2. Metabolic Enzyme/Protease Apoptosis
  3. PAI-1 Apoptosis
  4. TM5441

TM5441 is an orally bioavailable inhibitor of plasminogen activator inhibitor-1 (PAI-1), has IC50 values between 13.9 and 51.1 μM and induces intrinsic apoptosis in several human cancer cell lines. TM5441 attenuates Nω-nitro-l-arginine methyl ester-induced cardiac hypertension and vascular senescence.

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

CAS No. : 1190221-43-2

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

Based on 10 publication(s) in Google Scholar

Other Forms of TM5441:

TM5441 Related Antibodies

Top Publications Citing Use of Products

    TM5441 purchased from MedChemExpress. Usage Cited in: Sci Adv. 2025 Jun 6;11(23):eadu2695.  [Abstract]

    Percent αSMA reduction in male VICs (blue) and female VICs (red) cultured on TCPS with indicated doses of TM5441 (0-1000 μM).

    TM5441 purchased from MedChemExpress. Usage Cited in: Kidney Int. 2023 Sep;104(3):508-525.  [Abstract]

    TM5441 decreased SERPINE1, TGFB1 and CDH6.

    TM5441 purchased from MedChemExpress. Usage Cited in: Kidney Int. 2023 Sep;104(3):508-525.  [Abstract]

    TM5441 (PAI-1 inhibitor) or vehicle (DMSO) to the previous transwell systems. TM5441 treatment in the podocytes decreased TGFB1 and FN1.

    TM5441 purchased from MedChemExpress. Usage Cited in: Sci Rep. 2023 Sep 27;13(1):16210.  [Abstract]

    Paracrine senescence effects were largely abolished by the addition of the Serpin E1 inhibitor TM5441 (10 μM, pre-incubate for 1 hour) to the conditioned medium.

    TM5441 purchased from MedChemExpress. Usage Cited in: Res Sq. 2023 Jun 5:rs.3.rs-2986934.

    HEK293 cells with NC or ALDH1L2 siRNA were treated with PAI-1 inhibitor TM5441 and then subjected to TGF-b1 treatment.

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    TM5441 is an orally bioavailable inhibitor of plasminogen activator inhibitor-1 (PAI-1), has IC50 values between 13.9 and 51.1 μM and induces intrinsic apoptosis in several human cancer cell lines. TM5441 attenuates Nω-nitro-l-arginine methyl ester-induced cardiac hypertension and vascular senescence[1][2].

    IC50 & Target

    IC50: 13.9~51.1 μM (Tumor cell lines)[1]
    In Vitro

    TM5441 dose-dependently decreases HT1080, HCT116, Daoy, MDA-MB-231 and Jurkat cells with an IC50 ranging between 13.9 and 51.1 μM[1].
    TM5441 increases caspase 3/7 activity for both HT1080 and HCT116 cells in a dose dependant manner. TM5441 increases apoptosis in HT1080 and HCT116 cells[1].
    TM5441 induces mitochondrial depolarization[1].
    In mouse proximal tubular epithelial cells, TM5441 effectively inhibits PAI-1-induced mRNA expression of fibrosis and inflammation markers and also reverses PAI-1-induced inhibition of plasmin activity[2].

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

    TM5441 Related Antibodies
    In Vivo

    Oral administration of TM5441 (20 mg/kg daily) to HT1080 and HCT116 xenotransplanted mice increases tumor cell apoptosis and has a significant disruptive effect on the tumor vasculature that is associated with a decrease in tumor growth and an increase in survival. The average peak plasma concentration is 11.4 μM one hour after oral administration and undetectable levels 23 hours after administration[1].
    TM5441 attenuates Nω-nitro-l-arginine methyl ester-induced cardiac hypertension and vascular senescence, prolongs lifespan in klotho null mice and elicits anti-tumorigenic and anti-angiogenic activities in cancer[3].

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

    428.82

    Formula

    C21H17ClN2O6
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    ClC1=CC=C(NC(COCC(NC2=CC=CC(C3=COC=C3)=C2)=O)=O)C(C(O)=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 : 100 mg/mL (233.20 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 2.3320 mL 11.6599 mL 23.3198 mL
    5 mM 0.4664 mL 2.3320 mL 4.6640 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
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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

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    Volume (start)

    V1

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    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: ≥ 2.5 mg/mL (5.83 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.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (5.83 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    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: 99.97%

    SDS (393 KB)

    COA (252 KB) HNMR (272 KB) RP-HPLC (255 KB) LCMS (102 KB)

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

    HT1080, HCT116, Daoy, MDA-MB-231 and Jurkat cells are treated with 0-100 μM TM5441 for 48 hours at 37°C. Cell viability is measured by MTT assay[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [2]

    Mice: TM5275 at 50 mg/kg/day and TM5441 at 10 mg/kg/day were orally administered in control and diabetic mice for 16 weeks. Mice were monitored at least once a day. At the end, blood is collected for measurement of plasma glucose and creatinine, urine for protein measurement, and kidneys for immunohistochemical analysis[2].

    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 2.3320 mL 11.6599 mL 23.3198 mL 58.2995 mL
    5 mM 0.4664 mL 2.3320 mL 4.6640 mL 11.6599 mL
    10 mM 0.2332 mL 1.1660 mL 2.3320 mL 5.8300 mL
    15 mM 0.1555 mL 0.7773 mL 1.5547 mL 3.8866 mL
    20 mM 0.1166 mL 0.5830 mL 1.1660 mL 2.9150 mL
    25 mM 0.0933 mL 0.4664 mL 0.9328 mL 2.3320 mL
    30 mM 0.0777 mL 0.3887 mL 0.7773 mL 1.9433 mL
    40 mM 0.0583 mL 0.2915 mL 0.5830 mL 1.4575 mL
    50 mM 0.0466 mL 0.2332 mL 0.4664 mL 1.1660 mL
    60 mM 0.0389 mL 0.1943 mL 0.3887 mL 0.9717 mL
    80 mM 0.0291 mL 0.1457 mL 0.2915 mL 0.7287 mL
    100 mM 0.0233 mL 0.1166 mL 0.2332 mL 0.5830 mL
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    TM5441 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:

    TM54411190221-43-2TM 5441TM-5441PAI-1ApoptosisPlasminogen activator inhibitor-1Inhibitorinhibitorinhibit

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