Salermide

Salermide is a potent inhibitor of Sirt1/2 (Sirtuin 1/2) with a strong cancer-specific proapoptotic effect mediated by Sirt1. Class III histone deacetylases that are dependent on NAD+ (nicotinamide adenine dinucleotide-positive) include Sirt1 and Sirt2, which are involved in lifespan regulation. Since cancer is an age-related illness, focusing on sirtuins is becoming more and more popular as an antitumor tactic. Salermide is a reverse amide that significantly inhibits Sirt1 and Sirt2 in vitro. Salermide caused tumor-specific cell death in a variety of human cancer cell lines and was well tolerated by mice at concentrations up to 100 muM. Salermide's antitumor activity was mostly brought on by a significant induction of apoptosis. This suggested an in vivo mechanism of action via Sirt1 and was independent of global tubulin and K16H4 acetylation, ruling out a potential Sirt2-mediated apoptotic pathway. This is supported by the fact that cancer cells underwent apoptosis when Sirt1 but not Sirt2 was knocked down via RNA interference. Genetic p53 knockdowns demonstrated that Salermide's Sirt1-dependent proapoptotic effect is p53-independent, despite reports that p53 is a target of Sirt1. When combined, these findings point to the potential of salermide as an anticancer medication and provide light on the molecular pathway by which Sirt1 contributes to human carcinogenesis.

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.