Published TCIMAIL newest issue No.197
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SIRT1 and 2 Inhibitor
No.181(August 2019)
Cambinol (1) is a cell-permeable inhibitor of sirtuin (SIRT) 1 and 2.1) The IC50 values to NAD-dependent deacetylation of acetyl-histone H4 peptide are 56 µM and 59 µM for SIRT1 and SIRT2, respectively. The inhibition manners are competitive for the substrate peptide and non-competitive for NAD. 1 also is inhibits sphingomyelinase 2 with Ki value of 7 µM.2) The inhibition manner is uncompetitive.
＊1 is also known as NSC 112546.
References
- 1)Antitumor Activity of a Small-Molecule Inhibitor of Human Silent Information Regulator 2 Enzymes
- 2)Cambinol, a Novel Inhibitor of Neutral Sphingomyelinase 2 Shows Neuroprotective Properties
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