E7974

E7974 is a selective inhibitor of α-tubulin (α-tubulin) with an IC₅₀ of 3.9 μM. E7974 disrupts mitotic spindle formation, induces G₂-M phase cell cycle arrest, initiates apoptosis, activates caspase-3, and induces poly (ADP-ribose) polymerase cleavage. E7974 reduces the area of choroidal neovascularization in mouse models, and exerts anti-angiogenic effects when loaded in modified micelles. E7974 can be used in research related to cancer and choroidal neovascularization^[1][2]. In Vitro:E7974 (300 nM; 0-24 h) induces sustained G₂-M phase mitotic arrest in human histiocytic lymphoma U-937 cells, thereby triggering apoptosis characterized by the formation of subdiploid cells starting at 8 h post-treatment^[1].
E7974 (300 nM; 1-13 h) induces maximal mitotic arrest in human histiocytic lymphoma U-937 cells^[1].
E7974 (300 nM; 0-24 h) induces apoptosis in human histiocytic lymphoma U-937 cells, which is confirmed by the cleavage of procaspase-3 and PARP starting at 6 h post-treatment^[1].
E7974 (19.5-65 nM; 18 h) disrupts mitotic spindle formation and induces mitotic arrest in DU 145 human prostate cancer cells, and also reduces microtubule density in non-dividing cells at higher concentrations^[1].
E7974 (300 nM) induces G₂-M phase mitotic arrest and subsequent apoptosis in human prostate cancer cell line DU 145^[1]. In Vivo:E7974 (0.2-20 µM; intravitreal; single dose immediately after laser coagulation) via intravitreal administration of 20 µM alone significantly reduces CNV area in a murine laser-induced CNV model^[2].