T-5224 NEW
| Price | $41 | $97 | $147 |
| Package | 1mg | 5mg | 10mg |
| Supply Ability: | 10g |
| Update Time: | 2026-05-15 |
Product Details
| Product Name: T-5224 | CAS No.: 530141-72-1 |
| Purity: 99.15% | Supply Ability: 10g |
| Release date: 2026/05/15 |
Product Introduction
Bioactivity
| Name | T-5224 |
| Description | T-5224 is a selective inhibitor of the transcription factor c-Fos/activator protein (AP)-1 with anti-inflammatory effects. T-5224 specifically suppresses the DNA-binding activity of c-Fos/c-Jun, thereby inhibiting IL-1β-induced transcriptional upregulation of Mmp-3, Mmp-13, and Adamts-5, without affecting the binding activity of other transcription factors. T-5224 can be used in research on rheumatoid arthritis, osteoarthritis, and cartilage degeneration. |
| Cell Research | NIH/3T3 cells were transiently transfected with the luciferase reporter plasmids pAP-1-Luc (× 7 TGACTAA), pNF-kB-Luc (× 5 TGGGGACTTTCCGC) or control phRL-TK, and cultured overnight. Cells were incubated in 0.5% FBS/DMEM containing T-5224 for 1 h, and then stimulated with PMA (10 ng/ml) or TNFa (10 ng/ml), and then cultured for 3 h, followed by measurement of lysate by using dual-luciferase reporter assay system [1]. |
| Kinase Assay | The DNA binding activity of transcription factors was measured using the TransAM kits. Nuclear extracts containing factors such as c-Fos/AP-1, c-Jun/AP-1, ATF-2, C/EBPa, MyoD, Sp-1 or NF-kB/p65 and various concentrations of T-5224 were added in the multi-well plates precoated with respective consensus double-stranded (ds)DNA oligomers. After incubation for 1 h, the transcription factor bound to its respective consensus dsDNA sequences was detected by using antibodies reactive against the respective transcription factors according to the manufacturer's protocol [1]. |
| Animal Research | Mice were housed in an SPF (specific pathogen-free) grade environment and provided food and water ad libitum with a 12 h:12 h light/dark cycle. Male 8-week-old DBA/1J mice were immunized with bovine type II collagen emulsified in Freund's complete adjuvant on days 0 and 21. T-5224, MTX and LEF were orally administered once per day. Arthritis was assessed in a blind fashion for four paws per mouse using the following score: 0, uninvolved; 1, swelling of ≤2 toes or slight swelling in ankles and wrists; 2, swelling of ≥3 toes or moderate swelling in ankles and wrists; 3, extensive swelling of total paw. X-ray films of four paws taken using Softex were assessed for joint destruction in 2nd to 5th proximal interphalangeal joints and five metatarsophalangeal joints of four paws, the carpal joints of the forepaws, and the tarsal and calcaneal joints of the hind paws. Score was: 0, no change; 1, partial erosion; 2, complete erosion for joints; and 0, negative; 0.5, positive for osteoporosis. IL-1β (500 ng per unilateral hind paw) was administered into the footpads. The mice with ≥1 arthritis score were treated with either anti-TNFα antibody at 50 or 250 μg/mouse, intraperitoneally (i.p.) twice a week and/or with 3 mg/kg T-5224, orally once daily [1]. |
| In vitro | Methods: Human epidermal keratinocytes (NHEKs) were treated with T-5224 at concentrations ranging from 0.1 to 1 μM for 24 hours, followed by MTT assay to assess cell viability. Results: Within this concentration range, T-5224 exhibited no cytotoxicity and did not affect cell proliferation. [1] Methods: Add T-5224 at gradient concentrations (0, 20, 40, 80 μM) to HSC-3-M3 and OSC-19 cells. Measure cell migration area 24 hours after wounding. Results: T-5224 exhibited dose-dependent inhibition of migration in both cell types, with migration nearly completely suppressed at 80 μM. [2] |
| In vivo | Methods: Female BALB/c mice aged 8–10 weeks were used to establish a DNFB model. Following successful model establishment, topical application of 1% T-5224, 1% baricitinib, or 1% T-5224 + 1% baricitinib ointment was administered at 25 mg per ear, once daily for 8 days. Results: T-5224 significantly suppressed inflammation and restored Flg expression. T-5224 restored Elovl6 expression. T-5224 specifically suppressed Il17a/Il17f. [1] Methods: BALB/c nude mice were established with an orthotopic tumor model by injecting HSC-3-M3 cells (1×10?) into the tongue. T-5224 (150 mg/kg/day) was administered orally via gavage starting on day 1 post-tumor implantation, once daily for 4 consecutive weeks. Results: No significant difference in primary tumor volume was observed between groups, and T-5224 had no apparent effect on body weight. Cervical lymph node metastasis rates were 74.1% (20/27) in the control group and 40.0% (12/30) in the T-5224-treated group, representing a significant difference.[2] |
| Storage | Store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 5 mg/mL (9.66 mM), Suspension. H2O : Insoluble DMSO : 240 mg/mL (463.74 mM), Sonication is recommended. |
| Keywords | T-5224 | T5224 | T 5224 | MMP | Matrix metalloproteinases | Inhibitor | inhibit | c-Fos/AP-1 | AP-1 | Activator Protein 1 |
| Inhibitors Related | 5-Fluorouracil | Adenine hemisulfate | Rhamnose monohydrate | Doxycycline (hyclate) | Guanidine hydrochloride | Doxycycline | 1,4-Naphthoquinone | Adenine | Glucosamine | Carbazole | Thymidine | Usnic Acid |
| Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Protease Inhibitor Library | Angiogenesis related Compound Library | Inhibitor Library | NO PAINS Compound Library | Anti-Fibrosis Compound Library | Anti-Aging Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Anti-COVID-19 Compound Library | Transcription Factor-Targeted Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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- Address: 36 Washington Street, Wellesley Hill, MA
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