Name: T-5224
Brand: GlpBio
SKU: GC16165
Availability: InStock
Rating: 5 (12 reviews)

Product has been cited by 2 publications

Related Biological Data

Knockdown of AP-1 subunits caused the downregulation of TGFB1. (G) The effects of blocking the NF-κB and AP-1 signaling pathways on the expression of TGFB1.
Cells were treated with two NF-κB inhibitors, TPCA1, and BOT-64, and two AP-1 inhibitors, T-5224 (50µM, GLPBIO, Montclair, CA, USA, #GC16165) and SR11302 for 4h and then stimulated with 50ng/mL recombinant IL-1β for 2h.
Int J Biol Sci 16.2 (2020): 204. PMID: 31929749 IF: 6.58
Related Biological Data

EML4-ALK fusion protein regulates TF expression through pERK1/2/AP-1 pathway in H2228 cells. (C1-4) Pretreating H2228 cells with AP-1 inhibitor (T-5224, 400μm/L) also attenuated TF expression compared with DMSO control both at RNA (n=6) and protein level (n=3). Data are presented as means±SEM.
H2228 cells were Pretreated with T-5224 (GLPBIO, USA, 400μm/L).
J Thromb Thrombolys, 2023: 1-15. PMID: 37940761 IF: 4

Product Documents

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Purity: >98.00%

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 [1]:
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.

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.

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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Product has been cited by 2 publications

Related Biological Data