In vitro study | 1-20 μm SRT2183 can effectively inhibit cell growth and apoptosis. It causes increased mRNA levels of genes associated with pro-apoptosis, growth arrest, and DNA damage responses. SRT1720, SRT2183, SRT1460 and resveratrol have multiple off-target effects on some receptors, enzymes, transporters and ion channels. They are not direct activators of SIRT1. SRT2183 had no or little effect on SIRT1 deacetylation activity. SRT2183 activates AMPK, increases the expression of Sirt1, reduces the acetylation level of lysine at 310 of RelA/p65, plays a key role in the activation of NF-κB, the establishment of Sirt1 target, and plays a key role in bone marrow macrophages, inhibits RANKL-induced osteoclastogenesis and resorption capacity. |