GLPBio

AGK 2

Catalog No.: GC17881Purity:>99.50%
COASDSData Sheet
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.

Products are for research use only. Not for human use. We do not sell to patients.

AGK 2
Cas No.: 304896-28-4
10mM (in 1mL DMSO)In Stock
$79.00
1
5mgIn Stock
$72.00
1
10mgIn Stock
$108.00
1
25mgIn Stock
$216.00
1
50mgIn Stock
$360.00
1
100mgIn Stock
$630.00
1
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Description

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.

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.

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.

Product Documents

Purity:>99.50%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
304896-28-4
Chemical Name
(E)-2-cyano-3-(5-(2,5-dichlorophenyl)furan-2-yl)-N-(quinolin-5-yl)acrylamide
SMILES
ClC(C(C1=CC=C(/C=C(C#N)/C(NC2=C3C(N=CC=C3)=CC=C2)=O)O1)=C4)=CC=C4Cl
Molecular Formula
C23H13Cl2N3O2
Molecular Weight
434.27
Solubility
≥ 9.3mg/mL in DMSO
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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