Largazole ((+)-Largazole) is an orally active, blood-brain barrier-permeable class I histone deacetylase ( HDAC ) inhibitor with in vivo anticancer activity and osteogenic efficacy. As a prodrug, Largazole hydrolyzes to Largazole thiol ( HY-170890 ), which has a K i value of 0.07 nM against human HDAC2 . Largazole regulates the cell cycle, induces apoptosis , upregulates tumor suppressors and osteoblast differentiation markers, inhibits osteoclast formation, and upregulates neuroprotection-related genes. Largazole can be used in the research of various cancers including colorectal cancer , as well as neurodegenerative diseases.
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