RGFP966

  • 化学数据
CAS号 1396841-57-8 货号 BCP42941
中文名 RGFP966
英文名 RGFP966
中文别名
英文别名 RGFP-966;RGFP 966;
分子式 C21H19FN4O 分子量 362.4
  • 用途
生物活性 RGFP966 is an HDAC3 inhibitor with IC50 of 0.08 μM, exhibits > 200-fold selectivity over other HDAC. Systemic treatment with RGFP966 facilitates extinction in mice in a manner resistant to reinstatement. A single treatment of RGFP966 enhances extinction of a previously established cocaine-conditioned place preference, while simultaneously enhancing long-term object-location memory within subjects. HDAC3 inhibition using a first in class selective inhibitor, RGFP966, resulted in decreased cell growth in CTCL cell lines due to increased apoptosis that was associated with DNA damage and impaired S phase progression. Selective inhibition of HDAC3 could be useful in treatment of CTCL by disrupting DNA replication of the rapidly cycling tumor cells, ultimately leading to cell death.
信号通路 Cell Cycle/DNA Damage Epigenetics 
靶 点 HDAC 

结构式

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