MG-132

SKU: orb1306306

Description

MG-132

Research Area

Cell Biology, Protein Biochemistry

Key Properties

• CAS Number: 133407-82-6
• MW: 475.62
• Purity: 99.99%
• Formula: C₂₆H₄₁N₃O₅
• SMILES: CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)OCc1ccccc1)C=O
• Target: Autophagy,Apoptosis,Proteasome
• Solubility: Ethanol:47.5 mg/mL (99.87 mM);H2O:Insoluble;DMSO:240 mg/mL (504.6 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:9 mg/mL (18.92 mM)

Bioactivity

• Target IC50:
  HCT116 cells:0.82 μM|20S proteasome:100 nM (cell free)|Calpain:1.2 μM (cell free)|COS-7 cells < 10 μM
• In Vivo:
  METHODS: To detect anti-tumor activity in vivo MG-132 (1 mg/kg) was injected intravenously into C.B-17/lcr-scid/scidJcl mice harborin the human cervical cancer tumors HeLa, CaSki, or C33A twice a week for 4 weeks. Results: MG-132 significantly inhibite the growth of human cervical cancer tumors, indicating antitumor activity in vivo METHODS: To investigat the effects of long-term treatment with MG-132 on cardiac hypertrophy and its associated molecular mechanisms, MG-132 (0.1 mg/kg) was injected intraperitoneally into rats with an abdominal aortic and (AAB) once daily for 8 weeks. Results: MG-132 treatment significantly attenuated left ventricular myocyte area, left ventricular weight/body weight, and lung weight/body weight ratios, decreased left ventricular diastolic diameter and All thickness, and increase the shortening fraction in AAB rats. MG-132 treatment significantly reverse the elevated levels of ERK1/2 and JNK1 phosphorylation in AAB rats.
• In Vitro:
  METHODS: Human cervical cancer cells HeLa were treated with MG-132 (0.5-30 μM) for 24 h, and cell growth Inhibition was detected by MTT. Results: MG-132 dose-dependently inhibited HeLa cell growth with an IC50 of approximately 5 μM. METHODS: Human mesothelioma cells NCI-H2452 were treated with MG-132 (0.25-2 μM) for 36 h, an the expression levels of target proteins were detected by Western Blot. Results: MG-132 treatment induces cleavage of caspases 3 and 7, Bid, and PARP in NCI-H2452 cells. MG-132 induces a caspase-dependent apoptosis. METHODS: Human melanoma cells MeWo were treated with MG-132 (0.01-1 μM) for 24 h, an the cell cycle profiles were analyzed by Flow Cytometry. Results: MG-132 induces cell cycle arrest at G2 phase in MeWo cells.
• Cell Research:
  The effect of MG132 on HeLa cell growth was determined by trypan blue exclusion cell counting or measuring MTT dye absorbance of living cells as previously described. In brief, cells (5x10^5 cells per well) were seeded in 24-well plates for cell counting, and cells (5x10^4 cells per well) were seeded in 96-well microtiter plates fo the MTT assay. After exposure to indicated amounts of MG132 for 24 h, cells in 24-well plates or 96-well plates were collected with trypsin digestion for trypan blue exclusion cell counting or were used fo the MTT assay. Twenty microliters of MTT solution (2 mg mL in PBS) was added to each well of 96-well plates the plates were again incubated for 4 h at 37℃. MTT solution in the medium was aspirated off and 200 μL of DMSO was added to each well to solubiliz the formazan crystals formed in viable cells. Optical density was measured at 570 nM using a microplate reader. Each plate contained multiple wells at a given Experimental condition and multiple control wells. This procedure was replicated for 2-4 plates per condition.
• Animal Research:
  Male Sprague Dawley rats (8 weeks old, 180 – 230 g) were used to establish a pressure-overload model as described previously. All animals were separated into four groups (10 rats per group): (i) Vehicle-treated sham group; (ii) MG132-treated sham group; (iii) Vehicle-treated abdominal aortic anding (AAB) group; and (iv) MG132-treated AAB group. Under intraperitoneal pentobarbital (50 mg/kg) anesthesia, AAB was created using a 5-0 suture tied twice aroun the abdominal aorta in which. a 21-gauge needle was inserted the needle was then retracted yielding a 70 – 80% constriction with an outer aortic diameter of 0.8 mm. in the sham surgery rats the same surgery was performed as described above excep the aorta was constricted. At day 3 afte the surgery, MG132-treated rats were intraperitoneally injected with 0.1 mg/kg/day of MG132 for 8 weeks. All control animals were injected with a corresponding volume of Vehicle only (0.1% DMSO) . Sixteen-week-old Male CD1 mice were used for All our experiments. Thirty minutes befor the immobilization procedure, 0.1 mg/kg of buprenorphine was administrated IP the mice were then anesthetized using isoflurane the right hindlimb was immobilized as previously described. Briefly the hindlimb was immobilized 7 days by staplin the foot exploiting normal dorso-tibial flexion using an Autosuture Royal 35W skin stapler. One tine was inserted close to the toe a the plantar portion o the foot whil the Other was inserted in the distal portion o the gastrocnemius the Other hindlimb was used as a control. Durin the immobilization period the mice were injected Subcutaneously with MG132 (7.5 mg/kg/dose) or Vehicle (DMSO) twice daily. DMSO containing or not MG132 was diluted in sterile pure corn oil (1:100, injected volume 150 μL). After 7 days the tibialis anterior (TA) musclees of immobilized and non-i

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

complex, 26S, 20S proteasome, aldehyde, Apoptosis, Autophagy, calpain, inhibit, Inhibitor, MG132, MG-132, MG 132, Z-LLL-al, Z-Leu-Leu-Leu-CHO, Proteasome, proteolytic, peptide

Compound Identifiers

PubChem CID

462382