Splitomicin, 5 mg

STEMCELL Technologies supplies this small molecule as a cell-permeable, selective inhibitor of Sir2p NAD+-dependent histone deacetylase (HDAC) activity. Sir2p negatively regulates gene expression and initiation of DNA replication. The compound induces dose-dependent inhibition of Sir2p HDAC activity in vitro (IC50 = 60 µM) and in vivo (minimal inhibitory concentration = 0.49 µM) in yeast extract, and its hydrolytically unstable lactone ring is critically important for activity.

Chemically named 1,2-dihydro-3H-naphtho[2,1-b]pyran-3-one, the molecule has the formula C₁₃H₁₀O₂, a molecular weight of 198.2 g/mol, and a purity of ≥ 98% (CAS Number: 5690-03-9). It is supplied as a crystalline solid.

Storage guidance: stable at -20°C as supplied; protect from prolonged exposure to light; for long-term storage store with a desiccant; stable as supplied for 12 months from date of receipt. Solubility: ≤ 75 mM in DMSO, ≤ 75 mM in absolute ethanol; low solubility in aqueous media. For cell culture use, dilute the stock solution into culture medium immediately before use, and avoid final DMSO concentration above 0.1% due to potential cell toxicity. Published applications include inhibition of platelet aggregation induced by thrombin, collagen, arachidonic acid, and U46619 (immunology); reactivation of FMR1 expression in neurons from Fragile X patients in vitro (disease modeling); and sensitization of cancer cells to DNA-damaging agents by abrogating Sir2p downregulation of p53 expression (cancer research). For research use only.