Splitomicin
Epigenetic modifier; Inhibitor of Sir2p
Splitomicin
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Splitomicin is a cell-permeable, selective inhibitor of Sir2p NAD+-dependent histone deacetylase (HDAC) activity. Sir2p negatively regulates gene expression and initiation of DNA replication. Splitomicin induces dose-dependent inhibition of the HDAC activity of Sir2p in vitro (IC₅₀ = 60 μM) and in vivo (minimal inhibitory concentration = 0.49 µM) in yeast extract (Bedalov et al.; Hirao et al.). It was shown that the hydrolytically unstable lactone ring of Splitomicin is critically important for its activity (Posakony et al.).
IMMUNOLOGY
- Inhibits platelet aggregation induced by thrombin, collagen, arachidonic acid, and U46619 (Liu et al.).
DISEASE MODELING
- Reactivates FMR1 expression in neurons of Fragile X patients in vitro (Biacsi et al.).
CANCER RESEARCH
- li>Sensitizes cancer cells to a variety of DNA-damaging agents by abrogating Sir2p downregulation of p53 expression (Botta et al.).
