2. PI3K/Akt/mTOR Stem Cell/Wnt
  3. GSK-3
  4. AR-A014418

AR-A014418  (Synonyms: AR 0133418; GSK 3β inhibitor VIII; AR 014418)

Cat. No.: HY-10512 Purity: 99.14%
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AR-A014418 is a potent, selective and ATP-competitive GSK3β inhibitor (IC50=104 nM; Ki=38 nM).

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

AR-A014418 Chemical Structure

AR-A014418 Chemical Structure

CAS No. : 487021-52-3

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10 mM * 1 mL in DMSO
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Based on 19 publication(s) in Google Scholar

Other Forms of AR-A014418:

AR-A014418 Related Antibodies

Top Publications Citing Use of Products

    AR-A014418 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 Jun 25;37(1):122.  [Abstract]

    Treatment of MHCC97H cells with AR-A014418 for 24 h inhibits the expression of CD133, detected by RT-PCR.

    AR-A014418 purchased from MedChemExpress. Usage Cited in: Toxicol Sci. 2018 Apr 1;162(2):475-487.  [Abstract]

    Inhibition of GSK-3β enhances demethylation of PP2Ac induced by MC-LR. SH-SY5Y cells are treated with 20 μM AR-A014418 for 4 h and then treated with 10 μM MC-LR for 24 h. Levels of DM-PP2Ac and PP2Ac are measured by Western blots.

    View All GSK-3 Isoform Specific Products:

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    GSK-3 GSK-3α GSK-3β

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    AR-A014418 is a potent, selective and ATP-competitive GSK3β inhibitor (IC50=104 nM; Ki=38 nM)[1].

    IC50 & Target[1]

    GSK-3β

    104 nM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    BXPC-3 IC50
    14 μM
    Compound: 77, AR-A014418
    Growth inhibition of human BxPC3 cells after 72 hrs by MTS assay
    Growth inhibition of human BxPC3 cells after 72 hrs by MTS assay
    		[PMID: 19338355]
    HuP-T3 IC50
    22 μM
    Compound: 77, AR-A014418
    Growth inhibition of human HUPT3 cells after 72 hrs by MTS assay
    Growth inhibition of human HUPT3 cells after 72 hrs by MTS assay
    		[PMID: 19338355]
    MIA PaCa-2 IC50
    29 μM
    Compound: 77, AR-A014418
    Growth inhibition of human MIAPaCa2 cells after 72 hrs by MTS assay
    Growth inhibition of human MIAPaCa2 cells after 72 hrs by MTS assay
    		[PMID: 19338355]
    Sf21 IC50
    0.104 μM
    Compound: AR-A014418
    Inhibition of recombinant full length human GSK3beta expressed in Sf21 insect cells using biotinylated-AAEELDSRAGS(PO3H2)PQL peptide as substrate preincubated enzyme-substrate mixture for 15 to 20 mins followed by [gamma-33P]ATP addition and measured afte
    Inhibition of recombinant full length human GSK3beta expressed in Sf21 insect cells using biotinylated-AAEELDSRAGS(PO3H2)PQL peptide as substrate preincubated enzyme-substrate mixture for 15 to 20 mins followed by [gamma-33P]ATP addition and measured afte
    		[PMID: 32435391]
    In Vitro

    AR-A014418 blocks the phosphorylation of tau at a GSK3-specific site (Ser-396) in 3T3 fibroblasts expressing human four-repeat tau protein, with an IC50 of 2.7 μM, and protects cultured N2A cells from death cuased by PI3K/PKB pathway blockage. AR-A014418 also shows inhibitory effect on neurodegeneration mediated by beta-amyloid peptide in hippocampal slices[1].
    AR-A014418 decreases neuroendocrine markers and suppresses neuroblastoma cell growth in NGP and SH-5Y-SY cells[2].

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

    AR-A014418 Related Antibodies
    In Vivo

    AR-A014418 (0-4 mg/kg, i.p.) delays the onset of symptoms, enhances motor activity, blocks disease progression, and postpons the endpoint of the disease in ALS mouse model with the G93A mutant human SOD1[3].
    AR-A014418 suppresses acetic acid- and formalin-induced nociception in mice via modulating NMDA and metabotropic receptor signaling as well as TNF-α and IL-1β transmission in the spinal cord[4].

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

    308.31

    Formula

    C12H12N4O4S
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C(NCC1=CC=C(OC)C=C1)NC2=NC=C([N+]([O-])=O)S2
    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 : ≥ 100 mg/mL (324.35 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.2435 mL 16.2174 mL 32.4349 mL
    5 mM 0.6487 mL 3.2435 mL 6.4870 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.

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    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

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    C2

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    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: ≥ 2.5 mg/mL (8.11 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
    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
    References
    Kinase Assay
    [1]

    The competition experiments are carried out in duplicate with 10 concentrations of the inhibitor in clear-bottomed microtiter plates. The biotinylated peptide substrate, biotin-AAEELDSRAGS(PO3H2)PQL, is added at a final concentration of 2 μM in an assay buffer containing 6 milliunits of recombinant human GSK3 (equal mix of both α and β), 12 mM MOPS, pH 7.0, 0.3 mM EDTA, 0.01% β-mercaptoethanol, 0.004% Brij 35, 0.5% glycerol, and 0.5 μg of bovine serum albumin/25 μL and preincubated for 10-15 min. The reaction is initiated by the addition of 0.04 μCi of [γ-33P]ATP and unlabeled ATP in 50 mM Mg(Ac)2 to a final concentration of 1 μM ATP and assay volume of 25 μL. Blank controls without peptide substrate are used. After incubation for 20 min at room temperature, each reaction is terminated by the addition of 25 μL of stop solution containing 5 mM EDTA, 50 μM ATP, 0.1% Triton X-100, and 0.25 mg of streptavidin-coated SPA beads corresponding to appr 35 pmol of binding capacity. After 6 h the radioactivity is determined in a liquid scintillation counter. Inhibition curves are analyzed by non-linear regression using GraphPad Prism.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Cell Assay
    [1]

    Cell viability is assessed by calcein/propidium iodide uptake. Calcein AM is taken up and cleaved by esterases present within living cells, yielding yellowish-green fluorescence, whereas PI is only taken up by dead cells, which become orange-red fluorescent. In brief, N2A cells are cultured for 2 days in vitro and then treated with 50 μM LY-294002 in the presence of AR-A014418 or vehicle (DMSO) for 24 h. Subsequently, N2A cells are incubated for 30 min with 2 μM PI and 1 μM calcein-AM. The cultures are then rinsed three times with Hanks' buffered saline solution containing 2 mM CaCl2, and the cells are visualized by fluorescence microscopy using a Zeiss Axiovert 135 microscope. Three fields (selected at random) are analyzed per well (appr 300 cells/field) in at least three different experiments. Cell death is expressed as percentage of PI-positive cells from the total number of cells. In every experiment, specific cell death is obtained after subtracting the number of dead cells present in vehicle-treated cultures.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [3]

    First, to examine the effects of GSK-3 inhibition on the clinical symptoms, life span, and motor behavior function of ALS, 56 Tg mice are divided into four groups. In each group, 0.5 mL of normal saline is mixed with either 0 μg (control group), 1 μg (group A), 2 μg (group B) or 4 μg (group C) of AR-A014418 per gram of mouse, and injected intraperitoneally into 14 animals per group 5 days a week beginning 60 days after birth. The mice are sacrificed at the endpoint described below.

    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 3.2435 mL 16.2174 mL 32.4349 mL 81.0872 mL
    5 mM 0.6487 mL 3.2435 mL 6.4870 mL 16.2174 mL
    10 mM 0.3243 mL 1.6217 mL 3.2435 mL 8.1087 mL
    15 mM 0.2162 mL 1.0812 mL 2.1623 mL 5.4058 mL
    20 mM 0.1622 mL 0.8109 mL 1.6217 mL 4.0544 mL
    25 mM 0.1297 mL 0.6487 mL 1.2974 mL 3.2435 mL
    30 mM 0.1081 mL 0.5406 mL 1.0812 mL 2.7029 mL
    40 mM 0.0811 mL 0.4054 mL 0.8109 mL 2.0272 mL
    50 mM 0.0649 mL 0.3243 mL 0.6487 mL 1.6217 mL
    60 mM 0.0541 mL 0.2703 mL 0.5406 mL 1.3515 mL
    80 mM 0.0405 mL 0.2027 mL 0.4054 mL 1.0136 mL
    100 mM 0.0324 mL 0.1622 mL 0.3243 mL 0.8109 mL
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    AR-A014418 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:

    AR-A014418487021-52-3AR 0133418 GSK 3β inhibitor VIII AR 014418AR0133418AR-0133418AR014418AR 014418AR-014418GSK-3Glycogen synthase kinase-3Glycogen synthase kinase 3Inhibitorinhibitorinhibit

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