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Sirtinol是一种sirtuin(SIRT)抑制剂,对ySir2、hSIRT2和hSIRT2的IC50值分别为48 μM、57.7 μM和131 μM。
Suramin sodium salt (Suramin hexasodium salt) 是一种可逆的、竞争性的蛋白酪氨酸磷酸酶(PTPases)抑制剂。它是一种有效的sirtuins抑制剂:SirT1(IC50=297 nM)、SirT2(IC50=1.15 μM)和SirT5(IC50=22 μM),并且还作为一种逆转录酶的竞争性抑制剂(DNA拓扑异构酶II:IC50=5 μM)。苏拉明钠盐是一种有效的SARS-CoV-2 RNA依赖的RNA聚合酶(RdRp)抑制剂,并有效抑制IP5K。此外,它具有抗寄生虫、抗肿瘤和抗血管生成特性。
3-TYP是SIRT3的抑制剂(IC50: ~377 μM),也抑制蛋氨酸腺苷化转移酶(MAT)2和色氨酸2,3-二氧化酶(IDO)。它可能在NAD依赖的酶,包括脱氢酶上有许多非靶向作用。
Quercetin Dihydrate是一种天然黄酮类化合物,可刺激重组SIRT1并抑制PI3K,其对PI3K γ、PI3K δ和PI3K β的IC50值分别为2.4 μM、3.0 μM和5.4 μM。
EX-527 is a potent and selective SIRT1 inhibitor with IC50 of 38 nM, exhibits > 200-fold selectivity against SIRT2 and SIRT3.
OSS_128167 is a potent selective sirtuin 6 (SIRT6) inhibitor with IC50s of 89 μM, 1578 μM and 751 μM for SIRT6, SIRT1 and SIRT2, respectively. OSS_128167 has anti-HBV activity that inhibits HBV transcription and replication. OSS_128167 has anti-cancer, anti-inflammation and anti-viral effects.
Tenovin-6 is the water soluble analog of Tenovin-1 and acts as a potent SIRT1 (IC50=21 μM) and SIRT2 (IC50= 10 μM) inhibitor as well as p53 activator.
Resveratrol is one of the numerous polyphenolic compounds found in several vegetal sources, has a wide spectrum of targets with IC50 of 0.8, 1, 3.3 and 5 μM for Adenylyl cyclase, IKKβ, DNA polymerase α and δ, respectively.
Inauhzin is a small molecule that effectively reactivates p53 by inhibiting SIRT1 activity, and promotes p53-dependent apoptosis of human cancer cells without causing apparently genotoxic stress (IC50=3 μM, in A549 cell).
Salermide, a reverse amide, can act as an inhibitor of sirt, especially of sirt2, with the property of inducing apoptosis of tumor cells.
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Tags: SIRT1 | Sirtuin | SIRT1 相关产品 | SIRT1 基因表达
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