2. Metabolic Enzyme/Protease
  3. Pyruvate Kinase
  4. DASA-58

DASA-58 is a potential pyruvate kinase isozyme (PKM2) allosteric activator. DASA-58 can be used for the research of metabolism and kinds of cancer.

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

DASA-58 Chemical Structure

DASA-58 Chemical Structure

CAS No. : 1203494-49-8

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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Customer Review

Based on 14 publication(s) in Google Scholar

DASA-58 Related Antibodies

Top Publications Citing Use of Products

    DASA-58 purchased from MedChemExpress. Usage Cited in: Drug Des Dev Ther. 2020 May 27;14:2091-2100.  [Abstract]

    The growth inhibition of DHA after 24 hrs together with 40 μM DASA-58 (a PKM2 agonist). Tumor cell growth inhibition is determined by CCK-8 after treated with various concentrations of DHA at different times.

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    DASA-58 is a potential pyruvate kinase isozyme (PKM2) allosteric activator. DASA-58 can be used for the research of metabolism and kinds of cancer[1].

    In Vitro

    DASA-58 (15 μM; 2 h) potentiates the antitumor effects of other metabolic stressors[1].
    ? DASA-58 (15 μM; 24 h, 72 h) enhances pyruvate kinase activity in breast cancer cells without a clear effect on proliferation[1].
    ? DASA-58 (30 μM, 60 μM; 0-72 h) enhances extracellular acidification and lactate levels in BCa cell lines and induce extracellular acidification levels in prostate cancer cell lines[1].
    ? DASA-58 (15 μM, 30 μM; 0-72 h) affects respiration levels in BCa cells without an indication of mitochondrial damage[1].
    ? DASA-58 (15 μM; 0-72 h) not rescues TXNIP levels in any combintion and mitochondrial inhibitors enhance PKM2 effects on activating AMPK signaling (T172 phosphorylation of AMPK) [1].
    ? DASA-58 (15 μM; 0-72 h) leads to depletion in TXNIP levels independent of? AMPK and ER signaling, and not through enhanced? proteasomal degradation but rather depleted upstream glycolytic intermediates[1].

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

    DASA-58 Related Antibodies

    Cell Viability Assay[1]

    Cell Line: Five breast cancer cell lines (BCa cells)
    (MDA MB 231, MDA MB 468, HCC 1443, T47-D, MCF7, LnCap, PC3, and DU145)
    Concentration: 15 μM
    Incubation Time: 2 h
    Result: Could be exploited by other metabolic stressors.

    Western Blot Analysis[1]

    Cell Line: BCa cells
    Concentration: 15 μM
    Incubation Time: 24 h, 72 h
    Result: Showed comparable PKM2 protein levels in five breast cancer cell lines, except HCC1443 cells and MDA MB 468 that showed the highest and lowest PKM2 protein levels, respectively.
    Not changed PKM2 levels in five breast cancer cell lines but seemingly reduced TXNIP levels in cells expressing detectable TXNIP levels.
    Molecular Weight

    453.53

    Formula

    C19H23N3O6S2
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    NC1=CC=CC(S(=O)(N2CCN(S(=O)(C3=CC=C(OCCO4)C4=C3)=O)CCC2)=O)=C1
    Shipping

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

    DMSO : ≥ 35 mg/mL (77.17 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 2.2049 mL 11.0246 mL 22.0493 mL
    5 mM 0.4410 mL 2.2049 mL 4.4099 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.

    • 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

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    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: ≥ 2.08 mg/mL (4.59 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.59 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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
    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, 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 2.2049 mL 11.0246 mL 22.0493 mL 55.1231 mL
    5 mM 0.4410 mL 2.2049 mL 4.4099 mL 11.0246 mL
    10 mM 0.2205 mL 1.1025 mL 2.2049 mL 5.5123 mL
    15 mM 0.1470 mL 0.7350 mL 1.4700 mL 3.6749 mL
    20 mM 0.1102 mL 0.5512 mL 1.1025 mL 2.7562 mL
    25 mM 0.0882 mL 0.4410 mL 0.8820 mL 2.2049 mL
    30 mM 0.0735 mL 0.3675 mL 0.7350 mL 1.8374 mL
    40 mM 0.0551 mL 0.2756 mL 0.5512 mL 1.3781 mL
    50 mM 0.0441 mL 0.2205 mL 0.4410 mL 1.1025 mL
    60 mM 0.0367 mL 0.1837 mL 0.3675 mL 0.9187 mL
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    DASA-58 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:

    DASA-581203494-49-8DASA58DASA 58Pyruvate Kinasepyruvate kinase M2AMPKTXNIPglycolysiscancer metabolismbreast cancerInhibitorinhibitorinhibit

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