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规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1mL(10 mM in DMSO) | ¥500.00 | 现货 | |
25mg | ¥727.00 | 现货 | |
100mg | ¥1818.00 | 现货 |
特色产品
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- 可将信号灵敏度提高100倍
- 同时保持稳定的特异性和分辨率
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- 提供更高的转录效率并抑制免疫激活
- 使用5-moUTP和Cy5-utp修饰
产品描述
Stattic是STAT3的小分子抑制剂,在UM-SCC-17B、OSC-19、Cal33和UM-SCC-22B细胞系中的IC50值分别为2.562±0.409 μM、3.481±0.953 μM、2.282±0.423 μM和2.648±0.542 μM[1]。
据报道,stattic选择性抑制STAT3的二聚化、激活和核易位。Stattic也诱导STAT3依赖性乳腺癌细胞系的细胞凋亡[2]。
Stattic对STAT3的抑制导致STAT3介导的HIF-1表达的减少,及随后头颈部鳞状细胞癌(HNSCC)细胞的放射增敏作用。抑制STAT3信号通路可能代表了一种有效的用于治疗HNSCC的策略。Stattic在体内的活性也被发现。Stattic预处理可增加原位异种移植HNSCC肿瘤的放射增敏作用,显著减少肿瘤生长,尽管该效果不如体外研究预期的那么显著[1]。
参考文献:
[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.
产品性质
物理外观 | A solid |
CAS号 | 19983-44-9 |
分子式 | C8H5NO4S |
分子量 | 211.19 |
化学名称 | 6-nitro-1-benzothiophene 1,1-dioxide |
溶解度 | insoluble in H2O; insoluble in EtOH; ≥10.56 mg/mL in DMSO |
SMILES | C1=CC(=CC2=C1C=CS2(=O)=O)[N+](=O)[O-] |
存储条件 | -20°C |
运输条件 | 蓝冰 |
SDF文件 | Download SDF |
产品应用 (实验数据来自文献,APExBIO并未验证,仅供参考)
IC50和靶点
生物活性描述 | Stattic是STAT3的小分子抑制剂,在UM-SCC-17B、OSC-19、Cal33和UM-SCC-22B细胞系中的IC50值分别为2.562±0.409 μM、3.481±0.953 μM、2.282±0.423 μM和2.648±0.542 μM。 | |||
靶点 | STAT3 | STAT3 | STAT3 | STAT3 |
生物活性数据 | 2.562 ± 0.409 μM (UM-SCC-17B cell line) | 3.481 ± 0.953 μM (OSC-19 cell line) | 2.282 ± 0.423 μM (Cal33 cell line) | 2.648 ± 0.542 μM (UM-SCC-22B cell line) |
生物相关数据
质量控制
操作说明
产品引用文献
- 1. Junli Wang, Sijia Weng, et al. "PKCι induces differential phosphorylation of STAT3 to modify STAT3-related signaling pathways in pancreatic cancer cells." J Cell Commun Signal. 2023 Aug 7. PMID: 37548811
- 2. Jiang Li, Hong Huang, et al. "Complement factor H inhibits endothelial cell migration through suppression of STAT3 signaling." Exp Ther Med. 2023 Jul 10;26(2):408. PMID: 37522066
- 3. 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
- 4. 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
- 5. 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
- 6. 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
- 7. Linnan Yang, Jing Sun, et al. "Synergetic Functional Nanocomposites Enhance Immunotherapy in Solid Tumors by Remodeling the Immunoenvironment." Advanced Science. 16 February 2019.
- 8. 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
- 9. 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
- 10. 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
- 11. 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.