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    Splitomicin (Splitomycin)
    Splitomicin (Splitomycin)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0437
    CAS #: 5690-03-9Purity ≥98%

    Description: Splitomicin (known also as Splitomycin), a lactone derived from naphthol, is a potent, cell-permeable and selective inhibitor of NAD(+)-dependent histone deacetylase (HDAC) Sir2p with potential antineoplastic activity. It inhibits Sir2p with an IC50 of 60 μM. Splitomicin was discovered for yeast sirtuins but showed rather weak inhibition on human enzymes.

    References: Proc Natl Acad Sci U S A. 2001 Dec 18;98(26):15113-8; J Biol Chem. 2014 Sep 12;289(37):25890-906. 

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    Molecular Weight (MW)198.22
    FormulaC13H10O2
    CAS No.5690-03-9
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 39 mg/mL (196.0 mM)   
    Water: <1 mg/mL
    Ethanol: 39 mg/mL (196.0 mM)   
    Other info

    Chemical Name: 1H-benzo[f]chromen-3(2H)-one

    InChi Key: ISFPDBUKMJDAJH-UHFFFAOYSA-N

    InChi Code: 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

    SMILES Code: O=C1CCC2=C3C=CC=CC3=CC=C2O1

    SynonymsSplitomicin; Splitomycin



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    In Vitro

    In vitro activity: Splitomicin inhibits Sir2p deacetylase activity by altering or blocking access to the acetylated histone binding pocket. Splitomicin inhibits platelet aggregation induced by thrombin, collagen, AA and U46619 via inhibition of cyclic AMP phosphodiesterase activity and subsequent inhibition of intracellular Ca(++) mobilization, TXB2 formation and ATP release.


    Kinase Assay: Splitomicin (Splitomycin) is a selective Sir2p inhibitor. Splitomicin inhibits NAD+-dependent HDAC activity of Sir2 protein. Splitomicin induces dose-dependent inhibition of HDAC in the yeast extract with an IC50 of 60 μM


    Cell Assay: Splitomicin (10-333 μM; 24 hours) elicits antiproliferative effects in MCF-7 and H1299 cells in a dose-dependent manner in colony formation assay. Splitomicin (33 μM) fails to decrease the number of colonies, but Splitomicin (100 and 333 μM) effectively inhibits colony formation in MCF-7 and H1299 cells

    In VivoIn a photochemical injury mouse model, splitomicin (80 mg/kg/d i.p.) enhances tissue factor activity in the arterial vessel wall and promotes carotid artery thrombus formation.
    Animal modelCarotid artery thrombosis mouse model
    Formulation & DosageFormulated in 0.5% methylcellulose; 80 mg/kg; i.p. injection
    References

    Proc Natl Acad Sci U S A. 2001 Dec 18;98(26):15113-8; Thromb Res. 2009 Jun;124(2):199-207; J Biol Chem. 2014 Sep 12;289(37):25890-906. 


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Splitomicin
    Inhibition of NAD-dependent HDA of Sir2p by splitomicin. The effect of splitomicin on NAD+-dependent HDA in wild-type and drug-resistant Sir2p mutants is shown. Proc Natl Acad Sci U S A. 2001 Dec 18; 98(26): 15113–15118.



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