2. Cell Cycle/DNA Damage Epigenetics Apoptosis
  3. Sirtuin Apoptosis
  4. AGK2

AGK2 is a selective SIRT2 inhibitor with an IC50 of 3.5 μM. AGK2 inhibits SIRT1 and SIRT3 with IC50s of 30 and 91 μM, respectively.

For research use only. We do not sell to patients.

CAS No. : 304896-28-4

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Customer Review

Based on 19 publication(s) in Google Scholar

Other Forms of AGK2:

AGK2 Related Antibodies

Top Publications Citing Use of Products

    AGK2 purchased from MedChemExpress. Usage Cited in: Theranostics. 2021 Feb 25;11(9):4381-4402.  [Abstract]

    AGK2 (1 mg/kg/day) were injected intraperitoneally. Liver SIRT2 activity, liver NAD+ level, plasma NAD+ level, Serum ALT activity and serum irisin level were determined in five groups of mice. NAFLD model was induced by MCD diet for 4 weeks.

    AGK2 purchased from MedChemExpress. Usage Cited in: Theranostics. 2021 Feb 25;11(9):4381-4402.  [Abstract]

    AGK2 (1 mg/kg/day) were injected intraperitoneally. Representative images and quantitative analysis of lipid accumulation, NAFLD activity score, macrophage infiltration and liver fibrosis according to Oil Red O staining, H & E staining, F4/80 immunohistochemistry staining and Masson trichrome staining respectively.

    AGK2 purchased from MedChemExpress. Usage Cited in: Theranostics. 2021 Feb 25;11(9):4381-4402.  [Abstract]

    AGK2 (1 mg/kg/day) were injected intraperitoneally. Fndc5 protein expression in mice under normal or NAFLD status.

    AGK2 purchased from MedChemExpress. Usage Cited in: Theranostics. 2021 Feb 25;11(9):4381-4402.  [Abstract]

    AGK2 (1 mg/kg/day) were injected intraperitoneally. The liver tissues were lysed and then immunoprecipitated by anti-Fndc5 antibody followed by immunoblotting with anti-Acetylated-lysine (anti-Ac) or anti-Ubiquitin to monitor the acetylation or ubiquitination of endogenous Fndc5 in mice treated with NR or NR plus AGK2. AGK2 treatment significantly abolished the decreased acetylation and ubiquitination of Fndc5 by NR.

    AGK2 purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2019 Nov;9(6):1183-1192.  [Abstract]

    AGK2 at gradient concentrations (0, 0.2, 1, 6, 30, 100, and 500 μmol/L) in assay buffer at 37 °C for 30 min. Dose–response curves and IC50 value for AGK2 and SirReal2 examined by ne-D9-based assay and ne-K4a-based assay.

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    AGK2 is a selective SIRT2 inhibitor with an IC50 of 3.5 μM. AGK2 inhibits SIRT1 and SIRT3 with IC50s of 30 and 91 μM, respectively.

    IC50 & Target[1]

    SIRT2

    3.5 μM (IC50)

    SIRT1

    30 μM (IC50)

    SIRT3

    91 μM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    Hs 683 IC50
    80.2 μM
    Compound: 4; AGK2
    Antiproliferative activity against human Hs683 cells after 72 hrs by MTT assay
    Antiproliferative activity against human Hs683 cells after 72 hrs by MTT assay
    		[PMID: 28475330]
    U-373MG ATCC IC50
    47.6 μM
    Compound: 4; AGK2
    Antiproliferative activity against human U373 cells after 72 hrs by MTT assay
    Antiproliferative activity against human U373 cells after 72 hrs by MTT assay
    		[PMID: 28475330]
    In Vitro

    AGK2 significantly inhibits cell proliferation in a dose-dependent manner. AGK2 also significantly inhibits cell growth in a dose-dependent manner without inducing cytotoxicity at low doses. Twelve days after AGK2 (5 μM) treatment, cells show a significantly reducing colony forming ability in soft agar to 46% of the control cells. Western blot analysis shows that the levels of CDK4 or CDK6 and cyclin D1 are decreased after AGK2 treatment in a dose-dependent manner. In addition, AGK2 inhibits the expression of p53 protein[2]. Treatment of microglial BV2 cells with 10 μM AGK2 leads to a significant increase in PAR signals. Treatment of microglial BV2 cells with 10 μM AGK2 also leads to a significant decrease in the intracellular ATP and significant increases in both late-stage apoptosis and necrosis of the cells[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    AGK2 Related Antibodies
    In Vivo

    AGK2 significantly reduces mortality and decreases levels of cytokines in blood (TNF-α: 298.3±24.6 vs 26.8±2.8 pg/mL, p=0.0034; IL-6: 633.4±82.8 vs 232.6±133.0 pg/mL, p=0.0344) and peritoneal fluid (IL-6: 704.8±67.7 vs 391.4±98.5 pg/mL, p=0.033) compare to vehicle control. AGK2 also suppresses the TNF-α and IL-6 production in the culturing splenocytes (TNF-α: 68.1±6.4 vs 23.9±2.8 pg/mL, p=0.0009; IL-6: 73.1±4.2 vs 49.6±3.0 pg/mL; p=0.0051)[4].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Molecular Weight

    434.27

    Formula

    C23H13Cl2N3O2
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C(NC1=C2C=CC=NC2=CC=C1)/C(C#N)=C/C3=CC=C(C4=CC(Cl)=CC=C4Cl)O3
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : 10 mg/mL (23.03 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
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    ×
    Volume
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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 0.5 mg/mL (1.15 mM); Clear solution

      This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 0.5 mg/mL (1.15 mM); Clear solution

      This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.43%

    SDS (394 KB)

    COA (251 KB) HNMR (261 KB) RP-HPLC (247 KB) MS (68 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [2]

    Cells are exposed to different concentrations of AGK2 in 1 mL of 0.3% basal medium agar containing 10% FBS. The cultures are maintained at 37°C in a 5% CO2 incubator for 10-15 days, and the cell colonies are scored using an inverted microscope[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [4]

    Mice are intraperitoneally given either AGK2 (82 mg/kg) in dimethyl sulfoxide (DMSO) or DMSO alone, and 2 h later subjects to CLP. Survival is monitored for 240 hours. AGK2-treating mice are grouped into (i) DMSO vehicle, and (ii) AGK2, with sham mice (operating but without any treatment) serving as controls. Peritoneal fluid and peripheral blood are examined at 24 and 48 hours for cytokine production[4].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.3027 mL 11.5136 mL 23.0271 mL 57.5679 mL
    5 mM 0.4605 mL 2.3027 mL 4.6054 mL 11.5136 mL
    10 mM 0.2303 mL 1.1514 mL 2.3027 mL 5.7568 mL
    15 mM 0.1535 mL 0.7676 mL 1.5351 mL 3.8379 mL
    20 mM 0.1151 mL 0.5757 mL 1.1514 mL 2.8784 mL
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    AGK2 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    AGK2304896-28-4AGK 2AGK-2SirtuinApoptosisInhibitorinhibitorinhibit

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