AK-7 (420831-40-9) is a selective Sirt2 inhibitor (IC50=15.5 μM) which does not inhibit Sirt1 or Sirt3.1 It down regulates cholesterol biosynthesis genes in primary striatal neurons.1 AK-7 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 huntingtin.2
References/Citations:
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
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