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

TEPP-46 (Synonyms: ML-265)

Cat. No.: HY-18657 Purity: 99.71%
Handling Instructions

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 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
Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 180 In-stock
Estimated Time of Arrival: December 31
50 mg USD 540 In-stock
Estimated Time of Arrival: December 31
100 mg USD 780 In-stock
Estimated Time of Arrival: December 31
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500 mg   Get quote  

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Customer Review

Based on 10 publication(s) in Google Scholar

Top Publications Citing Use of Products

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

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

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

    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.
    • Biological Activity

    • Protocol

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    • References

    • Customer Review

    Description

    TEPP-46 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].

    IC50 & Target

    AC50: 92 nM (PKM2)

    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].

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

    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].

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

    Molecular Weight

    372.46

    Formula

    C₁₇H₁₆N₄O₂S₂

    CAS No.

    1221186-53-3

    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 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (134.24 mM; Need ultrasonic)

    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
    10 mM 0.2685 mL 1.3424 mL 2.6849 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      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

    • 2.

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

      Solubility: 2.5 mg/mL (6.71 mM); Suspended solution; Need ultrasonic

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (6.71 mM); Clear solution

    • 4.

      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

    *All of the co-solvents are provided by MCE.
    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

    Purity: 99.71%

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    Keywords:

    TEPP-46ML-265TEPP46TEPP 46ML265ML 265Pyruvate KinaseInhibitorinhibitorinhibit

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    Product Name:
    TEPP-46
    Cat. No.:
    HY-18657
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