MG-132

Introduction from Drug peptide supply about:MG-132

Overview of MG-132.

MG132, a proteasome inhibitor, is an effective, reversible 20S protease inhibitor that can penetrate cells. Its IC50 value of inhibiting the activity of proteasome chymotrypsin like peptidase is 24.2 nM. MG-132 inhibited the proliferation of thin Chemicalbook cells of C6 glioma in a time and dose dependent manner (IC50 value at 24 hours was 18.5 μ M）。 MG-132 induces apoptosis by down regulating the anti apoptotic response proteins Bcl-2 and XIAP, up regulating the pro apoptotic proteins Bax and caspase-3, and producing the cleaved C-terminal 85kDaPARP.

Role of MG-132.

MG-132 is a kind of polypeptide aldehyde, which is also effective and reversible. It can pass through the proteasome inhibitor of cells. The IC50 value is 100 nM, which effectively blocks the proteolytic activity of 26S proteasome complex.

In vitro activity of MG-132.

MG132 inhibits the growth of HeLa cells by inducing cell cycle arrest and inducing apoptosis. MG-132 inhibited the proliferation of C6 glioma cells in a time and dose dependent manner (IC50 value at 24 hours was 18.5 μ M）。 MG-132（18.5 μ M) At 3 hours, the proteasome activity was inhibited by about 70%. MG-132 can induce apoptosis by down regulating the anti apoptotic protein Chemicalbook white Bcl-2 and XIAP, up regulating the apoptotic protein Bax and caspase-3, and producing the cleaved C-terminal 85kDaPARP. MG-132 can also increase active oxygen more than 5 times. The IC50 of MG-132 on the survival rate of HeLa, CaSki and C33A cervical cancer cells after 48 hours of incubation was 2.1, 3.2 and 5.2, respectively μ M.

In vivo activity of MG-132.

The anti-tumor activity of MG-132 against cervical cancer in vivo was examined by subcutaneous injection. Heterogeneous migration model. MG-132 was injected at 1 mg/kg using the following protocol: for mice carrying HeLa tumors, days 1,4,8,12,15,18,23 and 26. Compared with the control Chemicalbook, the growth inhibition rate of MG132 was 49%. MG-132 (groin, 0.1 mg/kg/day) alleviates cardiac hypertrophy caused by pressure overload by regulating ERK1/2 and JNK1 signaling pathways and improves cardiac function of abdominal aortic banding (AAB) rats.

Biological activity of MG-132.

MG-132 (Z-Leu-Leu-Leu-al) is an effective and reversible proteasome inhibitor with an IC50 of 100 nM. MG-132 effectively blocks the proteolytic activity of 26S proteasome complex. MG-132 is a peptide aldehyde and an autophagy activator. MG-132 also induced apoptosis.

How to buy MG-132 in the U. S.

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