Hexamethylquercetagetin

Hexamethylquercetagetin (Hexa-O-methylquercetagetin; Quercetagetin hexamethyl ether; 3,5,6,7,3',4'-Hexamethoxyflavone) is an orally active NF-κB inhibitor. Hexamethylquercetagetin inhibits NF-κB-derived luciferase activity, reduces phosphorylated p65 and IκBα, Cyclin D1, Bcl-2 and blocks TNFα-induced NF-κB activation. Hexamethylquercetagetin inhibits survival and proliferation of cervical carcinoma cells. Hexamethylquercetagetin suppresses tumor volume and weight in BALB/c nude mouse xenograft models of cervical carcinoma. Hexamethylquercetagetin can be used for the research of cancer, such as cervical carcinoma^[1][2]. In Vitro:Hexamethylquercetagetin (25-100 μM; 24 h) potently suppresses NF-κB-driven luciferase activity in Ca Ski and C-33 A cervical carcinoma cells^[2].
Hexamethylquercetagetin (25-100 μM; 24 h) inhibits viability of Ca Ski, C-33 A, HeLa, and SiHa cervical carcinoma cells in a concentration-dependent manner, but does not affect viability of NIH3T3 normal fibroblast cells^[2].
Hexamethylquercetagetin (25-100 μM; 24 h) inhibits NF-κB signaling in Ca Ski and C-33 A cervical carcinoma cells by reducing concentration-dependent expression of p-p65, p-IκBα, Cyclin D1, and Bcl-2^[2].
Hexamethylquercetagetin (25-100 μM; 4 h pre-incubation) suppresses TNFα-induced NF-κB activation in Ca Ski and C-33 A cervical carcinoma cells, as measured by reduced p-p65 expression^[2]. In Vivo:Hexamethylquercetagetin (50-100 mg/kg; p.o.; daily; 15 days) acts as an NF-κB inhibitor to dose-dependently suppress cervical carcinoma tumor growth in BALB/c nude mice^[2].