CAS:410536-97-9
Storage:Powder:-20℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year
Purity:≥98%
Appearance:Light yellow to yellow Solid
Sirtinol是一种特异性SIRT1和SIRT2抑制剂
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SirtinolCAS:410536-97-9
Storage:Powder:-20℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year
Purity:≥98%
Appearance:Light yellow to yellow Solid
CAS | 410536-97-9 |
Chinese Name | 去乙酰化酶 |
English Name | Sirtinol |
Synonyms | 2-[[(2-羟基-1-萘基)亚甲基]氨基]-N-(1-苯基乙基0苯甲酰胺 |
Molecular Formula | C26H22N2O2 |
Molecular Weight | 394.47 |
Solubility | Soluble in DMSO |
Purity | ≥98% |
Appearance | Light yellow to yellow Solid |
Storage | Powder:-20℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year |
MDL | MFCD00810186 |
SMILES | O=C(NC(C1=CC=CC=C1)C)C2=CC=CC=C2/N=C/C3=C4C=CC=CC4=CC=C3O |
Target Point | SIRT1,2 |
Passage | Cell Cycle;DNA Damage/DNA Repair; Epigenetics |
Background | Sirtinol is a specific SIRT1 and SIRT2 inhibitor |
Biological Activity | Sirtinol 是 sirtuin 的抑制剂,对 ySir2,hSIRT2 和 hSIRT2 的 IC50 值分别为 48 μM,57.7 μM 和 131 μM。[1-4] |
IC50 | ySir2:48μM;hSIRT2:57.7μM;hSIRT1:131μM [1-4] |
In Vitro | Sirtinol减弱非小细胞肺癌(NSCLC)H1299细胞的增殖并诱导细胞凋亡,并导致FoxO3a水平显著增加,FoxO3a是Sirt1靶向的促凋亡转录因子[2]。Sirtinol以浓度和时间依赖性方式减少MCF-7细胞的生长。处理24和48小时后,sirtinol的IC50值分别为48.6μM和43.5μM。 Sirtinol显著降低SIRT1表达并增加乙酰化p53水平[1]。 |
In Vivo | Sirtinol通过直接抑制HNE活性具有抗炎作用,并减弱HNE诱导的和LPS介导的组织或器官损伤[3]。 |
Cell Experiment | 将Sirtinol以10mM的浓度溶解于100%DMSO中,并在-20℃下储存直至使用。通过台盼蓝染料排除测定法测定H1299细胞的细胞增殖。将人非小细胞肺癌(NSCLC)细胞接种在12孔板中,并分别用指定浓度的sirtinol(0,10,20和50μM)处理24小时和48小时。孵育后,用0.2%台盼蓝染色细胞,并用Countess [2]计数。 |
Animal Experiment | 小鼠:在该模型中使用30只雄性小鼠(20-25g,7-8周龄)。简而言之,将小鼠随机分成五组;然后给小鼠腹膜内注射50μLDMSO(载体组)或sirtinol(2.5或5.0mg/kg体重)。 1小时后,诱导爪炎症。在HNE或盐水注射之前和之后测量爪的厚度[3]。 |
Data Literature Source | [1]. Wang J,et al. Sirtinol,a class III HDAC inhibitor,induces apoptotic and autophagic cell death in MCF-7 human breast cancer cells. Int J Oncol. 2012 Sep;41(3):1101-1109. [2]. Fong Y,et al. The antiproliferative and apoptotic effects of sirtinol,a sirtuin inhibitor on human lung cancer cells by modulating Akt/β-catenin-Foxo3a axis. ScientificWorldJournal. 2014;2014:937051. [3]. Tsai YF,et al. Sirtinol inhibits neutrophil elastase activity and attenuates lipopolysaccharide-mediated acute lung injury in mice. Sci Rep. 2015 Feb 10;5:8347. [4]. Mai A,et al. Design,synthesis,and biological evaluation of sirtinol analogues as class III histone/protein deacetylase (Sirtuin) inhibitors. J Med Chem. 2005 Dec 1;48(24):7789-95. |
Unit | Bottle |
Specification | 5mg 10mg |
Sirtinol是一种特异性SIRT1和SIRT2抑制剂