Splitomicin

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.

A cell-permeable lactone derived from β-naphthol that acts as a selective inhibitor of NAD⁺-dependent histone deacetylase activity of Sir2 protein (IC₅₀ = 60 µM). It creates a conditional phenocopy of a sir2 deletion mutant in S. cerevisiae and 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.

Cell permeable: yes

Primary Target
NAD⁺-dependent histone deacetylase activity of Sir2 protein

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 60 µM against NAD+-dependent histone deacetylase activity of Sir2 protein

Packaged under inert gas

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Bedalov, A., et al. 2001. Proc. Natl. Acad. Sci. USA98, 15113.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Toxicity: Standard Handling (A)