1. Metabolic Enzyme/Protease
  2. MMP
  3. T-5224

T-5224 

Cat. No.: HY-12270 Purity: 99.03%
Handling Instructions

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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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 137 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 888 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 11 publication(s) in Google Scholar

Top Publications Citing Use of Products

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

    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.

    T-5224 purchased from MCE. Usage Cited in: Biochem Pharmacol. 2018 Sep;155:275-287.

    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.
    • Biological Activity

    • Protocol

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    • 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/activator protein (AP)-1[1]

    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].

    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].

    Molecular Weight

    517.53

    Formula

    C₂₉H₂₇NO₈

    CAS No.

    530141-72-1

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

    DMSO : ≥ 31 mg/mL (59.90 mM)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    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
    10 mM 0.1932 mL 0.9661 mL 1.9323 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: ≥ 2.08 mg/mL (4.02 mM); Clear solution

    • 2.

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

      Solubility: 2.08 mg/mL (4.02 mM); Suspended solution; Need ultrasonic

    • 3.

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

      Solubility: ≥ 2.08 mg/mL (4.02 mM); Clear solution

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

    Purity: 99.03%

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    Product name:
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    Cat. No.:
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