Splitomicin 5690-03-9

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Molecular Weight:

198.22 Splitomicin is a selective NAD(+)-dependent histone deacetylase Sir2p inhibitor with IC50 of 60 μM, showing a higher activity in a cell-based assay.


Biological Activity


Splitomicin inhibits Sir2p deacetylase activity by altering or blocking access to the acetylated histone binding pocket. Splitomicin inhibits platelet aggregation induced by thrombin,
collagen, AA and U46619 via inhibition of cyclic AMP phosphodiesterase
activity and subsequent inhibition of intracellular Ca(++) mobilization,
TXB2 formation and ATP release.


In a photochemical injury mouse model, splitomicin (80 mg/kg/d i.p.)
enhances tissue factor activity in the arterial vessel wall and promotes
carotid artery thrombus formation.


HDA Assay


Histone H4 is acetylated chemically by using the HDAC assay kit. The
whole-cell extract is prepared from an hst2Δ strain containing 2 μ
plasmid with galactose-inducible wild-type SIR2 (pAR14), mutant SIR2
(GAL-SIR2-Y298N or GAL-SIR2-H286Q), or empty vector. For histone
deacetylase assays, 50 μg of yeast whole-cell protein extract is
incubated with [3H]-acetylated histone H4 peptide (40,000
cpm) with or without 500 μM NAD+ in a 100-μL reaction.


The buffer
contained 150 mM NaCl, 25 mM sodium phosphate, pH 7.4, and 1 mM DTT.
Reactions are incubated at 30 °C for 16 h and stopped by the addition of
25 μL of 1 N HCl and 0.15 N acetic acid. Released [3H]-acetate is extracted with 400 μL of ethyl acetate.

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