Splitomicin was used to inhibit SIRT1 in human aortic endothelial cells and sirtuins in human breast cancer cells. Mouse leukaemic monocyte macrophage cell line was treated with Splitomicin prior to cholesterol efflux studies.

Sir2p (silent information regulator) and HDAC inhibitor.

Splitomicin, a derivative of β-naphthol is an inhibitor of Silent Information Regulator 2 (SIR2). It inhibits the NAD⁺-dependent deacetylase activity of Sir2 in vitro. It increases the levels of cyclic AMP by inhibiting the activity of cyclic AMP phosphodiesterase, interferes with mobilization of intracellular Ca⁺² and ATP release. This results in inhibition of platelet aggregation that is effective in cardiovascular and cerebrovascular diseases.

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