6-クロロ-2,3,4,9-テトラヒドロ-1H-カルバゾール-1-カルボキサミド

使用A selective inhibitor of SIRT1 over SIRT2 and SIRT3

一般的な説明A cell-permeable indole compound that acts as a potent and highly selective inhibitor of SIRT1 (IC50 = 98 nM). It inhibits other sirtuin family deacetylases only at much higher concentrations (IC50 = 19.6 and 48.7 μM for SIRT2 and SIRT3, respectively) and shows no inhibitory effect against class I and II HDACs or NAD glycohydrolase even at concentrations as high as 100 μM. Shown to be orally bioavailable with a serum half-life of 136 minutes in mice in vivo.