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.
Storage and Stability:
Short-term Storage: +4°C
Long-term Storage: -20°C
Stable for at least 2 years after receipt when stored at -20°C.
Purity: >98% (NMR)
Important Note: This product as supplied is intended for research use only, not for use in human, therapeutic or diagnostic applications without the expressed written authorization of United States Biological.
Product Reference: |
Identification of a small molecule inhibitor of Sir2p: A. Bedalov, et al.; PNAS 98, 15113 (2001)
Identification of selective inhibitors of NAD+-dependent deacetylases using phenotypic screens in yeast: M. Hirao, et al.; J. Biol. Chem. 278, 52773 (2003)
Inhibitors of Sir2: evaluation of splitomicin analogues: J. Posakony, et al.; J. Med. Chem. 47, 2635 (2004)
The Sir 2 family of protein deacetylases: J.M. Denu; Curr. Opin. Chem. Biol. 9, 431 (2005) (Review)
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)
SIRT1 inhibition alleviates gene silencing in Fragile X mental retardation syndrome: R. Biacsi, et al.; PLoS Genet. 4, e1000017 (2008)
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)
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)
Sirt1 inhibition promotes in vivo arterial thrombosis and tissue factor expression in stimulated cells: A. Breitenstein, et al.; Cardiovasc. Res. 89, 464 (2011)
Sirtuin-1 targeting promotes Foxp3+ T-regulatory cell function and prolongs allograft survival: U.H. Beier, et al.; Mol. Cell Biol. 31, 1022 (2011)
|Intended for research use only. Not for use in human, therapeutic, or diagnostic applications.|