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T-5224

T-5224

产品编号 T5416   CAS 530141-72-1

T-5224 是选择性的转录因子c-Fos/activator protein (AP)-1抑制剂,具有抗炎作用,能够特异性抑制 c-Fos/c-Jun 的 DNA 结合活性,但对其他转录因子的结合活性无影响。它抑制 IL-1β 诱导的 Mmp-3、Mmp-13、Adamts-5 转录上调。

TargetMol的所有产品仅用作科学研究或药证申报,不能被用于人体,我们不向个人提供产品和服务。请您遵守承诺用途,不得违反法律法规规定用于任何其他用途。
T-5224 Chemical Structure
T-5224, CAS 530141-72-1
规格 价格/CNY 货期 数量
1 mg ¥ 378 现货
2 mg ¥ 548 现货
5 mg ¥ 888 现货
10 mg ¥ 1,330 现货
25 mg ¥ 2,250 现货
50 mg ¥ 3,280 现货
100 mg ¥ 4,890 现货
500 mg ¥ 9,870 现货
1 mL * 10 mM (in DMSO) ¥ 987 现货
药物设计专题培训
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
产品目录号及名称: T-5224 (T5416)
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纯度: 99.29%
纯度: 98.01%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 T-5224 is a transcription factor c-Fos/AP-1 inhibitor, which specifically inhibits the DNA binding activity of c-Fos/c-Jun without affecting other transcription factors.
体外活性 In vitro production of the synovial cell mediators MMP-1, MMP-3, IL-6 and TNFα by IL-1b–stimulated human synovial SW982 cells was inhibited by T-5224. This was also the case for the chondrocyte inflammatory mediators MMP-3 and MMP-13 in IL-1b–stimulated human chondrocyte SW1353 cells. The IC50 values were ~10 μM for most of the cellular assays [1]. Vasopressin selectively stimulates an increase CDS1 mRNA that is dependent on protein kinase C and can be inhibited by the AP-1 inhibitor, T-5224 [3]. T-5224 significantly inhibited the invasion, migration, and MMP activity of HNSCC cells in a dose-dependent manner; there was no significant influence on cell proliferation [4].
体内活性 T-5224 efficiently inhibited the development of collagen-induced arthritis (CIA) when administered once daily from day 21, before the onset of arthritis. Arthritis on day 50 was inhibited by 64% and 91%, by 3 and 30 mg/kg of T-5224, respectively. The body weight of mice treated with T-5224 steadily recovered. X-ray studies showed that joint destruction was inhibited in treated but not in untreated arthritis controls, and notably, the joint was totally protected from destruction by 30 mg/kg of T-5224 [1]. Administration of T-5224 (300 mg/kg, p.o.) after intraperitoneal injection of LPS imparted 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 reduced the lethality (27 %) [2]. T-5224 (150 mg/kg) or vehicle was given orally every day for 4 weeks. The rate of cervical lymph node metastasis in the model was 40.0% in the T-5224-treated group versus 74.1% in the vehicle-treated group [4].
激酶实验 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].
细胞实验 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].
动物实验 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].
分子量 517.53
分子式 C29H27NO8
CAS No. 530141-72-1

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: Insoluble

DMSO: 16.67 mg/mL (32.2 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9323 mL 9.6613 mL 19.3226 mL 48.3064 mL
5 mM 0.3865 mL 1.9323 mL 3.8645 mL 9.6613 mL
10 mM 0.1932 mL 0.9661 mL 1.9323 mL 4.8306 mL
20 mM 0.0966 mL 0.4831 mL 0.9661 mL 2.4153 mL

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TargetMol Library Books参考文献

1. Aikawa Y, et al. Treatment of arthritis with a selective inhibitor of c-Fos/activator protein-1. Nat Biotechnol. 2008 Jul;26(7):817-23. 2. Izuta S, et al. T-5224, a selective inhibitor of c-Fos/activator protein-1, attenuates lipopolysaccharide-induced liver injury in mice. Biotechnol Lett. 2012 Dec;34(12):2175-82. 3. Blunsom NJ, et al. Sustained phospholipase C stimulation of H9c2 cardiomyoblasts by vasopressin induces an increase in CDP-diacylglycerol synthase 1 (CDS1) through protein kinase C and cFos. Biochim Biophys Acta Mol Cell Biol Lipids. 2019 Jul;1864(7):1072-1082. 4. Kamide D, et al. Selective activator protein-1 inhibitor T-5224 prevents lymph node metastasis in an oral cancer model. Cancer Sci. 2016 May;107(5):666-73.

TargetMol Library Books文献引用

1. Wang X, Li K, Cheng M, et al.RNPS1 stabilizes NAT10 protein to facilitate translation in cancer via tRNA ac4C modification.bioRxiv.2023: 2023.02. 11.528122. 2. Zhang Q, Hui M, Chen G, et al.Curcumin-Piperlongumine Hybrid Molecule Increases Cell Cycle Arrest and Apoptosis in Lung Cancer through JNK/c-Jun Signaling Pathway.Journal of Agricultural and Food Chemistry.2024
α-Solanine Stigmasterol 2,3-Dihydrohinokiflavone Morroniside BPHA Epitheaflagallin 3-O-gallate Isofraxidin Chondroitin sulfate

相关化合物库

该产品包含在如下化合物库中:
抑制剂库 血管生成库 蛋白酶抑制剂库 ReFRAME 相关化合物库 抗纤维化化合物库 NO PAINS 化合物库 转录因子库 抗COVID-19化合物库 经典已知活性库 已知活性化合物库

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体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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Keywords

T-5224 530141-72-1 Proteases/Proteasome MMP Activator Protein 1 Inhibitor inhibit Matrix metalloproteinases T 5224 AP-1 T5224 inhibitor

 

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