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• 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.

• 靶点： MMP

• 体外研究：
  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. 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. 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.

• 体内研究：
  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. 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 %). 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.

• 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.

• 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 unilate

• 参考文献：
  1. 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. 2. 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. 3. 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. 4. 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.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.932 ml	9.661 ml	19.323 ml
  5 mM	0.386 ml	1.932 ml	3.865 ml
  10 mM	0.193 ml	0.966 ml	1.932 ml
  50 mM	0.039 ml	0.193 ml	0.386 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *