STA-21 Catalog No.GC17761 |
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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Purity = 98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
Cas No. | 111540-00-2, 28882-53-3 | SDF | |
Synonyms | N/A | ||
Chemical Name | 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 | ||
Formula | C19H14O4 | M.Wt | 306.31 |
Solubility | Soluble in DMSO | Storage | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
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.