AGK 2 |
| Katalog-Nr.GC17881 |
AGK 2 ist ein selektiver SIRT2-Inhibitor mit einem IC50 von 3,5 μM. AGK 2 hemmt SIRT1 und SIRT3 mit IC50-Werten von 30 bzw. 91 μM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 304896-28-4
Sample solution is provided at 25 µL, 10mM.
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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].
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.
Average Rating: 5 (Based on Reviews and 36 reference(s) in Google Scholar.)
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