Uses
Splitomicin is a selective and potent inhibitor of Sir2 (silent information regulator 2), producing an inhibitory effect on neutrophils. Acts as an anti-inflammatory agent.
Definition
ChEBI: A benzochromenone that is 2,3-dihydro-1H-benzo[f]chromene substituted by an oxo group at position 3. It has been found to exhibit potential inhibitory activity against Sir2 proteins.
Synthesis Reference(s)
Journal of the American Chemical Society, 69, p. 2341, 1947
DOI: 10.1021/ja01202a027
General Description
A cell-permeable and selective inhibitor of NAD
+-dependent deacetylase activity of Sir2 protein (IC
50 = 60 μM). Creates a phenocopy of the
sir2 deletion mutant in
S. cerevisiae and sensitizes mammalian cells to a variety of DNA-damaging agents by abrogating Sir2p activity on p53. Reported to act by either altering or blocking access to the acetylated histone-binding pocket.
Biological Activity
Inhibitor of Sir2p (IC 50 = 60 μ M), an NAD + -dependent Sir2 family deacetylase required for chromatin-dependent silencing in yeast.
Biochem/physiol Actions
Cell permeable: yes
