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MedKoo Biosciences/Splitomicin/406571/100mg
Splitomicin is a cell-permeable lactone derived from naphthol and known to be a potent selective inhibitor of Sir2 (silent information regulator 2) and HDAC. 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, interferes with mobilization of intracellular Ca+2 and ATP release.

MedKoo Cat#: 406571 Name: Splitomicin CAS#: 5690-03-9 Chemical Formula: C13H10O2 Exact Mass: 198.06808 Molecular Weight: 198.22 Elemental Analysis: C, 78.77; H, 5.09; O, 16.14

Synonym: Splitomicin

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

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

Technical Data

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code: 293490

Additional Information

        

References

1: Liu FC, Day YJ, Liou JT, Yu HP, Liao HR. Splitomicin inhibits fMLP-induced superoxide anion production in human neutrophils by activate cAMP/PKA signaling inhibition of ERK pathway. Eur J Pharmacol. 2012 Aug 5;688(1-3):68-75. doi: 10.1016/j.ejphar.2012.05.006. Epub 2012 May 23. PubMed PMID: 22634165.

2: Freitag M, Schemies J, Larsen T, El Gaghlab K, Schulz F, Rumpf T, Jung M, Link A. Synthesis and biological activity of splitomicin analogs targeted at human NAD(+)-dependent histone deacetylases (sirtuins). Bioorg Med Chem. 2011 Jun 15;19(12):3669-77. doi: 10.1016/j.bmc.2011.01.026. Epub 2011 Jan 22. PubMed PMID: 21315612.

3: Liu FC, Liao CH, Chang YW, Liou JT, Day YJ. Splitomicin suppresses human platelet aggregation via inhibition of cyclic AMP phosphodiesterase and intracellular Ca++ release. Thromb Res. 2009 Jun;124(2):199-207. doi: 10.1016/j.thromres.2009.02.013. Epub 2009 Mar 26. PubMed PMID: 19327818.

4: Neugebauer RC, Uchiechowska U, Meier R, Hruby H, Valkov V, Verdin E, Sippl W, Jung M. Structure-activity studies on splitomicin derivatives as sirtuin inhibitors and computational prediction of binding mode. J Med Chem. 2008 Mar 13;51(5):1203-13. doi: 10.1021/jm700972e. Epub 2008 Feb 13. PubMed PMID: 18269226.

5: Posakony J, Hirao M, Stevens S, Simon JA, Bedalov A. Inhibitors of Sir2: evaluation of splitomicin analogues. J Med Chem. 2004 May 6;47(10):2635-44. PubMed PMID: 15115404.