EF24

EF24, a curcumin analogue, is an NF-kB inhibitor with great anti-tumor efficacy and oral bioavailability via deactivation of the MAPK/ERK signaling pathway in oral squamous cell carcinoma (OSCC). EF24 is active against melanoma and breast cancer cell lines with GI₅₀ values of 0.7 μM and 0.8 μM, respectively. EF24 induces cell cycle arrest and apoptosis in MDA-MB-231 human breast cancer cells and DU-145 human prostate cancer cells. EF24 increases the levels of activated caspase 3 and 9, and decreases the phosphorylated forms of MEK1 and ERK^[1][2][3][4]. In Vitro:EF24 (0-10 μM) exhibits cytotoxicity against human breast cancer cells in a dose-dependent increase^[2].
EF24 (0.1-100 μM, 6-72 h) effectively inhibits the active synthesis of DNA in both DU-145 prostate cancer cells and MDA-MB-231 breast cancer cells^[3].
EF24 (20 μM, 24-72 h) induces cell cycle arrest and apoptosis by means of a redox-dependent mechanism and produces a time-dependent increase in intracellular ROS in MDA-MB-231 human breast cancer cells and DU-145 human prostate cancer cells^[3].
In Vivo:EF24 (0.4 mg/kg, i.p., a single dose for 6 h) markedly ameliorates the post-hemorrhage morphologic changes and inflammatory cell infiltration, inhibits hemorrhage-induced NF-kB phosphorylation in rat model of hemorrhage^[4].