhibition of HDAC2 (unknown origin) to IC50 for... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5230283

实验名称：Inhibition of HDAC8 (unknown origin) using Fluor de lys as substrate by fluorescence ... 来源：ChEMBL 靶标：Histone deacetylase 8 External Id：CHEMBL5230269

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