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Ochromycinone

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Chemical Structure| 111540-00-2 同义名 : Sta-21;(Rac)-STA-21;NSC 628869.
CAS号 : 111540-00-2
货号 : A481314
分子式 : C19H14O4
纯度 : 98%
分子量 : 306.31
MDL号 : MFCD16883374
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 16 mg/mL(52.23 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • STAT3
描述 Signal transducer and activator of transcription (STAT) 3 is a key signalling protein engaged by a multitude of growth factors and cytokines to elicit diverse biological outcomes including cellular growth, differentiation, and survival[3].Ochromycinone ((Rac)-STA-21) is a natural antibiotic and a STAT3 inhibitor. Ochromycinone can inhibits STAT3 DNA binding activity, STAT3 dimerization. Ochromycinone has anticancer and antimicrobial activity[4].STA-21 inhibits STAT3 DNA binding activity, STAT3 dimerization, and STAT3-dependent luciferase activity. Moreover, STA-21 reduces the survival of breast carcinoma cells with constitutive STAT3 signaling but has minimal effect on the cells in which constitutive STAT3 signaling is absent[5]. STA-21 enhanced the clinical course of arthritis in CAIA mice and decreased CD8+RORγt+ and CD8+IL-21+ cells while inducing the production of CD8+Foxp3+ cells. Furthermore, STA-21 prevented the production of TNF-α and IL-6 in peripheral blood and increased IL-27 production by CD14+ cells. Moreover, STA-21 not only regulates Th1/Th2 serum cytokine levels but also the mRNA and protein expression of key factors including NF-κB p65, RORγt, T-bet, IL-4, GATA-3, JAK1, Stat3, and IL-21[6].STA-21 suppressed inflammatory arthritis in IL-1Ra-KO mice. The proportion of Th17 cells was decreased and the proportion of Treg cells expressing FoxP3 was markedly increased in the spleens of STA-21-treated mice. Adoptive transfer of CD4+CD25+ T cells obtained from STA-21-treated IL-1Ra-KO mice markedly suppressed inflammatory arthritis. In vitro treatment with STA-21 induced the expression of FoxP3 and repressed IL-17 expression in both mouse and human CD4+ T cells. Moreover, STA-21 prevented both mouse BMM cells and human monocytes from differentiating into osteoclasts in vitro[7].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.26mL

0.65mL

0.33mL

16.32mL

3.26mL

1.63mL

32.65mL

6.53mL

3.26mL
参考文献

[1]Chen CL, Loy A, et al. Signal transducer and activator of transcription 3 is involved in cell growth and survival of human rhabdomyosarcoma and osteosarcoma cells. BMC Cancer.

[2]Song H, Wang R, et al. A low-molecular-weight compound discovered through virtual database screening inhibits Stat3 function in breast cancer cells. Proc Natl Acad Sci U S A. 2005 Mar 29;102(13):4700-5.

[3] Aleks C Guanizo,et al. STAT3: a multifaceted oncoprotein. Growth Factors. 2018 Apr;36(1-2):1-14.

[4] Song H, et al. A low-molecular-weight compound discovered through virtual database screening inhibits Stat3 function in breast cancer cells. Proc Natl Acad Sci U S A. 2005 Mar 29;102(13):4700-5.

[5] Nataliya I. Kalinovskaya, et al. New Angucyclinones from the Marine Mollusk Associated Actinomycete Saccharothrix espanaensis An 113. Natural product communications. 2008, 3(10):1611-1616.

[6] Sheikh Fayaz Ahmad,et al. STA-21, a STAT-3 inhibitor, attenuates the development and progression of inflammation in collagen antibody-induced arthritis. Immunobiology. 2017 Feb;222(2):206-217.

[7]Jin-Sil Park,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.