Description
Chidamide is an inhibitor of histone deacetylases (HDACs; IC
50s = 0.095, 0.160, 0.067, 0.733, 0.078, and 0.432 μM for HDAC1-3, 8, 10, and 11, respectively). It is selective for these HDACs over HDAC4-7 and 9 (IC
50s = >30 μM for all). Chidamide also inhibits nicotinamide phosphoribosyltransferase (Nampt; IC
50 = 2.1 μM). It inhibits cell growth in a panel of 18 cancer cell lines (GI
50s = 0.4-40 μM) but has no effect on the growth of non-cancerous CCC-HEK human fetal kidney or CCC-HEL human liver cells (GI
50s = >100 μM).
In vivo, tucidinostat (12.5, 25, and 50 mg/kg) reduces tumor growth in HCT-8, A549, BEL-7402, and MCF-7 mouse xenograft models.
Uses
Chidamide is a newly designed histone deacetylase inhibitor that induces an antitumor effect in various cancer by increasing the acetylation levels of histone H3 and decrease histone deacetylase (HDAC) activity, induces apoptosis. Also, it is a potential utility of Chidamide for the treatment of Myelodysplastic syndromes.
