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STA-21 (Synonyms: Ochromycinone)

Catalog No.GC17761

A STAT3 inhibitor

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STA-21 Chemical Structure

Cas No.: 111540-00-2,28882-53-3

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$139.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

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.

Chemical Properties

Cas No. 111540-00-2,28882-53-3 SDF
Synonyms Ochromycinone
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 DMF: 25 mg/ml,DMF:PBS(pH7.2) (1:2): 0.3 mg/ml,DMSO: 16 mg/ml Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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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
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Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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