2. Immunology/Inflammation Metabolic Enzyme/Protease
  3. AP-1 MMP
  4. T-5224

T-5224 is a transcription factor c-Fos/activator protein (AP)-1 inhibitor with anti-inflammatory effects, which specifically inhibits the DNA binding activity of c-Fos/c-Jun without affecting other transcription factors. T-5224 inhibits the IL-1β-induced up-regulation of Mmp-3, Mmp-13 and Adamts-5 transcription.

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

T-5224 Chemical Structure

T-5224 Chemical Structure

CAS No. : 530141-72-1

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 137 In-stock
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10 mg USD 180 In-stock
50 mg USD 540 In-stock
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Customer Review

Based on 62 publication(s) in Google Scholar

T-5224 Related Antibodies

Top Publications Citing Use of Products

60 Publications Citing Use of MCE T-5224

WB

    T-5224 purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2018 Sep;155:275-287.  [Abstract]

    Twist1, nuclear NF-κB-p65 and secreted TNF-α in macrophages after transfection with Twist1 siRNA (100 pmol/well) for 48 h and then treatment with LPS, TT-TFM (200 μM) and T5224 (50 μM) for another 24 h.

    T-5224 purchased from MedChemExpress. Usage Cited in: Endocrinology. 2017 Nov 1;158(11):4064-4075.  [Abstract]

    Cyp27b1 induction by LPS or TNF-α is mediated by NF-κB. HCT116 cells are treated with 100 ng/mL LPS or 100 ng/mL TNF-α overnight in the presence or absence of 20 ng/mL T-5224 as indicated. Cyp27b1 protein levels are measured by Western blotting.

    View All AP-1 Isoform Specific Products:

    View All Isoforms
    c-Fos c-Jun

    View All MMP Isoform Specific Products:

    View All Isoforms
    MMP-1 MMP-2 MMP-3 MMP-8 MMP-9 MMP-13 MMP-14 MMP-17 ADAM10 ADAM17 MMP-7 MMP-12 MMP-10 MMP ADAM8

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    T-5224 is a transcription factor c-Fos/activator protein (AP)-1 inhibitor with anti-inflammatory effects, which specifically inhibits the DNA binding activity of c-Fos/c-Jun without affecting other transcription factors. T-5224 inhibits the IL-1β-induced up-regulation of Mmp-3, Mmp-13 and Adamts-5 transcription[1][2].

    IC50 & Target

    c-Fos

     

    Cellular Effect
    Cell Line Type Value Description References
    NIH3T3 IC50
    10 μM
    Compound: 51
    Inhibition of AP-1 (unknown origin) expressed in TPA-stimulated mouse NIH3T3 cells by luciferase reporter gene assay
    Inhibition of AP-1 (unknown origin) expressed in TPA-stimulated mouse NIH3T3 cells by luciferase reporter gene assay
    		[PMID: 24831826]
    In Vitro

    T-5224 inhibits in-vitro production of the mediators MMP-1, MMP-3, IL-6 and TNF-α by IL-1β-stimulated human synovial SW982 cells with the mean IC50 of about 10 μM[2].
    T-5224 (0-80 μM) significantly inhibits the invasion, migration, and MMP activity of HSC-3-M3 cells in a dose-dependent manner[3].

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

    T-5224 Related Antibodies
    In Vivo

    Administration of T-5224 (300 mg/kg, p.o.) after intraperitoneal injection of LPS impartes appreciable protection against acute elevations in serum levels of TNFα, HMGB1, ALT/AST as well as in liver tissue levels of MIP-1α and MCP-1, and reduces the lethality (27%)[4].
    G2 is observed in rat and monkey liver microsomes as a major metabolite of T-5224, suggesting that G2 is not a human-specific metabolite[5].
    T-5224 (300 mg/kg, p.o.) inhibits the production of TNF-alpha and other downstream effectors in C57BL/6 mice[6].

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

    517.53

    Formula

    C29H27NO8
    CAS No.
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    OC1=NOC2=CC(COC3=C(CCC(O)=O)C=C(C(C4=C(O)C=C(OC5CCCC5)C=C4)=O)C=C3)=CC=C21
    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 (193.23 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 1.9323 mL 9.6613 mL 19.3225 mL
    5 mM 0.3865 mL 1.9323 mL 3.8645 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

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    Volume (start)

    V1

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    C2

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    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    90% (20% SBE-β-CD in Saline)

      Solubility: 5 mg/mL (9.66 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
    • Protocol 2

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

      Solubility: 5 mg/mL (9.66 mM); Clear solution; Need ultrasonic

      This protocol yields a clear solution of 5 mg/mL. 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 (50.0 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)

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    Dosing volume
    (per animal)

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    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: 99.59%

    SDS (393 KB)

    COA (250 KB) HNMR (239 KB) LCMS (90 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [4]

    HSC-3-M3 cells are starved for 24 h with DMEM containing 0.5% FBS. The top chamber of the cell invasion device is coated with 50 μL of 0.1 × basement membrane extract solution and incubataed overnight. HSC-3-M3 cells (5.0 × 104 cells/well) are added to the top chamber with DMEM containing 0.5% FBS mixed with 0-80 μM T-5224; DMEM with 10% FBS is added to the bottom chamber and incubated for 48 h. The bottom plate is read using a multilabel plate reader. The data are compared with the standard curve to determine the fraction of invaded cells.

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

    Mice in LPS group are administered orally with polyvinylpyrrolidone solution in the same volume of T-5224 solution immediately after LPS injection, while in the T-5224 group, mice are administered orally with T-5224 (300 mg/kg, p.o.) in the same manner. In the control group, mice receives polyvinylpyrrolidone solution orally soon after intraperitoneal saline injection. Blood samples are collected for each measurement at the optimal time.

    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 1.9323 mL 9.6613 mL 19.3226 mL 48.3064 mL
    5 mM 0.3865 mL 1.9323 mL 3.8645 mL 9.6613 mL
    10 mM 0.1932 mL 0.9661 mL 1.9323 mL 4.8306 mL
    15 mM 0.1288 mL 0.6441 mL 1.2882 mL 3.2204 mL
    20 mM 0.0966 mL 0.4831 mL 0.9661 mL 2.4153 mL
    25 mM 0.0773 mL 0.3865 mL 0.7729 mL 1.9323 mL
    30 mM 0.0644 mL 0.3220 mL 0.6441 mL 1.6102 mL
    40 mM 0.0483 mL 0.2415 mL 0.4831 mL 1.2077 mL
    50 mM 0.0386 mL 0.1932 mL 0.3865 mL 0.9661 mL
    60 mM 0.0322 mL 0.1610 mL 0.3220 mL 0.8051 mL
    80 mM 0.0242 mL 0.1208 mL 0.2415 mL 0.6038 mL
    100 mM 0.0193 mL 0.0966 mL 0.1932 mL 0.4831 mL
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    T-5224 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:

    T-5224530141-72-1T5224T 5224AP-1MMPActivator Protein 1Matrix metalloproteinasesInhibitorinhibitorinhibit

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