Stattic

- Overview
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    Background
    
    Stattic is a small molecule inhibitor of STAT3 with IC50 values of 2.562 ± 0.409 μM, 3.481 ± 0.953 μM, 2.282 ± 0.423 μM and 2.648 ± 0.542 μM, respectively, in UM-SCC-17B, OSC-19, Cal33 and UM-SCC-22B cell lines [1].
    Stattic is reported to selectively inhibit dimerization, activation and nuclear translocation of STAT3. It can also induce the apoptosis of STAT3-dependent breast cancer cell lines [2].
    The inhibition of STAT3 by Stattic results in decreased STAT3-mediated HIF-1 expression and subsequent radiosensitization of HNSCC cells. Inhibiting the STAT3 signaling pathway may represent an effective strategy in the treatment of HNSCC. The evidence of Stattic activity in vivo has also been found. Stattic pre-treatment sensitizes orthotopic xenograft HNSCC tumors to radiation, wich results in signiﬁcantly reduced tumor growth, although this effect was not as dramatic as anticipated by the in vitro studies [1].
    
    [1] Makoto Adachi, Caixia Cui, Cristina T. Dodge, Mihir K. Bhayani, Stephen Y. Lai. Targeting STAT3 inhibits growth and enhances radiosensitivity in head and neck squamous cell carcinoma. Oral Oncology. 2012 July(48):1220-1226.
    [2] Jochen Schust, Bianca Sperl, Angela Hollis, Thomas U. Mayer, and Thorsten Berg. Stattic: A Small-Molecule Inhibitor of STAT3 Activation and Dimerization. Chemistry & Biology. 2006(13):1235-1242.
- Properties
  - Alternative Name
    
    6-nitro-1-benzothiophene 1,1-dioxide
    
    CAS Number
    
    19983-44-9
    
    Molecular Formula
    
    C8H5NO4S
    
    Molecular Weight
    
    211.19
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in H2O; insoluble in EtOH; ≥10.56 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Weibo Zhong, Kaihui Wu, et al. "Gut dysbiosis promotes prostate cancer progression and docetaxel resistance via activating NF-κB-IL6-STAT3 axis." Microbiome. 2022 Jun 16;10(1):94. PMID: 35710492
    2. Ying Zhang, Cong Liu, et al. "IL-22 promotes tumor growth of breast cancer cells in mice." Aging (Albany NY). 2020 Jul 15; 12(13): 13354–13364. PMID: 32649314
    3. Li L, Shang L, et al. "Janus kinase inhibitor ruxolitinib blocks thymic regeneration after acute thymus injury." Biochem Pharmacol. 2019 Nov 11:113712. PMID: 31726048
    4. Zhang Q, Liu RX, et al. "Exosomal transfer of p-STAT3 promotes acquired 5-FU resistance in colorectal cancer cells." J Exp Clin Cancer Res. 2019 Jul 19;38(1):320. PMID: 31324203
    5. Linnan Yang, Jing Sun, et al. "Synergetic Functional Nanocomposites Enhance Immunotherapy in Solid Tumors by Remodeling the Immunoenvironment." Advanced Science. 16 February 2019.
    6. Lee YC, Wang LJ, et al. "ABT-263-induced MCL1 upregulation depends on autophagy-mediated 4EBP1 downregulation in human leukemia cells." Cancer Lett. 2018 Jun 15;432:191-204. PMID: 29913235
    7. Kim W, Khan SK, et al. "Hippo signaling interactions with Wnt/β-catenin and Notch signaling repress liver tumorigenesis." J Clin Invest. 2017 Jan 3;127(1):137-152. PMID: 27869648
    8. Furtek SL, Matheson CJ, et al. "Evaluation of quantitative assays for the identification of direct signal transducer and activator of transcription 3 (STAT3) inhibitors." Oncotarget. 2016 Nov 22;7(47):77998-78008. PMID: 27793003
    9. Syn Kok Yeo, Jian Wen, et al. "Autophagy differentially regulates distinct breast cancer stem-like cells in murine models via EGFR/Stat3 and Tgfß/Smad signaling." Published OnlineFirst April 13, 2016.

Stattic

Background

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