Initial drug development efforts focused on SIRT1 and SIRT2 have yielded a number of potent SIRT2 inhibitors and SIRT1 activators that have now been through the first clinical trials, with …

Sep 29, 2016 · Sirtuin 1 (SIRT1) is known to suppress differentiation of pluripotent/multipotent cells and neural progenitor cells into neurons by blocking activation of transcription factors …

To understand better the effects of cellular administration of NAM, we reviewed published literature in which treatment with NAM was used to inhibit SIRT1 and found that the expected …

Most of the sirtuin inhibitors characterized so far only inhibit SIRT1 and/or SIRT2, but also some of them inhibit SIRT3 and SIRT5 with a lower affinity. This review outlines biological …

The investigation of SIRT1 inhibitors provides insights into the complex regulatory networks within cells and offers a deeper understanding of the role of SIRT1 in maintaining cellular homeostasis.

Several synthetic inhibitors and activators of SIRT1 have been developed, and some therapeutic applications have been explored. The indole EX-527 and its derivatives are among the most …

Jul 24, 2023 · Compounds that inhibit either SIRT1 or SIRT2 show promising antitumor effects in several types of cancer models, both in vitro and in vivo. The simultaneous inhibition of SIRT1 …

Inauhzin is a cell-permeable SIRT1 inhibitor with an IC50 of 0.7-2 μM and reactivates p53 by inhibiting SIRT1 deacetylation activity. Scopolin, a coumarin isolated from Arabidopsis thaliana …

Sep 17, 2024 · E × 527 (Selisistat) is a specific inhibitor of SIRT1 activity with safe and well tolerance in clinical trials. Here, we show that E × 527 could strengthen significantly activation …

Apr 6, 2020 · MHY2245 significantly inhibited SIRT1 enzyme activity, reduced the expression of SIRT1, increased cell cycle arrest at G 2 /M phase, and induced apoptotic cell death in SKOV3 …