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AGK 2

AGK2 is a selective SIRT2 inhibitor, with an IC50 of 3.

原价
¥875-7550
价格
700-6040
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  • 货号: ajci20004
  • CAS: 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
  • 分子式: C23H13Cl2N3O2
  • 分子量: 434.27
  • 纯度: >98%
  • 溶解度: ≥ 9.3mg/mL in DMSO
  • 储存: Store at -20°C
  • 库存: 现货

Background

AGK2 is a selective SIRT2 inhibitor, with an IC50 of 3.5 μM. AGK2 inhibits SIRT1 and SIRT3 with IC50 of 30 and 91 μM, respectively[1,2].


AGK2(0.01-20 μM;24 h) inhibits mast cell degranulation in vitro, AGK2 treatment reduced high levels of β-hexosaminidase and histamine in RBL-2H3 cells[3]. AGK2(1-5 μM;24 h) suppress cell growth and migration by inhibiting HSF1 protein stability in HeLa cells[4]. Sirtuin 2 (SIRT2) inhibition by AGK2 significantly enhances the BCG vaccine efficacy during primary infection and TB recurrence through enhanced stem cell memory (TSCM) responses[5].


AGK2(1 μmol/mouse;i.p;26h) could inhibit the activation of BV2 microglia and expression of iNOS and SIRT2 in LPS treated mice brain tissue[6]. AGK2 (1μmol/mouse;i.p;26h)pretreatment also reduced the levels of pro-inflammatory cytokines in acute liver failure (ALF) liver tissues. AGK2 improved the thioacetamide (TAA)-induced survival rate[7]. AGK2(82 mg/kg;i.p;7days) treatment inhibited serum HBV DNA, HBeAg and HBsAg levels as well as hepatic HBV DNA, RNA and HBc in the HBV transgenic mice[8].


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]。

参考文献:
[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.

Protocol

Cell experiment [1]:

Cell lines

RBL-2H3 cell

Preparation method

Cells were incubated with AGK2, total β-glucosamine activity was measured.

Reaction Conditions

0.01–20 μM;24 h

Applications

AGK2 treatment reduced high levels of β-hexosaminidase and histamine in RBL-2H3 cells.

Animal experiment [2]:

Animal models

Male C57BL/6 J mice (6–7 weeks)

Preparation method

Mice were divided into four groups: namely, control, LPS, AGK2 plus LPS, and AGK2 group.

The LPS group was administrated by intraperitoneal injection with LPS (10 mg/kg). The dosage of AGK2 was 1 μmol/mouse.

AGK2 (25 mg) was dissolved in DMSO and formed 10 mM mother liquor. Then, the solution was diluted in normal saline (NS) and formed final concentration of AGK2 (400 μM, 4% DMSO).

For AGK2 + LPS group and AGK2 group, 2.5 ml AGK2 (400 μM) was injected into abdominal cavities of each mouse. AGK2 was given in AGK2 plus LPS group before LPS administration 2 h. The same volume of 4% DMSO solution was injected in control group as well.

All mice were sacrificed, and the brain tissues were harvested at 24 h after LPS treatment.

Dosage form

1 μmol/mouse; i.p;26h

Applications

AGK2 suppressed the expression of inflammatory cytokines after LPS treatment in mice brain.

参考文献:

[1]. 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.

[2]. 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.

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