Name: MG-115
Brand: GlpBio
SKU: GC10178
Availability: InStock
Rating: 5 (30 reviews)

GlpBio Products Cited In Reputable Papers

Nature
610.7931 (2022): 366-372

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618, 1017–1023 (2023)

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183.7 (2020): 1867-1883

Cell Research
31, 1291–1307 (2021)

Cell Research
33, 273–287 (2023)

Cell Research
33, 546–561 (2023)

Molecular Cancer
21.1 (2022): 1-17

Molecular Cancer
21.1 (2022): 1-18

Cancer Cell
39 (2021): 1-16

Cell Host Microbe
30.8 (2022): 1124-1138

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31.5 (2023): 766-780

Cell Host Microbe
31.3 (2023): 418-43

Cell Metabolism
34.2 (2022): 240-255

Ann Rheum Dis
82(4): 533-545 (2023)

Cell Mol Immunol
20, 264–276 (2023)

Adv Funct Mater
33.35 (2023): 2214998

Product Documents

Quality Control & SDS

View current batch:

Purity: >98.00%

Protocol

Kinase experiment [1]:
Preparation Method	Proteasome fractions were prepared from rabbit psoas muscle homogenates by differential centrifugation and were resolved into 26S and 20S particles by precipitation with ammonium sulfate (0%-38% and 40%-80%, respectively) followed by chromatography sequentially on a Mono Q and a Superose 6 column. Peptide-AMC substrates and inhibitor(including MG-115) (1-10 μl) in DMSO were added to 2 ml of assay buffer that for the 20S proteasome contained 20 mM Tris-HCI, 0.5 mM EDTA, and 0.035% SDS (pH 8.0); for the 26S proteasome, contained 20 mM Tris-HCI, 1 mM ATP, and 2 mM MgCls (pH 8.0); for cathepsin B, contained 100 mM NaOAc, 5 mM EDTA, and 2 mM DTT; and for calpain, contained 20 mM Tris-HCI, 1 mM CaCl2, and 2 mM DTT (pH 8.0). After equilibration at 37℃ (proteasomes and cathepsin B) or 20℃ (calpain), enzyme (1-5 μl) was added, and reaction progress was monitored by the increase in fluorescence emission at 440 nm (lar, 380 nm).
Applications	MG-115 is a more potent inhibitor with Kis of 21 nM and 35 nM for 20S and 26S proteasome, respectively.
Cell experiment [2]:
Cell lines	Rat-1 and PC12 cells
Preparation Method	Actively proliferating Rat-1 fibroblasts and PC12 pheochromocytoma cells were treated with PSI and MG-115. After 4 h of treatment, apoptosis was assayed by DNA fragmentation.
Reaction Conditions	30 μM MG-115 for 4 h
Applications	Both Rat-1 and PC12 cells underwent apoptosis following treatment with MG-115.
References: [1]. Rock KL, Gramm C, et,al. Inhibitors of the proteasome block the degradation of most cell proteins and the generation of peptides presented on MHC class I molecules. Cell. 1994 Sep 9;78(5):761-71. doi: 10.1016/s0092-8674(94)90462-6. PMID: 8087844. [2]. Lopes UG, Erhardt P, et,al. p53-dependent induction of apoptosis by proteasome inhibitors. J Biol Chem. 1997 May 16;272(20):12893-6. doi: 10.1074/jbc.272.20.12893. PMID: 9148891.

MG-115 is a potent inhibitor with Kis of 21 nM and 35 nM for 20S and 26S proteasome, respectively ^[1].

MG-115 (50 μM, 2 h) increased the expression of the insulin receptor and its mature beta subunit by a factor of 3 and 4.2, respectively in Leu1193 and Asp1179 COS-7 mutant cell lines^[2].Treated Rat-1 and PC12 cells with MG-115(30 μM, 4 h) can induced apoptosis of both cell types^[3]. Iisolated rat islets were cultured and pre-treated with proteasome inhibitors and subsequently exposed for 48 h to 25 U/ml human IL-1beta. Pre-treatment with 10 uM of the proteasome inhibitor MG-115 counteracted the suppressive effects^[4]. HCC cells SK-Hep1, HLE and HepG2 were treated with the proteasome inhibitors MG-115. MG-115 induce apoptosis in the three cell types tested in a dose-dependent manner. MG-115 downregulated expression of XIAP in SK-Hep1, and survivin in SK-Hep1 and HepG2^[5]. MG-115 decreased within 120 min the aldosterone and corticosterone secretion from freshly dispersed zona glomerulosa and zona fasciculata-reticularis (ZF/R) cells. After a 24-h incubation MG-115 alone lowered corticosterone production and enhanced proliferation rate of cultured ZF/R cells^[6]. The proteasome inhibitor MG-115 can inhibit ATF6, which is the direct target of the proteasome-ubiquitin pathway^[7]. MG-115 was diminished by adding at a time corresponding to the half time required for germinal vesicle breakdown. Potent inhibition of germinal vesicle breakdown was also observed by microinjection of anti-proteasome-a-subunit antibodies^[8]. MG-115 induced a decrease in Bid, Bcl-2, and survivin protein levels, an increase in Bax, loss of the mitochondrial transmembrane potential, cytochrome c release, activation of caspases (-8, -9 and -3), and an increase in the tumor suppressor p53 levels in PC3^[9].

References:
[1]. Rock KL, Gramm C, et,al. Inhibitors of the proteasome block the degradation of most cell proteins and the generation of peptides presented on MHC class I molecules. Cell. 1994 Sep 9;78(5):761-71. doi: 10.1016/s0092-8674(94)90462-6. PMID: 8087844.
[2]. Imamura T, Haruta T, et,al. Involvement of heat shock protein 90 in the degradation of mutant insulin receptors by the proteasome. J Biol Chem. 1998 May 1;273(18):11183-8. doi: 10.1074/jbc.273.18.11183. PMID: 9556607
[3]. Lopes UG, Erhardt P, et,al. p53-dependent induction of apoptosis by proteasome inhibitors. J Biol Chem. 1997 May 16;272(20):12893-6. doi: 10.1074/jbc.272.20.12893. PMID: 9148891.
[4]. Sternesj? J, Karlsen AE, et,al.Involvement of the proteasome in IL-1beta induced suppression of islets of Langerhans in the rat. Ups J Med Sci. 2003;108(1):37-50. doi: 10.3109/2000-1967-122. PMID: 12903836.
[5]. Inoue T, Shiraki K, et,al. Proteasome inhibition sensitizes hepatocellular carcinoma cells to TRAIL by suppressing caspase inhibitors and AKT pathway. Anticancer Drugs. 2006 Mar;17(3):261-8. doi: 10.1097/00001813-200603000-00004. PMID: 16520654.
[6]. Ziolkowska A, Tortorella C, et,al.Accumulation of steroidogenic acute regulatory protein mRNA, and decrease in the secretory and proliferative activity of rat adrenocortical cells in the presence of proteasome inhibitors. Int J Mol Med. 2006 May;17(5):865-8. PMID: 16596272.
[7]. Hong M, Li M, et,al. Endoplasmic reticulum stress triggers an acute proteasome-dependent degradation of ATF6. J Cell Biochem. 2004 Jul 1;92(4):723-32. doi: 10.1002/jcb.20118. PMID: 15211570.
[8].Takagi Sawada M,et,al. The proteasome is an essential mediator of the activation of pre-MPF during starfish oocyte maturation. Biochem Biophys Res Commun. 1997 Jul 9;236(1):40-3. doi: 10.1006/bbrc.1997.6900. PMID: 9223422.
[9].Nam YJ, Lee DH, et,al. 3,4,5-tricaffeoylquinic acid attenuates proteasome inhibition-mediated programmed cell death in differentiated PC12 cells. Neurochem Res. 2014 Aug;39(8):1416-25. doi: 10.1007/s11064-014-1327-x. Epub 2014 May 14. PMID: 24825618.

Cas No.	133407-86-0	SDF
Chemical Name	benzyl N-[(2S)-4-methyl-1-[[(2S)-4-methyl-1-oxo-1-[[(2S)-1-oxopentan-2-yl]amino]pentan-2-yl]amino]-1-oxopentan-2-yl]carbamate
Canonical SMILES	CCCC(C=O)NC(=O)C(CC(C)C)NC(=O)C(CC(C)C)NC(=O)OCC1=CC=CC=C1
Formula	C₂₅H₃₉N₃O₅	M.Wt	461.59
Solubility	25mg/mL in DMSO, 25mg/mL in DMF, 30mg/mL in Ethanol	Storage	Store at -20°C
General tips	Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition	Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
		1 mg	5 mg	10 mg
	1 mM	2.1664 mL	10.8321 mL	21.6642 mL
	5 mM	0.4333 mL	2.1664 mL	4.3328 mL
	10 mM	0.2166 mL	1.0832 mL	2.1664 mL

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

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3. All of the above co-solvents are available for purchase on the GlpBio website.

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