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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C13H10O2 |
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分子量 | 198.22 | CAS No. | 5690-03-9 | |
Solubility (25°C)* | 体外 | DMSO | 39 mg/mL (196.75 mM) | |
Ethanol | 39 mg/mL (196.75 mM) | |||
Water | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | Splitomicin is a selective NAD(+)-dependent histone deacetylase Sir2p inhibitor with IC50 of 60 μM, showing a higher activity in a cell-based assay. |
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in vitro | Splitomicin inhibits Sir2p deacetylase activity by altering or blocking access to the acetylated histone binding pocket. [1] 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. [2] |
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. [3] |
キナーゼアッセイ | HDA Assay | |
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Histone H4 is acetylated chemically by using the HDAC assay kit. The whole-cell extract is prepared from an hst2Δ strain containing 2 μg plasmid with galactose-inducible wild-type SIR2 (pAR14), mutant SIR2 (GAL-SIR2-Y298N or GAL-SIR2-H286Q), or empty vector. For histone deacetylase assays, 50 μg of yeast whole-cell protein extract is incubated with [3H]-acetylated histone H4 peptide (40,000 cpm) with or without 500 μM NAD+ in a 100-μL reaction. The buffer contained 150 mM NaCl, 25 mM sodium phosphate, pH 7.4, and 1 mM DTT. Reactions are incubated at 30 °C for 16 h and stopped by the addition of 25 μL of 1 N HCl and 0.15 N acetic acid. Released [3H]-acetate is extracted with 400 μL of ethyl acetate. | ||
動物実験 | 動物モデル | Carotid artery thrombosis mouse model |
投薬量 | 80 mg/kg/d | |
投与方法 | i.p. |
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長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。