Description
Salermide is an inhibitor of sirtuins that exhibits anti-parasitic and anticancer chemotherapeutic activities. In Schistosoma mansoni, salermide decreases egg-laying activity, disrupts morphology of reproductive organs, and induces apoptosis and cell death. In breast cancer cells, salermide downregulates expression of sirtuin1, causing increases in p53 acetylation and cell death; additionally, salermide upregulates expression of DR5, ATF3, ATF4, and CHOP. Salermide also induces apoptosis in non-small cell lung cancer (NSCLC) cells) and inhibits tumor growth across a variety of animal models.
References
Lancelot J, Caby S, Dubois-Abdesselem F, et al. Schistosoma mansoni Sirtuins: characterization and potential as chemotherapeutic targets. PLoS Negl Trop Dis. 2013 Sep 12;7(9):e2428. PMID: 24069483.
Dastjerdi MN, Salahshoor MR, Mardani M, et al. The apoptotic effects of sirtuin1 inhibitor on the MCF-7 and MRC-5 cell lines. Res Pharm Sci. 2013 Apr;8(2):79-89. PMID: 24019817.
Liu G, Su L, Hao X, et al. Salermide up-regulates death receptor 5 expression through the ATF4-ATF3-CHOP axis and leads to apoptosis in human cancer cells. J Cell Mol Med. 2012 Jul;16(7):1618-28. PMID: 21801305.
Lara E, Mai A, Calvanese V, Altucci L, et al. Salermide, a Sirtuin inhibitor with a strong cancer-specific proapoptotic effect. Oncogene. 2009 Feb 12;28(6):781-91. Erratum in: Oncogene. 2009 Feb 26;28(8):1168. Inhof, A [corrected to Imhof, A]. PMID: 19060927.
ABOUT LKT LABS
LKT Laboratories is a biochemical supply company focused on the synthesis, purification, and isolation of small molecules for research applications. Its range of products exhibit known biological activities that have found uses in a wide array of research fields, especially cancer and neuroscience. These products include protein kinase inhibitors, ion channel modulators, and activators. LKT serves the global research community by supplying the highest purity products for use in cell culture models, animal studies, or as reference materials or analytical standards.
