Resminostat hydrochloride

  • 化学数据
CAS号 1187075-34-8 货号 BCP39644
中文名 Resminostat hydrochloride
英文名 Resminostat hydrochloride
中文别名
英文别名 Resminostat HCl;
分子式 C16H20ClN3O4S 分子量 385.86
  • 用途
生物活性 Resminostat is an inhibitor of histone deacetylase (HDAC) with IC50 values of 42.5nM, 50.1nM and 71.8nM, respectively against HDAC1, 3 and 6. As an inhibitor of HDACs, resminostat also inhibits HDAC8 with a weak activity (IC50=877nM). 5μM resminostat induces the acetylation of histone H4 in U266 myeloma cells. 10μM resminostat completely suppresses the cell growth in human myeloma cell lines, such as OPM-2, RPMI-8226 and U266. This inhibition is proved to be caused by the induction of apoptosis. In primary myeloma cells, resminostat also induces apoptosis of cells. Besides that, resminostat is proved to downregulate the expression of cell cycle proteins, including phosphorylated Rb, cdc25a, cyclin D1, Cdk4 and p53. In addition, resminostat is reported to be well tolerated, have no unexpected toxicities and do not cause clinically significant myelosuppression in the first-human study.
信号通路 Cell Cycle/DNA Damage Epigenetics 
靶 点 HDAC 

结构式

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