A (R) - MG-132 proteasome inhibitor

A (R) - MG-132 proteasome inhibitor

Product label

MG-132（Z-Leu-Leu-Leu-CHO）； Proteasome inhibitor proteasome inhibitor; Calpain inhibitor;; NF-κB activation； CAS：1211877-36-9；

Product Information

Product description

MG-132（MG132，MG 132）， Also known as Z-Leu-Leu-Leu-al, Z-Leu-Leu-Leu-CHO, it is a potent, reversible, and cell permeable proteasome Proteasome inhibitor (IC50=100 nM), as well as a calpain inhibitor required for cell cycle and cell cycle protein degradation (IC50=1.2 μ M) [1]. MG-132 (10 μ M) effectively inhibits TNF α - induced NF - κ B activation, IL-8 gene transcription, and IL-8 protein secretion in A549 cells by inhibiting proteasome mediated degradation of I κ B α [2].

The inhibitory effect of MG-132 (10 μ M) on NF - κ B makes human pancreatic cancer cells more sensitive to the apoptosis induction of etoposide or doxorubicin [3]. MG-132 significantly improves the ability of inositol hexaphosphate (IP6) to reduce cellular metabolism in androgen independent prostate cancer (AIPCa) cell lines PC3 and DU145 [4].

(R) MG-132 (R) - MG132) is a negative control for proteasome inhibitor MG-132. Used as a negative control for MG-132 in protease inhibition experiments. Compared with (S) - MG132, the stereoisomers of (R) - MG132 can more effectively inhibit the activities of ChTL, TL, and PGPH.

Product Features

1） CAS NO：1211877-36-9

2） 化学名： benzyl ((S)-4-methyl-1-(((R)-4-methyl-1-(((S)-4-methyl-1-oxopentan-2-yl)amino)-1-oxopentan-2-yl) amino)-1-oxopentan-2-yl)carbamate

3） 同义名： (R)-MG132; Z-L-Leu-D-Leu-L-Leu-al; Cbz-L-Leu-D-Leu-L-Leucinal;

4) Molecular formula: C26H41N3O5

5) Molecular weight: 475.6

6) Purity: ≥ 98%

7) Appearance: White to off white solid

8) Solubility: soluble in DMSO (~30mg/ml), DMF (~30mg/ml), anhydrous ethanol (~20mg/ml)

9) Chemical structure diagram:

Preservation and transportation methods

Storage: Dry storage at -20 ℃, effective for at least 2 years.

Transportation: Ice pack transportation.

Product Usage

1) Preheat at room temperature for at least 20 minutes and briefly centrifuge to allow the powder/solid to settle at the bottom of the tube before dissolving.

2) Weigh an appropriate amount of powder and dissolve it in anhydrous DMSO to prepare a storage solution (e.g. 20 mg/ml, add 500 μ l DMSO to 10mg (R) - MG-132, vortex and mix well until completely dissolved). After packaging according to a single dosage, store at -20 ° C to avoid repeated freezing and maintain stability for at least one month. Alternatively, store at -80 ° C to extend the storage period.

3) According to the specific experimental application, choose a suitable solvent to dilute to the desired concentration. The commonly used working concentration for in vitro cell experiments is 5-50 µ M, with a processing time of 1-24 hours. Please refer to relevant literature for the specific working concentration and processing time of this product, and explore and optimize according to your own experimental conditions (such as experimental objectives, cell types, culture characteristics, etc.).

Precautions

1) This product is only for scientific research purposes and should not be used for clinical diagnosis or treatment. It should not be used in food or medicine, and should never be used on humans.

2) For your safety and health, please wear lab coats and disposable gloves when operating.

References

[1] Tsubuki S, et al. Differential inhibition of calpain and proteasome activities by peptidyl aldehydes of di-leucine and tri-leucine. J Biochem,119(3), 572-576 (1996).

[2] Fiedler MA, et al. Inhibition of TNF-alpha-induced NF-kappaB activation and IL-8 release in A549 cells with the proteasome inhibitor MG-132. Am J Respir Cell Mol Biol, 19(2), 259-268 (1998).

[3] A. Arlt, J. Vorndamm, M. Breitenbroich, et al. Inhibition of NF- k B sensitizes human pancreatic carcinoma cells to apoptosis induced by etoposide (VP16) or doxorubicin. Oncogene 20, 859-868 (2001).

[4]Diallo JS, et al. Enhanced killing of androgen-independent prostate cancer cells using inositol hexakisphosphate in combination with proteasome inhibitors. Br J Cancer, 99(10), 1613-1622 (2008).

[5]Mroczkiewicz, M., et al. Studies of the synthesis of all stereoisomers of MG-132 proteasome inhibitors in the tumor targeting approach. J. Med. Chem. 53(4), 1509-1518 (2010).

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——Written/Edited by V. Shallan [Copyright belongs to MKBio Maokang]

Shanghai Maokang Biotechnology Co., Ltd. is a company engaged in the research of reagents, instruments, laboratory consumables, and experimental services in the fields of life sciences and biotechnology. It mainly engages in cell biology, botany, molecular biology, immunology, biochemistry, and proteomics. In the fields of biopharmaceuticals and diagnostic reagent research and production. Our company adheres to the business philosophy of "people-oriented, honesty and trustworthiness, and contract keeping". Adhere to the principle of 'quality assurance' to provide high-quality products to our customers.