product name Splitomicin
Description: Splitomicin is a cell-permeable lactone derived from naphthol and a selective NAD(+)-dependent histone deacetylase Sir2p inhibitor with IC50 of 60 μM. Splitomicin inhibits the NAD+-dependent deacetylase activity of Sir2 in vitro. It increases the levels of cyclic AMP by inhibiting the activity of cyclic AMP phosphodiesterase.
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.
198.22
Formula
C13H10O2
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)
Solubility (In vivo)
Synonyms
other peoduct :
| 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: Cell Assay: |
|---|---|
| In Vivo | In 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 model | Carotid artery thrombosis mouse model |
| Formulation & Dosage | Formulated 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. |
