产品简介:

    AGK2是一种选择性的SIRT2 抑制剂,IC50为3.5 µM。AGK2 抑制SIRT1 和SIRT3 的IC50 分别为30和91 µM [1,2]。

AGK2 (0.01-20 µM；24h)在体外抑制肥大细胞脱颗粒作用,AGK2 处理能够减少RBL-2H3 细胞中β-己糖苷酶和组胺高水平的表达[3]。AGK2 (1-5 µM；24h) 通过抑制HeLa 细胞中HSF1 蛋白的稳定性,抑制细胞的生长和迁移[4]。AGK2 对SIRT2 抑制可通过增强干细胞记忆(TSCM)反应,显著增强卡介苗(BCG)的主要感染和结核病复发的疗效[5]。

AGK2 (1 µmol/mice；i.p；26h) 能够抑制LPS 处理小鼠脑组织中BV2 微胶质细胞的活化和iNOS、SIRT2 的表达[6]。AGK2 (1µmol/mice；i.p；26h) 预处理可以降低ALF 肝脏组织中的促炎性细胞因子水平。AGK2 也能改善TAA 引起的生存率[7]。AGK2 (82 mg/kg；i.p；7days) 处理可以抑制HBV 转基因小鼠血清中的HBV DNA、HBeAg 和HBsAg 水平,以及肝脏中的HBV DNA、RNA 和HBc 的表达[8]。

产品性质:

Cas No.:304896-28-4

别名:2-氰基-3-[5-(2,5-二氯苯基)-2-呋喃基]-N-5-喹啉基-2-丙烯酰胺

化学名:(E)-2-cyano-3-(5-(2,5-dichlorophenyl)furan-2-yl)-N-(quinolin-5-yl)acrylamide

Canonical SMILES:ClC(C(C1=CC=C(/C=C(C#N)/C(NC2=C3C(N=CC=C3)=CC=C2)=O)O1)=C4)=CC=C4Cl

分子式:C23H13Cl2N3O2

分子量:434.27

溶解度:≥ 9.3mg/mL in DMSO

储存条件:Store at -20°C

注意事项:

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References:

[1]. Tatum PR, Sawada H, et,al. Identification of novel SIRT2-selective inhibitors using a click chemistry approach. Bioorg Med Chem Lett. 2014 Apr 15;24(8):1871-4. doi: 10.1016/j.bmcl.2014.03.026. Epub 2014 Mar 20. PMID: 24675380.

[2]. Outeiro TF, Kontopoulos E, et,al. Sirtuin 2 inhibitors rescue alpha-synuclein-mediated toxicity in models of Parkinson's disease. Science. 2007 Jul 27;317(5837):516-9. doi: 10.1126/science.1143780. Epub 2007 Jun 21. PMID: 17588900.

[3]. Kim YY, Hur G, et,al. AGK2 ameliorates mast cell-mediated allergic airway inflammation and fibrosis by inhibiting FcεRI/TGF-β signaling pathway. Pharmacol Res. 2020 Sep;159:105027. doi: 10.1016/j.phrs.2020.105027. Epub 2020 Jun 18. PMID: 32565308.

[4]. Kim HW, Kim SA, et,al. Sirtuin inhibitors, EX527 and AGK2, suppress cell migration by inhibiting HSF1 protein stability. Oncol Rep. 2016 Jan;35(1):235-42. doi: 10.3892/or.2015.4381. Epub 2015 Nov 2. PMID: 26530275.

[5]. Bhaskar A, Pahuja I, et,al. SIRT2 inhibition by AGK2 enhances mycobacteria-specific stem cell memory responses by modulating beta-catenin and glycolysis. iScience. 2023 Apr 10;26(5):106644. doi: 10.1016/j.isci.2023.106644. PMID: 37192966; PMCID: PMC10182326.

[6]. Jiao F, Wang Y, et,al. AGK2 Alleviates Lipopolysaccharide Induced Neuroinflammation through Regulation of Mitogen-Activated Protein Kinase Phosphatase-1. J Neuroimmune Pharmacol. 2020 Jun;15(2):196-208. doi: 10.1007/s11481-019-09890-x. Epub 2019 Nov 30. PMID: 31786712.

[7]. Jiao FZ, Wang Y, et,al. Protective role of AGK2 on thioacetamide-induced acute liver failure in mice. Life Sci. 2019 Aug 1;230:68-75. doi: 10.1016/j.lfs.2019.05.061. Epub 2019 May 23. PMID: 31129140.

[8]. Yu HB, Jiang H, et,al. AGK2, A SIRT2 Inhibitor, Inhibits Hepatitis B Virus Replication In Vitro And In Vivo. Int J Med Sci. 2018 Sep 7;15(12):1356-1364. doi: 10.7150/ijms.26125. PMID: 30275764; PMCID: PMC6158674.