dacinostat

Dacinostat is a novel small molecule hydroxamate histone deacetylase inhibitor (HDAC inhibitor) developed as an experimental anticancer agent. It inhibits the enzymatic activity of histone deacetylases, particularly HDAC1, leading to increased acetylation of histones and transcriptional activation of genes such as p21. Dacinostat also induces acetylation of HSP90 and degradation of its client oncoproteins. In preclinical studies and early-phase clinical trials, it demonstrated antitumor effects by causing cell cycle arrest at G2/M phase and inducing apoptosis selectively in cancer cells. Dacinostat was initially developed by Novartis for the treatment of solid tumors but further development was discontinued after phase II trials[1][2][6][7].

Other names

404951-53-7(E)-N-hydroxy-3-[4-[[2-hydroxyethyl-[2-(1H-indol-3-yl)ethyl]amino]methyl]phenyl]prop-2-enamide