STAC-103

STAC-103 is a small-molecule sirtuin-activating compound (STAC) that acts as an allosteric activator of SIRT1 (Sirtuin 1). Developed by Sirtris Pharmaceuticals (later acquired by GlaxoSmithKline), STAC-103 was part of a library of synthetic compounds designed to mimic the effects of resveratrol but with significantly higher potency and improved pharmacological properties. It binds to the N-terminal domain of SIRT1, lowering the Michaelis constant (Km) for acetylated substrates and increasing the enzyme's catalytic activity. Preclinical studies explored its potential in treating metabolic diseases, such as type 2 diabetes and obesity, by improving insulin sensitivity and mitochondrial function. However, like many early STACs from the Sirtris pipeline, its development was largely superseded by later-generation compounds like SRT2104, and it remains primarily a research tool.

Other names

STAC-103STAC103STAC 103SRT103SRT-103SRT 103