Cas No.: | 52328-97-9 |
Chemical Name: | Tetramethylcurcumin |
Synonyms: | Tetramethylcurcumin;(1E,6E)-1,7-bis(3,4-dimethoxyphenyl)-4,4-dimethylhepta-1,6-diene-3,5-dione;(E,E)-1,7-Bis(3,4-dimethoxyphenyl)-4,4-dimethyl-1,6-heptadiene-3,5-dione;FLLL31;(1E,6E)-1,7-Bis(3,4-dimethoxyphenyl)-4,4-dimethyl-1,6-heptadiene-3,5-dione |
SMILES: | CC1C(/C=C/C(CC(/C=C/C2C=C(OC)C(O)=CC=2)=O)=O)=CC=C(O)C=1OC(C)(C)C |
Formula: | C25H28O6 |
M.Wt: | 424.48622 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | FLLL31 selectively binds to Janus kinase 2 and the STAT3 Src homology-2 (SH2) domain, effective inhibitors of STAT3 phosphorylation. STAT3 plays a critical role in early embryogenesis, but is largely dispensable in normal adult cells and tissues. On the other hand the JAK2/STAT3 signaling pathway is persistently activated in great number of human solid and blood cancers. Such activation is commonly associated with a worse prognosis. FLLL31 is a curcumin derivative locked in diketone-tautomeric form, which supposedly improves binding to SH2 domain. The compound inhibits JAK2 kinase activity and prevents STAT3 phosphorylation. FLLK31 is a potent and selective inhibitor of the STAT3 signaling pathway. |
Target: | STAT3 |
In Vitro: | 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[1]. 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[1]. |
References: | [1]. 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. [2]. Yuan S, et al. FLLL31, a derivative of curcumin, attenuates airway inflammation in a multi-allergen challenged mouse model. Int Immunopharmacol. 2014 Jul;21(1):128-36. |