embalaje : 25mg
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Synonyms: Z-LLL-al, Z-Leu-Leu-Leu-CHO, MG132
| Description | MG-132 (Z-Leu-Leu-Leu-al) is a 26S proteasome inhibitor (IC50=100 nM) that is cell-permeable and reversible. MG-132 acts as an autophagy activator and also induces apoptosis. |
| Targets & IC50 | Calpain:1.2 μM (cell free), COS-7 cells:< 10 μM, 20S proteasome:100 nM (cell free), HCT116 cells:0.82 μM |
| 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. [1] METHODS: Human mesothelioma cells NCI-H2452 were treated with MG-132 (0.25-2 μM) for 36 h, and 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. [2] METHODS: Human melanoma cells MeWo were treated with MG-132 (0.01-1 μM) for 24 h, and the cell cycle profiles were analyzed by Flow Cytometry. RESULTS: MG-132 induces cell cycle arrest at G2 phase in MeWo cells. [3] |
| 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 harboring the human cervical cancer tumors HeLa, CaSki, or C33A twice a week for 4 weeks. RESULTS: MG-132 significantly inhibited the growth of human cervical cancer tumors, indicating antitumor activity in vivo. [4] METHODS: To investigate 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 band (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 wall thickness, and increased the shortening fraction in AAB rats. MG-132 treatment significantly reversed the elevated levels of ERK1/2 and JNK1 phosphorylation in AAB rats. [5] |
| Synonyms | Z-LLL-al, Z-Leu-Leu-Leu-CHO, MG132 |
| Molecular Weight | 475.62 |
| Formula | C26H41N3O5 |
| Cas No. | 133407-82-6 |
| 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 |
| Relative Density. | 1.073 g/cm3 |
| 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. | ||||||||||||||||||||||||||||||||||||||||
| Solubility Information | H2O: Insoluble Ethanol: 47.5 mg/mL (99.87 mM), Sonication is recommended. DMSO: 240 mg/mL (504.6 mM), Sonication is recommended.  | ||||||||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 9 mg/mL (18.92 mM), Suspension. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | |||||||||||||||||||||||||||||||||||||||||
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
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