tcsc0471 MG-132

MG-132 is a potent, non-specific 20S proteasome inhibitor, with IC₅₀ of 24.2 nM for the β5 chymotrypsin-like active site.

IC50 & Target: IC50: 24.2 nM (chymotrypsin-like activity)^[1]

In Vitro: Dose-dependent inhibition of cell growth is observed in HeLa cells with an IC₅₀ of approximately 5 μM MG132 for 24 h. MG132 inhibits the growth of HeLa cells via inducing the cell cycle arrest as well as triggering apoptosis^[2]. MG-132 inhibits C6 glioma cell proliferation in a time- and dose-dependent manner (the IC₅₀ value at 24 h is 18.5 μM). MG-132 (18.5 μM) suppresses the proteasome activity by about 70% at 3 h. MG-132 induces apoptosis via down-regulation of antiapoptotic proteins Bcl-2 and XIAP, up-regulation of pro-apoptotic protein Bax and caspase-3, and production of cleaved C-terminal 85 kDa PARP. MG-132 also causes a more than 5-fold increase of reactive oxygen species^[3]. The IC₅₀ of MG-132 against HeLa, CaSki, and C33A cervical cancer cells viability after 48 h of incubation is 2.1, 3.2, and 5.2 μM, respectively^[4].

In Vivo: The in vivo antitumor activity of MG-132 against cervical cancer is examined using s.c. xenograft models. MG-132 is injected at 1 mg/kg using the following schedule: days 1, 4, 8, 12, 15 18, 23, and 26 for mice bearing HeLa tumors. The growth inhibition rates of MG132 compared to control is 49%^[4]. MG-132 (i.p., 0.1 mg/kg/day) attenuates pressure-overload-induced cardiac hypertrophy and improves cardiac function in abdominal aortic banding (AAB) rats through regulation of ERK1/2 and JNK1 signaling pathways^[5].