SPLITOMICIN 1PC X 5MG

General description

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.

Biochem/physiol Actions

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

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Other Notes

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

Legal Information

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

Molecular Weight: 198.22. Empirical Formula: C₁₃H₁₀O₂. Quality Level: 100. Assay: ≥. 95% (HPLC). form: powder. manufacturer/tradename: Calbiochem^®. . storage condition: OK to freeze, protect from light. color: off-white. solubility: DMSO: 100 . mg/mL. shipped in: ambient. storage temp.: 2-8°C. InChI: 1S/C13H10O2/c14-13-8-6-11-10-4-2-1-3-9(10)5-7-12(11)15-13/h1-5,7H,6,8H2. InChI key: ISFPDBUKMJDAJH-UHFFFAOYSA-N. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.