{"id":1809,"date":"2026-10-13T16:12:57","date_gmt":"2026-10-13T08:42:57","guid":{"rendered":"http:\/\/bioactivecompoundlibrary.com\/?p=1809"},"modified":"2026-10-13T16:12:57","modified_gmt":"2026-10-13T08:42:57","slug":"abmole-mini-lecture-selisistat-ex527-a-core-tool-compound-for-exploring-sirt1-function","status":"publish","type":"post","link":"http:\/\/bioactivecompoundlibrary.com\/index.php\/2026\/10\/13\/abmole-mini-lecture-selisistat-ex527-a-core-tool-compound-for-exploring-sirt1-function\/","title":{"rendered":"AbMole Mini Lecture | Selisistat (EX527): A Core Tool Compound for Exploring SIRT1 Function"},"content":{"rendered":"\n

Selisistat<\/u><\/a> (EX527, AbMole, M1708) is a potent and highly selective inhibitor of SIRT1 (Sirtuin 1). Selisistat (CAS No.: 49843-98-3) binds to the complex of SIRT1 and nicotinamide adenine dinucleotide (NAD+), thereby blocking the deacetylase activity of SIRT1. In research, Selisistat serves as a key tool for investigating SIRT1 function. For example, in metabolic studies, Selisistat (EX527) was used to reveal that SIRT1 regulates PPAR\u03b1 protein stability, showing that SIRT1 inhibition prevents ubiquitin-mediated degradation of PPAR\u03b1[1]<\/sup>. In tumor models, Selisistat, alone or in combination with Paclitaxel<\/u><\/a>, inhibits tumor growth via mechanisms involving cell cycle regulation and metabolic reprogramming[2]<\/sup>. In neuroscience, Selisistat (EX527) influences microglial phenotype switching by inhibiting SIRT1, thereby altering the production of inflammatory cytokines and reactive oxygen species[3]<\/sup>. In virology, downregulating SIRT1 activity with Selisistat significantly inhibits hepatitis B virus replication[4]<\/sup>. Selisistat also affects various other cellular processes through SIRT1 inhibition. For instance, in inflammatory responses, Selisistat (EX527) reverses the SIRT1-activating effects of Resveratrol<\/u><\/a>, thereby attenuating its anti-inflammatory activity[5]<\/sup>. In oxidative stress models, Selisistat treatment reduces mitochondrial function and promotes apoptosis[6]<\/sup>. Selisistat has also been used to elucidate the role of SIRT1 in autophagy[7]<\/sup>. In skin hair follicle regeneration studies, Selisistat promotes hair regrowth by inhibiting the ferroptosis pathway [8]<\/sup>.<\/p>\n\n\n\n

Case Study<\/strong><\/strong><\/p>\n\n\n\n

Int J Biol Sci. 2022 Jan 31;18(4):1594-1611<\/strong><\/p>\n\n\n\n

In the above study, researchers from the Shanghai Institute of Materia Medica, Chinese Academy of Sciences, and Shanghai University of Traditional Chinese Medicine investigated the potential of Atractylenolide III<\/u><\/a> (ATL III), a bioactive compound derived from Atractylodes macrocephala, to inhibit non-alcoholic fatty liver disease (NAFLD) and its possible mechanisms. The study found that ATL III alleviated liver injury and lipid accumulation in high-fat diet (HFD)-induced NAFLD mouse models and free fatty acid (FFA)-treated HepG2 cells by activating the AdipoR1-mediated AMPK and SIRT1 signaling pathways. In this study, researchers used Dorsomorphin<\/u><\/a> (Compound C, AbMole, M2238) and EX 527<\/u><\/a> (Selisistat, AbMole, M1708) as inhibitors of the AMPK and SIRT1 pathways, respectively, confirming that both pathways are essential for the biological activity of Atractylenolide III. In cell experiments, the CCK-8 kit<\/u><\/a> (AbMole, M4839) was also used to verify the effect of Atractylenolide III on the viability of FFA-treated HepG2 cells [9]<\/sup>.<\/p>\n\n\n\n

\"\"<\/a><\/figure>\n\n\n\n

ATL III administration reduces FFAs-induced lipid accumulation in HepG2 cell<\/p>\n\n\n\n

References and Acknowledgments<\/strong><\/strong><\/p>\n\n\n\n

[1] J. H. Suh, K. H. Kim, M. E. Conner, et al., Hepatic PPARalpha Is Destabilized by SIRT1 Deacetylase in Undernourished Male Mice, Frontiers in nutrition 9 (2022) 831879.<\/p>\n\n\n\n

[2] A. Wawruszak, J. Luszczki, D. Bartuzi, et al., Selisistat, a SIRT1 inhibitor, enhances paclitaxel activity in luminal and triple-negative breast cancer: in silico, in vitro, and in vivo studies, Journal of enzyme inhibition and medicinal chemistry 40(1) (2025) 2458554.<\/p>\n\n\n\n

[3] J. Zhu, P. Jin, T. Zhou, et al., SIRT1 modulates microglia phenotypes via inhibiting drp1 phosphorylation reduces neuroinflammation in heatstroke, Brain research bulletin 218 (2024) 111101.<\/p>\n\n\n\n

[4] W. Zhang, J. Cui, L. Li, et al., Notoginsenoside R1 inhibits hepatitis B virus replication by modulating SIRT1 activity, Acta virologica 67(1) (2023) 51-58.<\/p>\n\n\n\n

[5] X. M. Chen, Y. J. Guo, H. W. Ling, et al., The Effect of Resveratrol in Sirt1\/CST Pathway to Inhibit TNF-alpha Induced Inflammatory Response in Rat Primary Fibroblast-Like Synoviocytes, Biological & pharmaceutical bulletin 46(11) (2023) 1592-1600.<\/p>\n\n\n\n

[6] Y. Wang, Q. Yang, S. Shen, et al., Mst1 promotes mitochondrial dysfunction and apoptosis in oxidative stress-induced rheumatoid arthritis synoviocytes, Aging 12(16) (2020) 16211-16223.<\/p>\n\n\n\n

[7] P. Cao, Y. Wang, C. Zhang, et al., Quercetin ameliorates nonalcoholic fatty liver disease (NAFLD) via the promotion of AMPK-mediated hepatic mitophagy, The Journal of nutritional biochemistry 120 (2023) 109414.<\/p>\n\n\n\n

[8] Z. Zeng, B. Wang, M. Ibrar, et al., Schizochytrium sp. Extracted Lipids Prevent Alopecia by Enhancing Antioxidation and Inhibiting Ferroptosis of Dermal Papilla Cells, Antioxidants (Basel, Switzerland) 12(7) (2023).<\/p>\n\n\n\n

[9] Q. Li, J. X. Tan, Y. He, et al., Atractylenolide III ameliorates Non-Alcoholic Fatty Liver Disease by activating Hepatic Adiponectin Receptor 1-Mediated AMPK Pathway, International journal of biological sciences 18(4) (2022) 1594-16<\/p>\n","protected":false},"excerpt":{"rendered":"

Selisistat (EX527, AbMole, M1708) is a potent and highly selective inhibitor of SIRT1 (Sirtuin 1). Selisistat (CAS No.: 49843-98-3) binds to the complex of SIRT1 and nicotinamide adenine dinucleotide (NAD+), thereby blocking the deacetylase activity of SIRT1. In research, Selisistat serves as a key tool for investigating SIRT1 function. For example, in metabolic studies, Selisistat (EX527) … <\/p>\n

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