MG-132是一种蛋白酶体抑制剂，IC₅₀为100 nM。还能抑制钙蛋白酶，IC₅₀为1.2 μM。

≥98%

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

MG 132；MG132；Z-Leu-Leu-Leu-CHO；Carbobenzoxy-L-leucyl-L-leucyl-L-leucinal

White to off white powder

Ethanol : 95 mg/mL (199.73 mM)
DMSO : 90 mg/mL (189.23 mM)

Proteasome

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. 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. 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.

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%. 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.