STA-21
(Synonyms: Ochromycinone) 目录号 : GC17761A STAT3 inhibitor
Cas No.:111540-00-2,28882-53-3
Sample solution is provided at 25 µL, 10mM.
IC50: 12.2 μM for DU145 cells
STA-21 is a STAT3 inhibitor.
STAT-3, a transcription factor encoded by the STAT-3 gene, exists in a latent form in the cytoplasm. STAT-3 will be phosphorylated on tyrosine residues upon receptor activation by cytokines including IL-6, and forms homo- or heterodimers translocating to the cell nucleus. STAT-3 is also the major transcription factor in Th17 cell differentiation, and STAT-3 can be activated in inflamed synovium, which has been demonstrated in a RA animal model.
In vitro: Previous in vitro study showed that, in both mouse and human CD4+ T cells, the treatment with STA-21 could induce the expression of FoxP3 and repressed IL-17 expression. In addition, STA-21 was able to prevent both human monocytes and mouse BMM cells from differentiating into osteoclasts [1].
In vivo: In previous animal study, IL-1Ra-KO mice were treated with i.p. injections of STA-21 at 0.5 mg/kg 3 times per week for 3 weeks. Results showed that STA-21 could suppress inflammatory arthritis in IL-1Ra-KO mice. The Th17 cell proportion decreased and the proportion of Treg cells expressing FoxP3 was increased in the spleens of STA-21-treated mice markedly. Moreover, the adoptive transfer of CD4+CD25+ T cells from STA-21-treated IL-1Ra-KO mice suppressed inflammatory arthritis markedly [1].
Clinical trial: The topical efficacy of STA-21on psoriasis has been conducted at 2010, however, this study has been completed [https://clinicaltrials.gov/ct2/show/NCT01047943].
Reference:
[1] Park JS et al. STA-21, a promising STAT-3 inhibitor that reciprocally regulates Th17 and Treg cells, inhibits osteoclastogenesis in mice and humans and alleviates autoimmune inflammation in an experimental model of rheumatoid arthritis. Arthritis Rheumatol.2014 Apr;66(4):918-29.
Cas No. | 111540-00-2,28882-53-3 | SDF | |
别名 | Ochromycinone | ||
化学名 | 8-hydroxy-3-methyl-3,4-dihydrotetraphene-1,7,12(2H)-trione | ||
Canonical SMILES | O=C1CC(C)CC(C1=C2C3=O)=CC=C2C(C4=C3C=CC=C4O)=O | ||
分子式 | C19H14O4 | 分子量 | 306.31 |
溶解度 | DMF: 25 mg/ml,DMF:PBS(pH7.2) (1:2): 0.3 mg/ml,DMSO: 16 mg/ml | 储存条件 | Store at -20°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 3.2647 mL | 16.3233 mL | 32.6467 mL |
5 mM | 0.6529 mL | 3.2647 mL | 6.5293 mL |
10 mM | 0.3265 mL | 1.6323 mL | 3.2647 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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- Purity: >98.00%
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