|(1E,6E)-1,7-双(3,4-二甲氧基苯基)-4,4-二甲基庚-1,6-二烯-3,5-二酮|CsnPharm

CAS No.: 52328-97-9

四甲基姜黄素 Catalog No. CSN32598

Synonyms: FLLL31;四甲基姜黄素

Apoptosis Inducers, STAT3 Inhibitors, Signal Transduction Modulators

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400-920-2911

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技术信息

生物活性

描述As a point of convergence for numerous oncogenic signaling pathways, signal transducer and activator of transcription 3 (STAT3) is central in regulating the anti-tumor immune response. STAT3 is broadly hyperactivated both in cancer and non-cancerous cells within the tumor ecosystem and plays important roles in inhibiting the expression of crucial immune activation regulators and promoting the production of immunosuppressive factors^[1]. STAT3 is widely expressed and located in the cytoplasm in an inactive form. STAT3 is rapidly and transiently activated by tyrosine phosphorylation by a range of signalling pathways, including cytokines from the IL-6 family and growth factors, such as EGF and PDGF. STAT3 activation and subsequent dimer formation initiates nuclear translocation of STAT3 for the regulation of target gene transcription^[2].Tetramethylcurcumin (FLLL31), derived from curcumin, specifically suppresses the phosphorylation of STAT3 by binding selectively to Janus kinase 2 and the STAT3 Src homology-2 domain. Tetramethylcurcumin exhibits anti-inflammatory and anti-cancer effects^[3]. Tetramethylcurcumin (FLLL31; 2.5 and 5 µM; for 24 hours) downregulats STAT3 phosphorylation and DNA-binding activity in MDA-MB-231 breast and PANC-1 pancreatic cancer cells. Tetramethylcurcumin inhibits cell viability, cell invasion. Tetramethylcurcumin is a effective inhibitor of STAT3 phosphorylation, DNA-binding activity, and transactivation in vitro, leading to the impediment of multiple oncogenic processes and the induction of apoptosis in pancreatic and breast cancer cell lines^[3].
参考文献

[1] Sailan Zou,et al. Targeting STAT3 in Cancer Immunotherapy. Mol Cancer. 2020 Sep 24;19(1):145.
[2] Yun Liu,et al. STAT3 and its targeting inhibitors in osteosarcoma. Cell Prolif. 2021 Feb;54(2):e12974.
[3] Lin L, et al. Novel STAT3 phosphorylation inhibitors exhibit potent growth-suppressive activity in pancreatic and breast cancer cells. Cancer Res. 2010 Mar 15;70(6):2445-54.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.3558 mL
- 11.7789 mL
- 23.5579 mL
- 5 mM
- 0.4712 mL
- 2.3558 mL
- 4.7116 mL
- 10 mM
- 0.2356 mL
- 1.1779 mL
- 2.3558 mL

技术信息

CAS号	52328-97-9	储存条件	粉末 Sealed in dry,2-8°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C25H28O6	运输	蓝冰
分子量	424.49	别名	FLLL31;四甲基姜黄素

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