SIRT2 inhibitor / A selective Sirt2 inhibitor (IC50=15.5 µM) which does not inhibit Sirt1 or Sirt31. It down regulates cholesterol biosynthesis genes in primary striatal neurons1. Displays neuroprotective effects in Huntington’s disease mouse models including improved motor function, extended survival and reduced brain atrophy all of which were associated with reduced aggregated mutant huntingtin2.
Biochemicals & reagents
420831-40-9
1) Tylor et al. (2011), A brain-permeable small molecule that reduces neuronal cholesterol by inhibiting activity of sirtuin 2 deacetylase; ACS Chem. Biol., 6 540 2) Chopra et al. (2012), The sirtuin 2 inhibitor AK-7 is neuroprotective in Huntington’s disease mouse models; Cell Rep., 2 1492
RT
TARGET: Protein deacetylase -- PATHWAY: Chromatin; Cholesterol metabolism; Posttranslational modification -- RESEARCH AREA: Epigenetics; Neuroscience -- DISEASE AREA: Neurodegeneration; Ageing