AGK 2 |
| رقم الكتالوجGC17881 |
AGK 2 هو مثبط انتقائي لـ SIRT2 مع IC 50 من 3.5 ميكرومتر. AGK 2 يمنع SIRT1 و SIRT3 مع IC50s من 30 و 91 ميكرومتر ، على التوالي.
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.
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Cell experiment [1]: |
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Cell lines |
RBL-2H3 cell |
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Preparation method |
Cells were incubated with AGK2, total β-glucosamine activity was measured. |
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Reaction Conditions |
0.01–20 μM;24 h |
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Applications |
AGK2 treatment reduced high levels of β-hexosaminidase and histamine in RBL-2H3 cells. |
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Animal experiment [2]: |
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Animal models |
Male C57BL/6 J mice (6–7 weeks) |
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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. |
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Dosage form |
1 μmol/mouse; i.p;26h |
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Applications |
AGK2 suppressed the expression of inflammatory cytokines after LPS treatment in mice brain. |
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References: [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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| Cas No. | 304896-28-4 | SDF | |
| Chemical Name | (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 | ||
| Formula | C23H13Cl2N3O2 | M.Wt | 434.27 |
| الذوبان | ≥ 9.3mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3027 mL | 11.5136 mL | 23.0271 mL |
| 5 mM | 0.4605 mL | 2.3027 mL | 4.6054 mL |
| 10 mM | 0.2303 mL | 1.1514 mL | 2.3027 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 36 reference(s) in Google Scholar.)
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