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T-5224

Catalog No.GC16165

T-5224 is a non-peptidic small molecule AP-1 inhibitor

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T-5224 Chemical Structure

Cas No.: 530141-72-1

Size Price Stock Qty
10mM (in 1mL DMSO)
$83.00
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5mg
$73.00
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10mg
$115.00
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50mg
$343.00
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100mg
$577.00
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500mg
$1,236.00
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Sample solution is provided at 25 µL, 10mM.

Product has been cited by 2 publications

Product Documents

Quality Control & SDS

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Protocol

Cell experiment [1]:

Cell lines

Human oral squamous carcinoma cell lines, OSC-19 and HSC-3-M3.

Preparation Method

Cells were grown in DMEM supplemented with 10% FBS and penicillin (50 units ⁄ mL) ⁄ streptomycin (50 μg ⁄ mL) in a humidified atmosphere (5% CO2) at 37°C. T-5224 was dissolved in DMSO and diluted in culture medium to the target concentration for each experiment. For oral gavage administration, T-5224 was dissolved in polyvinylpyrrolidone (PVP) solution according to the manufacturer’s recommended procedure.

Reaction Conditions

Cells were incubated in T-5224 (0–80 μM), and cell counts were carried out at 24, 48, and 72 h after treatment.

Applications

T-5224 treatment could inhibit the invasion activity of highly metastatic tumor cell line HSC-3-M3. Cell migration was potently inhibited by T-5224 in both cell lines in a dose-dependent manner. Migration activity was almost completely inhibited in the medium containing 80 μM T-5224.

Animal experiment [2]:

Animal models

Female 5–7-week-old BALB⁄ c mice

Preparation Method

HSC-3-M3 (1 x 105 cells) were suspended in 50 μL Hank’s Balanced Salts Solution and injected in the flank of the tongue at day 0. T-5224 was diluted in PVP solution, and T-5224 was given orally to the mice of the treatment group every day from day 1 for 4 weeks.

Dosage form

150 mg⁄ kg

Applications

T-5224 showed significant inhibitory effects against lymph node metastasis in the animal model of HNSCC. The rate of positive metastasis was significantly lower by T-5224 treatment. It is possible that higher doses (150 mg/kg) might be required for cells in which activity of AP-1 is intensively and constitutively activated by genetic mutations or substantial inflammation.

References:

[1]. Daisuke K. et al. Selective activator protein-1 inhibitor T-5224 prevents lymph node metastasis in an oral cancer model. Cancer Sci. 2016 May; 107 (5) 666–673.

Background

T-5224 is a non-peptidic small molecule AP-1 inhibitor that specifically inhibits the binding of AP-1 to the AP-1 binding site of the promoter region and was originally developed as an anti-inflammatory drug for the treatment of rheumatoid arthritis (RA) suppressing inflammatory cytokines and MMPs without any side-effects.[1]

In vitro study indicated that transcriptional inhibition of the expression of MMPs by T-5224 is not limited to tumor cells only; it also occurs in the ECM of the surrounding tissue, and consequently, inhibits tumor cells from infiltrating the surrounding tissue. In addition, T-5224 potently inhibits the essential steps of metastasis, infiltration through the basement membrane barrier and migration into the ECM, by transcriptionally suppressing the expression of MMP-2 and -9.[1]

In vivo experiments demonstrated that T-5224 blocked serum TNF-α, HMGB-1, BUN, and creatinine concentrations, reducing mortality of LPS-induced AKI. These findings suggest that T-5224 may be protective against lethal LPS-induced AKI. T-5224 attenuated LPS-induced liver injury in mice. T-5224 may have beneficial effects in sepsis-induced organ dysfunctions. [3]

References:
[1]. Daisuke K. et al. Selective activator protein-1 inhibitor T-5224 prevents lymph node metastasis in an oral cancer model. Cancer Sci. 2016 May; 107 (5) 666–673.
[2]. Mari I. et al. T-5224, a selective inhibitor of c-Fos/activator protein-1, improves survival by inhibiting serum high mobility group box-1 in lethal lipopolysaccharide-induced acute kidney injury model. Journal of Intensive Care (2015) 3:49.

Chemical Properties

Cas No. 530141-72-1 SDF
Chemical Name 3-(5-(4-(cyclopentyloxy)-2-hydroxybenzoyl)-2-((3-oxo-2,3-dihydrobenzo[d]isoxazol-6-yl)methoxy)phenyl)propanoic acid
Canonical SMILES O=C1NOC2=CC(COC(C=CC(C(C3=C(O)C=C(OC4CCCC4)C=C3)=O)=C5)=C5CCC(O)=O)=CC=C12
Formula C29H27NO8 M.Wt 517.53
Solubility ≥ 25.88mg/mL in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 1.9323 mL 9.6613 mL 19.3226 mL
5 mM 0.3865 mL 1.9323 mL 3.8645 mL
10 mM 0.1932 mL 0.9661 mL 1.9323 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 12 reference(s) in Google Scholar.)

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