2. Metabolic Enzyme/Protease
  3. Pyruvate Kinase
  4. TEPP-46

TEPP-46 est un activateur puissant et sélectif de pyruvate kinase M2 (PKM2) avec un AC50 de 92 nM, montrant peu ou pas d'effet sur PKM1, PKL et PKR.

TEPP-46 ist ein potenter und selektiver Pyruvatkinase M2 (PKM2) -Aktivator mit einem AC50 von 92 nM, der nur geringe oder keine Auswirkungen auf PKM1, PKL und PKR zeigt.

TEPP-46 (ML-265) is a potent and selective pyruvate kinase M2 (PKM2) activator with an AC50 of 92 nM, showing little or no effect on PKM1, PKL and PKR.

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

TEPP-46 Chemical Structure

TEPP-46 Chemical Structure

CAS No. : 1221186-53-3

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 132 In-stock
Solution
10 mM * 1 mL in DMSO USD 132 In-stock
Solid
1 mg USD 33 In-stock
5 mg USD 120 In-stock
10 mg USD 180 In-stock
50 mg USD 450 In-stock
100 mg USD 720 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 40 publication(s) in Google Scholar

TEPP-46 Related Antibodies

Top Publications Citing Use of Products

38 Publications Citing Use of MCE TEPP-46

WB
IF

    TEPP-46 purchased from MedChemExpress. Usage Cited in: Cell Rep. 2020 May 26;31(8):107690.  [Abstract]

    Immunofluorescence of PKM2 in DCs. When added TEPP-46 to prevent the dissociation of PKM2 tetramers, LPS-induced accumulation of nuclear PKM2 as well as IL-12 expression is diminished.

    TEPP-46 purchased from MedChemExpress. Usage Cited in: Cell Rep. 2020 May 26;31(8):107690.  [Abstract]

    Analysis of enzymatic activity of PKM2. Protein level of PKM2 is analyzed using Western Blotting.

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    TEPP-46 (ML-265) is a potent and selective pyruvate kinase M2 (PKM2) activator with an AC50 of 92 nM, showing little or no effect on PKM1, PKL and PKR[1].

    In Vitro

    TEPP-46 and DASA-58 activate PKM2 by a mechanism similar to that of the endogenous activator FBP. Pre-treatment of cells with TEPP-46 or DASA-58 prevents pervanadate-induced inhibition of PKM2 activity. TEPP-46 also induces a decrease in the intracellular levels of acetyl-coA, lactate, ribose phosphate and serine[1]. TEPP-46 inhibits LPS-induced Hif-1α and IL-1β, as well as the expression of a range of other Hif-1α-dependent genes. TEPP-46 treatment significantly downregulates the expression of the M1 markers Il12p40 and Cxcl-10. Activation of PKM2 using TEPP-46 significantly inhibits FSL-1 and CpG-induced Il1b mRNA expression. TEPP-46 inhibits Mtb-induced Il1b mRNA levels, boosts Mtb-induced levels of Il10 mRNA, and has no effect on levels of Tnf[2].

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

    TEPP-46 Related Antibodies
    In Vivo

    TEPP-46 exhibits good oral bioavailability with relatively low clearance, long half-life, and good volume of distribution-parameters that predict for drug exposure in tumor tissues. TEPP-46 at 150 mg/kg readily achieves maximal PKM2 activation measured in A549 xenograft tumors[1].

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

    372.46

    Formula

    C17H16N4O2S2
    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    O=C1C(N(C)C2=C3SC(S(C)=O)=C2)=C3C=NN1CC4=CC=CC(N)=C4
    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 : 50 mg/mL (134.24 mM; Need ultrasonic; 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 2.6849 mL 13.4243 mL 26.8485 mL
    5 mM 0.5370 mL 2.6849 mL 5.3697 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
    =
    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:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: ≥ 2.87 mg/mL (7.71 mM); Clear solution

    • Protocol 2

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

      Solubility: ≥ 2.5 mg/mL (6.71 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.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  50% PEG300    50% Saline

      Solubility: 10 mg/mL (26.85 mM); Suspended solution; Need ultrasonic

    • Protocol 2

      Add each solvent one by one:  0.5% CMC-Na/saline water

      Solubility: 5 mg/mL (13.42 mM); Suspended solution; Need ultrasonic

    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: 99.93%

    COA (251 KB) LCMS (94 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [1]

    2,000 cells are seeded in 96-well plates 24 h prior to treatment start. CellTiter96® AQueous is used to assess cell viability following oxidant and PKM2 activator combination treatments. MTS: (3-(4,5-dimethylthiazol-2-yl)-5- (3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium).

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

    H1299 parental and H1299 cells with constitutive expression of a mouse PKM1 cDNA (H1299-PKM1 cells) are propagated in RPMI supplemented with 10% fetal bovine serum, 2 mM glutamine, and hygromycin for transgene selection. Cells are harvested, resuspended in sterile PBS, and 5×105 cells are injected subcutaneously into nu/nu mice. Tumor growth is monitored by caliper measurement, the mice are sacrificed and tumors harvested after the time indicated. Tumors are weighed, divided and either flash-frozen in liquid nitrogen or fixed in formalin for later analysis.

    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, 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 2.6849 mL 13.4243 mL 26.8485 mL 67.1213 mL
    5 mM 0.5370 mL 2.6849 mL 5.3697 mL 13.4243 mL
    10 mM 0.2685 mL 1.3424 mL 2.6849 mL 6.7121 mL
    15 mM 0.1790 mL 0.8950 mL 1.7899 mL 4.4748 mL
    20 mM 0.1342 mL 0.6712 mL 1.3424 mL 3.3561 mL
    25 mM 0.1074 mL 0.5370 mL 1.0739 mL 2.6849 mL
    30 mM 0.0895 mL 0.4475 mL 0.8950 mL 2.2374 mL
    40 mM 0.0671 mL 0.3356 mL 0.6712 mL 1.6780 mL
    50 mM 0.0537 mL 0.2685 mL 0.5370 mL 1.3424 mL
    60 mM 0.0447 mL 0.2237 mL 0.4475 mL 1.1187 mL
    80 mM 0.0336 mL 0.1678 mL 0.3356 mL 0.8390 mL
    100 mM 0.0268 mL 0.1342 mL 0.2685 mL 0.6712 mL
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    TEPP-46 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:

    TEPP-461221186-53-3ML-265TEPP46TEPP 46ML265ML 265Pyruvate KinaseInhibitorinhibitorinhibit

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