Sirtuin
Sirtuin (Sir2 proteins) are a class of proteins that possess either mono-ADP-ribosyltransferase, or deacylase activity, including deacetylase, desuccinylase, demalonylase, demyristoylase and depalmitoylase activity. Sirtuins regulate important biological pathways in bacteria, archaea and eukaryotes.
Sirtuins have been implicated in influencing a wide range of cellular processes like aging, transcription, apoptosis, inflammation and stress resistance, as well as energy efficiency and alertness during low-calorie situations. Sirtuins can also control circadian clocks and mitochondrial biogenesis.
The dependence of sirtuins on NAD links their enzymatic activity directly to the energy status of the cell via the cellular NAD:NADH ratio, the absolute levels of NAD, NADH or nicotinamide or a combination of these variables.
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Nicotinamide (NAM), an amide form of niacin (vitamin B3), is a water-soluble and noncompetitive inhibitor of the deacetylation reaction catalyzed by Sirtuins and it acts as constituent of the enzyme cofactors NAD and NADP. Nicotinamide (Vitamin B3) 是一种水溶性维生素，是NAD 和 NADP的活性成分，也是一种sirtuins抑制剂。
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EX 527 (Selisistat)是一种有效的，选择性的SIRT1抑制剂，IC50为38 nM，比作用于SIRT2和SIRT3选择性高200倍以上。
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ME0328 是一种高度选择性PARP抑制剂，IC50 为0.89 μM，其作用于PARP3的选择性比作用于PARP1的选择性约高七倍。
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Fisetin 是有效的Sirtuin活化化合物(STAC)，可以调节Sirtuin。Fisetin 抑制 p90RSK/YB-1 信号通道并且在A375黑素瘤细胞中下调药物抗性相关的 P-糖蛋白。
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Splitomicin是一种选择性的NAD(+)-dependent histone deacetylase Sir2p抑制剂，IC50为60 μM。在细胞中有着更高的活性。
More
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Nicotinamide (NAM), an amide form of niacin (vitamin B3), is a water-soluble and noncompetitive inhibitor of the deacetylation reaction catalyzed by Sirtuins and it acts as constituent of the enzyme cofactors NAD and NADP. Nicotinamide (Vitamin B3) 是一种水溶性维生素，是NAD 和 NADP的活性成分，也是一种sirtuins抑制剂。
More
-
EX 527 (Selisistat)是一种有效的，选择性的SIRT1抑制剂，IC50为38 nM，比作用于SIRT2和SIRT3选择性高200倍以上。
More
-
ME0328 是一种高度选择性PARP抑制剂，IC50 为0.89 μM，其作用于PARP3的选择性比作用于PARP1的选择性约高七倍。
More
-
Fisetin 是有效的Sirtuin活化化合物(STAC)，可以调节Sirtuin。Fisetin 抑制 p90RSK/YB-1 信号通道并且在A375黑素瘤细胞中下调药物抗性相关的 P-糖蛋白。
More
-
Splitomicin是一种选择性的NAD(+)-dependent histone deacetylase Sir2p抑制剂，IC50为60 μM。在细胞中有着更高的活性。
More
