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SIRT1 Inhibitor

SIRT1 is a member of the sirtuin family of enzymes that catalyze the deacetylation of acetyl-lysine residues in histones and other proteins.1) SIRT1 plays an important role in a variety of processes including stress resistance, metabolism, differentiation, and aging.1) Sirtuins are the mammalian orthologues of the yeast Sir2 (silent information regulator 2).1,2) In the catalytic process of SIRT1, NAD+ is cleaved and O-acetyl ADP-ribose is generated.1,3,4)
Ex-527 (1) is a small molecule inhibitor of SIRT1 and possesses much higher selectivity for SIRT1 than others as shown below (Table).5) 1 also does not inhibit class I/II HDACs at concentrations up to 100 μM.6)
* Class I/II HDACs are histone deacetylases and remove acetyl groups without hydrolysis of NAD+.

Table. Sirtuin inhibitory activity of Ex-5275)

Table. Sirtuin inhibitory activity of Ex-527

This product is for research purpose only.


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