同义名 :	FLLL31
	CAS号 :	52328-97-9
	货号 :	A987384
	分子式 :	C25H28O6
	纯度 :	95%
	分子量 :	424.49
	MDL号 :	MFCD19443859
	存储条件：	Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	动物实验配方：

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].

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	2.36mL 0.47mL 0.24mL	11.78mL 2.36mL 1.18mL	23.56mL 4.71mL 2.36mL

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.