Splitomicin (Splitomycin, 1,2-Dihydro-3H-naphthopyran-3-one, 1-Naphthalen propanoic acid)

Potent cell permeable and selective inhibitor of yeast NAD+-dependent histone deacetylase (HDAC) Sir2p. Displays higher activity in vivo than in vitro. 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. Shown to have diverse effects also in mammalian cells.\n\nStorage and Stability:\nShort-term Storage: +4 degrees C\nLong-term Storage: -20 degrees C\nStable for at least 2 years after receipt when stored at -20 degrees C.

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SPECIFICATIONS

Catalog Number

045308

Size

1mg

Purity

>98% (NMR)

References

Product Reference: \n?Identification of a small molecule inhibitor of Sir2p: A. Bedalov, et al.; PNAS 98, 15113 (2001)\n?Identification of selective inhibitors of NAD+-dependent deacetylases using phenotypic screens in yeast: M. Hirao, et al.; J. Biol. Chem. 278, 52773 (2003)\n?Inhibitors of Sir2: evaluation of splitomicin analogues: J. Posakony, et al.; J. Med. Chem. 47, 2635 (2004)\n?The Sir 2 family of protein deacetylases: J.M. Denu; Curr. Opin. Chem. Biol. 9, 431 (2005) (Review)\n?Histone deacetylase inhibitor-mediated radiosensitization of human cancer cells: class differences and the potential influence of p53: I.A. Kim, et al.; Clin. Cancer Res. 12, 940 (2006)\n?SIRT1 inhibition alleviates gene silencing in Fragile X mental retardation syndrome: R. Biacsi, et al.; PLoS Genet. 4, e1000017 (2008)\n?Splitomicin suppresses human platelet aggregation via inhibition of cyclic AMP phosphodiesterase and intracellular Ca++ release: F.C. Liu, et al.; Thromb. Res. 124, 199 (2009)\n?Reciprocal roles of SIRT1 and SKIP in the regulation of RAR activity: implication in the retinoic acid-induced neuronal differentiation of P19 cells: M.R. Kang, et al.; Nucleic Acids Res. 38, 822 (2010)\n?Sirt1 inhibition promotes in vivo arterial thrombosis and tissue factor expression in stimulated cells: A. Breitenstein, et al.; Cardiovasc. Res. 89, 464 (2011)\n?Sirtuin-1 targeting promotes Foxp3+ T-regulatory cell function and prolongs allograft survival: U.H. Beier, et al.; Mol. Cell Biol. 31, 1022 (2011)\n?

Alternative Names

Splitomycin, 1,2-Dihydro-3H-naphthopyran-3-one, 1-Naphthalen propanoic acid