The sirtuins (SIRTs) are a family of NAD+-dependent histone deacetylases involved in gene regulation that is relevant to longevity, cancer, gene regulation, energy homeostasis, and apoptosis. JGB1741 is a small molecule inhibitor of SIRT1 with an IC50 value of 15 μM in a cell-free assay. It shows relatively weak inhibition for SIRT2 and SIRT3 with IC50 values greater than 100 μM. JGB1741 inhibits metastatic breast cancer MDA-MB 231 cell proliferation with an IC50 value of 512 nM in a cell-based assay and dose-dependently increases p53 acetylation and p53-mediated apoptosis in these cells.
