SRT 2183 is a selective Sirtuin-1 (SIRT1) activator with an EC1.5 value of 0.36 μM. SRT 2183 induces growth arrest and apoptosis, concomitant with deacetylation of STAT3 and NF-κB, and reduction of c-Myc protein levels[2].IC50 & Target: EC1.5: 0.36 μM (SIRT1)In Vitro: SRT 2183 (1-10 μM; 24-72 hours) inhibits the growth of Reh and Nalm-6 cells in a time- and dose-dependent manner[2].
SRT 2183 (5-10 μM in Reh cells; 10 μM in Ly3 cells; 24 hours) induces expression of DNA-damage response genes associated with accumulation of phospho-H2A.X levels[2].
SRT2183 inhibits RANKL-induced osteoclast differentiation, fusion and resorptive capacity without affecting osteoclast survival.