sirtuin 2

AGK7 是 sirtuin 2 (SIRT2) 抑制剂。它在体外和帕金森病果蝇模型中均能抑制多巴胺能细胞的凋亡。在帕金森病细胞模型中，它改善了 α-突触核蛋白毒性和修饰的包涵体形态

Sirtuin modulator 2 (N-(3-(imidazo[2,1-b]thiazol-6-yl)phenyl)-2-methoxybenzamide) 具有抗糖尿病、抗炎和抗肿瘤活性。

Sirtuin-IN-2 (compound 20) 作为一种有效的 Sirtuin5 抑制剂，对白血病和乳腺癌中的关键靶点 Sirtuin5 发挥作用。

Resveratrol (SRT 501) 属于多酚类天然产物，是一种植物抗毒素，具有抗氧化和化学预防活性。Resveratrol 的靶点广泛，包括 COX、SIRT、LOC 等。Resveratrol 可以诱导细胞自噬和凋亡。

Sirt2-IN-1 是 sirtuin 2 的抑制剂 (IC50 = 163 nM)。

Dihydrocoumarin (melilotin) 是在草木犀中发现的一种天然产物。它是酵母 Sir2p 抑制剂，还抑制人 SIRT1和SIRT2，IC50分别为 208 和 295 μM。

JFD00244 is an inhibitor of sirtuin 2 (SIRT2). It has an anti-tumor effect.

Tenovin-6 是 Tenovin-1 的类似物，能抑制二氢乳清酸脱氢酶。它也抑制纯化人 SIRT1、SIRT2 和 SIRT3 蛋白脱乙酰酶活性，IC50分别为 21 μM、10 μM 和 67 μM。它是一种 p53转录活性的激活剂。

Inauhzin (INZ) 是一种新型小分子，通过抑制 SIRT1 活性有效地重新激活 p53，促进人 Y 细胞的 p53 依赖性凋亡，在 A549 细胞中的IC50为3 uM。

SRT 1720 是人 SIRT1 的选择性激活剂 ，EC1.5为 0.16 μM，对 SIRT2 和 SIRT3 的效力要低 230 倍以上。

Sirtinol 是一种 sirtuin 的抑制剂，对 ySir2，hSIRT2 和 hSIRT2 的IC50值分别为 48 μM，57.7 μM 和 131 μM。

B2 (Linazolamide intermediate B impurity 2) 促进亨廷顿病和帕金森病细胞模型中的包涵体形成。

AK-1是一种特异性有效和细胞可渗透的SIRT2抑制剂，其IC50值为 12.5 μM。它可防止阿尔茨海默病模型中的海马神经退行性变并诱导结肠癌细胞中的细胞周期停滞。

SIRT-IN-2 是一种 SIRT1 2 3 有效抑制剂，IC50 分别为 4、1和 7 μM。

SirReal1-O-propargyl is a selective and highly potent Sirtuin 2 (Sirt2) inhibitor, with an IC50 of 2.4 μM. SirReal1-O-propargyl, the SirReal1-based moiety, binds to the cereblon ligand via a linker to form PROTAC to degrade Sirt2[1].

Tenovin-1 抑制 SirT1 和 SirT2 的蛋白质去乙酰化活性，并防止 MDM2 介导的 p53 降解，这涉及泛素化。它具有癌症的研究潜力。

Alaproclate is a selective serotonin reuptake inhibitor (SSRI).1,2 It inhibits depletion of serotonin (5-HT) induced by 4-methyl-α-ethyl-m-tyramine in rat cerebral cortex, hippocampus, hypothalamus, and striatum (EC50s = 18, 4, 8, and 12 mg kg, respectively).1 Alaproclate inhibits NMDA-evoked currents and depolarization-induced voltage-dependent potassium currents in rat hippocampal neurons (IC50s = 1.1 and 6.9 μM, respectively) and does not inhibit GABA-evoked currents when used at concentrations up to 100 μM.2 It increases sirtuin 1 (SIRT1) levels in N2a murine neuroblastoma cells expressing apolipoprotein E4 (ApoE4; IC50 = 2.3 μM) and in the hippocampus in the FXFAD-ApoE4 transgenic mouse model of Alzheimer's disease when administered at a dose of 20 mg kg twice daily.3 Alaproclate (40 mg kg) decreases immobility time in the forced swim test in rats, indicating antidepressant-like activity.4References1. Michael, G.B., Eidam, C., Kadlec, K., et al. Increased MICs of gamithromycin and tildipirosin in the presence of the genes erm(42) and msr(E)-mph(E) for bovine Pasteurella multocida and Mannheimia haemolytica. Journal of Antimicrobial Chemotherapy 67(6), 1555-1557 (2012).2. Svensson, B.E., Werkman, T.R., and Rogawski, M.A. Alaproclate effects on voltage-dependent K+ channels and NMDA receptors: Studies in cultured rat hippocampal neurons and fibroblast cells transformed with Kv1.2 K+ channel cDNA. Neuropharmacology 33(6), 795-804 (1994).3. Campagna, J., Soilman, P., Jagodzinska, B., et al. A small molecule ApoE4-targeted therapeutic candidate that normalizes sirtuin 1 levels and improves cognition in an Alzheimer's disease mouse model. Sci. Rep. 8(1), 17574 (2018).4. Danysz, W.P., A., Kostowski, W., Malatynska, E., et al. Comparison of desipramine, amitriptyline, zimeldine and alaproclate in six animal models used to investigate antidepressant drugs. Pharmacol. Toxicol. 62(1), 42-50 (1988). Alaproclate is a selective serotonin reuptake inhibitor (SSRI).1,2 It inhibits depletion of serotonin (5-HT) induced by 4-methyl-α-ethyl-m-tyramine in rat cerebral cortex, hippocampus, hypothalamus, and striatum (EC50s = 18, 4, 8, and 12 mg kg, respectively).1 Alaproclate inhibits NMDA-evoked currents and depolarization-induced voltage-dependent potassium currents in rat hippocampal neurons (IC50s = 1.1 and 6.9 μM, respectively) and does not inhibit GABA-evoked currents when used at concentrations up to 100 μM.2 It increases sirtuin 1 (SIRT1) levels in N2a murine neuroblastoma cells expressing apolipoprotein E4 (ApoE4; IC50 = 2.3 μM) and in the hippocampus in the FXFAD-ApoE4 transgenic mouse model of Alzheimer's disease when administered at a dose of 20 mg kg twice daily.3 Alaproclate (40 mg kg) decreases immobility time in the forced swim test in rats, indicating antidepressant-like activity.4 References1. Michael, G.B., Eidam, C., Kadlec, K., et al. Increased MICs of gamithromycin and tildipirosin in the presence of the genes erm(42) and msr(E)-mph(E) for bovine Pasteurella multocida and Mannheimia haemolytica. Journal of Antimicrobial Chemotherapy 67(6), 1555-1557 (2012).2. Svensson, B.E., Werkman, T.R., and Rogawski, M.A. Alaproclate effects on voltage-dependent K+ channels and NMDA receptors: Studies in cultured rat hippocampal neurons and fibroblast cells transformed with Kv1.2 K+ channel cDNA. Neuropharmacology 33(6), 795-804 (1994).3. Campagna, J., Soilman, P., Jagodzinska, B., et al. A small molecule ApoE4-targeted therapeutic candidate that normalizes sirtuin 1 levels and improves cognition in an Alzheimer's disease mouse model. Sci. Rep. 8(1), 17574 (2018).4. Danysz, W.P., A., Kostowski, W., Malatynska, E., et al. Comparison of desipramine, amitriptyline, zimeldine and alaproclate in six animal models used to investigate antidepressant drugs. Pharmacol. Toxicol. 62(1), 42-50 (1988).

Cambinol (SIRT1 2 Inhibitor IV) 是一种SIRT1和SIRT2的抑制剂，IC50值分别为 56 μM 和 59 μM。它是中性鞘磷脂酶的外泌体抑制剂。

Benzamide, 3-methoxy-N-(3-thiazolo[5,4-b]pyridin-2-ylphenyl) (3-methoxy-N-(3-(thiazolo[5,4-b]pyridin-2-yl)phenyl)benzamide) 是一种 sirtuin 调节剂，可用于延长细胞寿命，治疗和 或预防多种 疾病和障碍包括糖尿病、心血管疾病、凝血障碍、炎症、癌症等。

WAY-270360 (N-[4-(1H-benzimidazol-2-yl)phenyl]-2,4-dimethoxybenzamide) 是一种 Sirtuin 调节剂和一种表皮生长因子受体 (EGFR) 抑制剂。

AGK2 是一种选择性SIRT2抑制剂，其IC50值为 3.5 μM。它抑制 SIRT1 和 SIRT3，IC50值分别为 30 和 91 μM。

SirReal2 是一种同型选择性 Sirt2有效抑制剂，IC50值为 140 nM。它导致 HeLa 细胞中的微管蛋白高乙酰化并诱导检查点蛋白 BubR1 的不稳定。

Nicotinamide Hydrochloride 是维生素 B3 或烟酸的一种形式，可抑制SIRT2的体外活性，其EC50值为 2 μM。 Nicotinamide Hydrochloride 可抑制 90% 的黑色素瘤细胞数量，并增加细胞内 NAD+、ATP、ROS 水平。Nicotinamide Hydrochloride 抑制黑色素瘤小鼠的肿瘤生长并提高生存率，可用于黑色素瘤等皮肤癌相关的研究。

SRT 1460 是一种有效的SIRT1激动剂，其EC1.5值为 2.9 μM。