2. Epigenetics PI3K/Akt/mTOR
  3. AMPK
  4. EX229

EX229, a Benzimidazole derivative, is a potent and allosteric activator of AMP-activated protein kinase (AMPK), with Kds of 0.06 μM, 0.06 μM and 0.51 μM for α1β1γ1, α2β1γ1 and α1β2γ1 in biolayer interferometry, respectively.

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CAS. Nr. : 1219739-36-2

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10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 5 publication(s) in Google Scholar

EX229 Related Antibodies

Top Publications Citing Use of Products

    EX229 purchased from MedChemExpress. Usage Cited in: Redox Biol. 2025 Apr:81:103567.  [Abstract]

    Cell death measurement in AMPK WT and DKO H1299 cells treated with nab-PTX (50 nM) with or without EX229 (40 μM; 36 h).

    EX229 purchased from MedChemExpress. Usage Cited in: Redox Biol. 2025 Apr:81:103567.  [Abstract]

    Immunoblot showing the levels of AMPK T172 phosphorylation, AMPK, ACC S79 phosphorylation, ACC, cleaved-caspase 7 (C-Cas-7), and cleaved PARP (C-PARP) in AMPK WT and DKO H1299 cells treated with nab-PTX (50 nM) with or without EX229 (40 μM; 36 h).

    EX229 purchased from MedChemExpress. Usage Cited in: Redox Biol. 2025 Apr:81:103567.  [Abstract]

    EX229 (40 μM; 24 h) significantly enhanced the activation of AMPK in H1299 cells with WT-LKB1.

    EX229 purchased from MedChemExpress. Usage Cited in: Redox Biol. 2025 Apr:81:103567.  [Abstract]

    EX229 (40 μM; 36 h) reduced the death of H1299 cells with WT-LKB1 induced by nab-PTX.

    EX229 purchased from MedChemExpress. Usage Cited in: Redox Biol. 2025 Apr:81:103567.  [Abstract]

    EX229 (40 μM; 24 h) activated AMPK in A549 cells with mutated LKB1.

    Alle AMPK Isoform-spezifische Produkte anzeigen:

    Alle Isoformen anzeigen
    NUAK1 NUAK2 AMPK AMPK α1β1γ1 AMPK α2β1γ1 AMPK α1β2γ1 AMPK α2β2γ1 BRSK1 BRSK2 HUNK AMPKα

    • Biologische Aktivität

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    Beschreibung

    EX229, a Benzimidazole derivative, is a potent and allosteric activator of AMP-activated protein kinase (AMPK), with Kds of 0.06 μM, 0.06 μM and 0.51 μM for α1β1γ1, α2β1γ1 and α1β2γ1 in biolayer interferometry, respectively.

    IC50 & Target[1]

    AMPK α1β1γ1

    0.06 μM (Kd)

    AMPK α2β1γ1

    0.06 μM (Kd)

    AMPK α1β2γ1

    0.51 μM (Kd)

    Cellular Effect
    Cell Line Type Value Description References
    Sf21 EC50
    3 nM
    Compound: 20
    Activation of full length human recombinant AMPK alpha1/beta1/gamma1 expressed in baculovirus infected sf21 cells using SAMS peptide substrate after 30 mins in presence of [33P]ATP by TopCount analysis
    Activation of full length human recombinant AMPK alpha1/beta1/gamma1 expressed in baculovirus infected sf21 cells using SAMS peptide substrate after 30 mins in presence of [33P]ATP by TopCount analysis
    		[PMID: 27727125]
    In Vitro

    EX229 is a potent and allosteric activator of AMP-activated protein kinase (AMPK), with Kds of 0.06 μM, 0.06 μM and 0.51 μM for α1β1γ1, α2β1γ1 and α1β2γ1, respectively.[1]. Treatment of hepatocytes with EX229 (991) alone results in a slight increase in the phosphorylation of AMPK and RAPTOR only at 0.3 μM, whereas a robust increase in ACC phosphorylation is readily observed and saturated at a concentration of 0.03 μM EX229. AICAR or C13 alone robustly increases T172 phosphorylation of AMPKα, and when EX229 is coincubated, there is a modest additional dose-dependent increase in AMPKα phosphorylation. RAPTOR phosphorylation is modestly increased by AICAR or C13 alone, and it is dose dependently increased when coincubations are carried out with EX229. EX229 also dose dependently (0.01 and 0.1 μM) inhibits lipogenesis (34% and 63%, respectively), which is further reduced when it is coincubated with a low dose of AICAR (0.03 mM) or C13 (1 μM). Treatment with EX229 promotes dose-dependent increases in ACC and RAPTOR phosphorylation. Similar to the observations in hepatocytes[2].

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

    EX229 Related Antibodies
    Molekulargewicht

    431.87

    Formel

    C24H18ClN3O3
    CAS. Nr.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(O)C1=CC(OC2=NC3=CC(Cl)=C(C4=CC5=C(N(C)C=C5)C=C4)C=C3N2)=CC=C1C
    Versand

    Room temperature in continental US; may vary elsewhere.
    Speicherung
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Lösungsmittel & Löslichkeit
    In Vitro: 

    DMSO : 13 mg/mL (30.10 mM; Need ultrasonic and warming; 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 2.3155 mL 11.5776 mL 23.1551 mL
    5 mM 0.4631 mL 2.3155 mL 4.6310 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molaritätsrechner

    • Verdünnungsrechner

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    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: ≥ 1.3 mg/mL (3.01 mM); Clear solution

      This protocol yields a clear solution of ≥ 1.3 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (13.0 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: ≥ 1.3 mg/mL (3.01 mM); Clear solution

      This protocol yields a clear solution of ≥ 1.3 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (13.0 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.
    Reinheit & Dokumentation

    Purity: 99.44%

    SDS (393 KB)

    COA (249 KB) HNMR (250 KB) RP-HPLC (256 KB) LCMS (104 KB)

    Handling Instructions (2659 KB)
    Verweise

    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.3155 mL 11.5776 mL 23.1551 mL 57.8878 mL
    5 mM 0.4631 mL 2.3155 mL 4.6310 mL 11.5776 mL
    10 mM 0.2316 mL 1.1578 mL 2.3155 mL 5.7888 mL
    15 mM 0.1544 mL 0.7718 mL 1.5437 mL 3.8592 mL
    20 mM 0.1158 mL 0.5789 mL 1.1578 mL 2.8944 mL
    25 mM 0.0926 mL 0.4631 mL 0.9262 mL 2.3155 mL
    30 mM 0.0772 mL 0.3859 mL 0.7718 mL 1.9296 mL
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    EX229 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:

    EX2291219739-36-2EX 229EX-229AMPKAMP-activated protein kinaseInhibitorinhibitorinhibit

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    Art. -Nr.:
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