T-5224

製品コードS8966 バッチS896608

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C29H27NO8
分子量 517.53 CAS No. 530141-72-1
Solubility (25°C)* 体外 DMSO 100 mg/mL (193.22 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

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生物活性

製品説明 T-5224 is a selective inhibitor of transcription factor c-Fos/activator protein (AP)-1 with anti-inflammatory effects. T-5224 specifically inhibits the DNA binding activity of c-Fos/c-Jun and the IL-1β-induced up-regulation of Mmp-3, Mmp-13 and Adamts-5 transcription.
in vitro

T-5224 inhibits matrix-degrading MMPs and inflammatory cytokines including interleukin 1β. T-5224 reduces the amounts of inflammatory cytokines and MMPs in vitro in synovial cell and chondrocyte cultures.[1]
in vivo

T-5224 is an inhibitor of c-Fos/activator protein-1 (AP-1) that prevents type II collagen–induced arthritis by reducing the amounts of inflammatory cytokines, MMPs and anti-tumor necrosis factor α in vivo in sera and joints.[1]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 NIH/3T3, RAW264.7, human synovial sarcoma SW982 and human chondrosarcoma SW1353 cells
濃度 5.2 μM, 10 μM, 17 μM, 30 μM, 14 μM, 20 μM, 28 μM, 40 μM, 57 μM, 80 μM
反応時間 1 h
実験の流れ

Reporter assay. NIH/3T3 cells are 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 are 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.
動物実験 動物モデル Male 8-week-old DBA/1J mice
投薬量 3 mg/kg
投与方法 Oral gavage

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Dynamic regulation of tissue fluidity controls skin repair during wound healing [ Cell, 2024, S0092-8674(24)00825-0] PubMed: 39168124
Collagen signaling and matrix stiffness regulate multipotency in glandular epithelial stem cells in mice [ Nat Commun, 2024, 15(1):10482] PubMed: 39695111
Positive and negative feedback regulation of the TGF-β1 explains two equilibrium states in skin aging [ iScience, 2024, 27(5):109708] PubMed: 38706856
AP-1 Mediates Cellular Adaptation and Memory Formation During Therapy Resistance [ bioRxiv, 2024, 2024.07.25.604999] PubMed: 39091739
Shear Stress Drives the Cleavage Activation of Protease-Activated Receptor 2 by PRSS3/Mesotrypsin to Promote Invasion and Metastasis of Circulating Lung Cancer Cells [ Adv Sci (Weinh), 2023, 10(25):e2301059] PubMed: 37395651
c-FOS is an integral component of the IKZF1 transactivator complex and mediates lenalidomide resistance in multiple myeloma [ Clin Transl Med, 2023, 13(8):e1364] PubMed: 37581569
c-FOS is an integral component of the IKZF1 transactivator complex and mediates lenalidomide resistance in multiple myeloma [ Clin Transl Med, 2023, 13(8):e1364] PubMed: 37581569
Flubendazole inhibits PD-1 and suppresses melanoma growth in immunocompetent mice [ J Transl Med, 2023, 21(1):467] PubMed: 37452307
Flubendazole inhibits PD-1 and suppresses melanoma growth in immunocompetent mice [ J Transl Med, 2023, 21(1):467] PubMed: 37452307
Androgen Receptor/AP-1 Activates UGT2B15 Transcription to Promote Esophageal Squamous Cell Carcinoma Invasion [ Cancers (Basel), 2023, 15(24)5719] PubMed: 38136265

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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