5690-03-9

Potent inhibitor of yeast NAD+-dependent histone deacetylase Sir2p (IC50=60μM). Sensitizes mammalian cells to a variety of DNA-damaging agents by abrogating Sir2p activity on p53. Acts by either altering or blocking access to the acetylated histone binding pocket.

ChEBI: A benzochromenone that is 2,3-dihydro-1H-benzo[f]chromene substituted by an oxo group at position 3. It has been found to exhibit potential inhibitory activity against Sir2 proteins.

Journal of the American Chemical Society, 69, p. 2341, 1947 DOI: 10.1021/ja01202a027

A cell-permeable and selective inhibitor of NAD⁺-dependent deacetylase activity of Sir2 protein (IC₅₀ = 60 μM). Creates a phenocopy of the sir2 deletion mutant in S. cerevisiae and sensitizes mammalian cells to a variety of DNA-damaging agents by abrogating Sir2p activity on p53. Reported to act by either altering or blocking access to the acetylated histone-binding pocket.

Inhibitor of Sir2p (IC 50 = 60 μ M), an NAD + -dependent Sir2 family deacetylase required for chromatin-dependent silencing in yeast.

Cell permeable: yes

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