| CAS NO: | 5690-03-9 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 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) | |
| 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 |
| Synonyms | Splitomicin; Splitomycin |
| 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 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. |
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