JGB1741, also known as ILS-JGB-1741, is a potent, specific inhibitor of SIRT1 activity with an IC50 of 15 μM. JGB1741 is a weak inhibitor of both SIRT2 and SIRT3, with IC50s greater than 100 μM. JGB1741 enhances the level of acetylated p53, leading to p53-mediated apoptosis, and regulates Bax/Bcl2 ratio. JGB1741 increased the level of acetylated p53, led to p53-mediated apoptosis, and regulated Bax/Bcl2 ratio, cytochrome c release and PARP fragmentation. JGB1741 inhibited the proliferation of MDA-MB 231 cells at a concentration of less than 10 μM for 24 h. JGB1741 caused cell cycle arrest in G1 phase, increased the proportion of cells entering sub-G0/G1 phase, and induced apoptosis of MDA-MB 231 cells. At a concentration range of 0.01-1 μM for 24 hours of action, JGB1741 resulted in increased levels of global acetylation of H3K9, p53 expression and acetylated p53K382[1].
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