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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。

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T-5224, CAS 530141-72-1

规格	价格/CNY	货期
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

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选择批次

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

相关产品

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	IL-1b刺激下的人类滑膜SW982细胞产生滑膜细胞介质MMP-1、MMP-3、IL-6和TNFα的体外生产，以及IL-1b刺激下的人类软骨细胞SW1353细胞产生软骨炎症介质MMP-3和MMP-13，均被T-5224所抑制。大多数细胞实验的IC50值约为10μM [1]。加压素选择性地刺激CDS1 mRNA的增加，这一过程依赖于蛋白激酶C，并可被AP-1抑制剂T-5224所抑制 [3]。T-5224显著以剂量依赖的方式抑制HNSCC细胞的侵袭、迁移和MMP活性；而对细胞增殖没有显著影响 [4]。
体内活性	T-5224通过每日一次从第21天开始使用，有效抑制了胶原蛋白诱导的关节炎(CIA)的发展，在第50天时，3 mg/kg和30 mg/kg剂量的T-5224分别抑制了关节炎的发展64%和91%。接受T-5224治疗的小鼠体重稳定恢复。X光研究显示，接受治疗的关节破坏得到了抑制，未经治疗的关节炎对照组则没有这种现象，特别是，30 mg/kg的T-5224完全保护了关节不受破坏[1]。在腹腔注射LPS后，口服给予T-5224 (300 mg/kg)能显著保护，对抗急性血清TNFα、HMGB1、ALT/AST水平的升高以及肝组织中MIP-1α和MCP-1的水平，减少了致死率(27%)[2]。T-5224 (150 mg/kg)或安慰剂每日口服4周。在模型中，接受T-5224治疗组的颈淋巴结转移率为40.0%，而安慰剂治疗组为74.1%[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

计算器

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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.

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

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

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。

第一步：请输入动物实验的基本信息

剂量

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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