| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
MG115 targets the proteasome, specifically inhibiting its chymotrypsin-like activity. The proteasome is a multi-catalytic protease complex that degrades ubiquitinated proteins, playing a critical role in the regulation of protein turnover, cell cycle progression, and apoptosis. By inhibiting the proteasome, MG115 prevents the degradation of pro-apoptotic proteins, such as p53 and Bax, and promotes the accumulation of ubiquitinated proteins, leading to apoptosis. MG115's inhibition of the proteasome makes it a valuable tool for studying proteasome function and the ubiquitin-proteasome system.
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| ln Vitro |
HepG2 cell viability is dose-dependently decreased by MG-115 (0.1–10 μM; 24 hours) [3]. The CWK18 DNA concentrate-mediated reporter gene expression is amplified by MG-115 (0.1-10 μM) throughout a 24-hour period [3].
In vitro, MG115 is a potent, selective, and reversible inhibitor of the proteasome's chymotrypsin-like activity. It inhibits the degradation of ubiquitinated proteins and promotes apoptosis in cancer cell lines. In cell-based assays, MG115 treatment results in the accumulation of ubiquitinated proteins, increased expression of pro-apoptotic proteins, and induction of apoptosis. The compound's effects on cell cycle progression and cell viability are assessed using flow cytometry and MTT assays. These studies confirm the compound's mechanism of action as a proteasome inhibitor. |
| ln Vivo |
In vivo, MG115 has been studied for its potential in cancer research. By inhibiting the proteasome, the compound can induce apoptosis and inhibit tumor growth in animal models of cancer. MG115 has been evaluated in preclinical studies, where it demonstrates antitumor activity. Comprehensive in vivo efficacy studies are needed to fully characterize its therapeutic potential. MG115 is a valuable research tool for studying proteasome function and apoptosis.
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| Enzyme Assay |
In vitro enzyme assays for MG115 involve measuring the inhibition of the proteasome's chymotrypsin-like activity. The proteasome is incubated with a fluorogenic peptide substrate (e.g., Suc-LLVY-AMC) and varying concentrations of MG115. The cleavage of the substrate is measured fluorometrically, and the IC₅₀ is calculated. These assays confirm the compound's mechanism of action as a proteasome inhibitor.
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| Cell Assay |
Cell Viability Assay [3]
Cell Types: HepG2 Cell Tested Concentrations: 0.1, 1, 2, 5, 10 μM Incubation Duration: 24 hrs (hours) Experimental Results: Dose-dependent decrease in cell viability. Inhibits proteasome activity with an IC50 of 2 μM. In vitro cell-based assays for MG115 evaluate its effects on proteasome function and apoptosis. Cells are cultured and treated with MG115, and the accumulation of ubiquitinated proteins is assessed by Western blot. Apoptosis is quantified by measuring caspase-3/7 activity or by Annexin V staining. Cell viability is assessed using MTT or CellTiter-Glo assays. These assays confirm the compound's functional activity as a proteasome inhibitor. |
| Animal Protocol |
In vivo animal experiments for MG115 have been conducted in mouse xenograft models of cancer. Tumor-bearing mice are treated with MG115 via various routes of administration. Tumor growth is monitored by caliper measurements, and tumor growth inhibition is calculated. Ubiquitinated protein accumulation and apoptosis in tumor tissues are assessed by immunohistochemistry. Pharmacokinetic studies are conducted to determine the compound's half-life, clearance, and tissue distribution. Comprehensive in vivo studies are ongoing.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) data for MG115 are limited. The compound has a molecular weight of 474.60 g/mol. It is soluble in DMSO. The compound's metabolic stability, half-life, and bioavailability have not been fully characterized. Comprehensive ADME studies are needed to fully characterize the pharmacokinetic profile of MG115.
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| Toxicity/Toxicokinetics |
The toxicity profile of MG115 has not been extensively characterized. In laboratory settings, MG115 should be handled as a hazardous chemical. Appropriate personal protective equipment should be used when handling the compound. The compound is for research use only and is not intended for human or veterinary use. Comprehensive toxicological studies are needed.
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| References |
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| Additional Infomation |
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 (benzyl) ester is a peptide.
MG115 is a potent, selective, and reversible inhibitor of the proteasome. It has a molecular formula of C₂₅H₃₈N₄O₅ and a molecular weight of 474.60 g/mol. MG115 inhibits the chymotrypsin-like activity of the proteasome, preventing the degradation of ubiquitinated proteins and promoting apoptosis. The compound has been studied for its potential in cancer research. MG115 is a valuable research tool for studying proteasome function and apoptosis. |
| Molecular Formula |
C25H39N3O5
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|---|---|
| Molecular Weight |
461.59426
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| Exact Mass |
461.288
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| Elemental Analysis |
C, 65.05; H, 8.52; N, 9.10; O, 17.33
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| CAS # |
133407-86-0
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| PubChem CID |
9868928
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| Appearance |
White to off-white solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
678.8±55.0 °C at 760 mmHg
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| Flash Point |
364.3±31.5 °C
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| Vapour Pressure |
0.0±2.1 mmHg at 25°C
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| Index of Refraction |
1.508
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| LogP |
5.41
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
15
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| Heavy Atom Count |
33
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| Complexity |
617
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| Defined Atom Stereocenter Count |
3
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| SMILES |
CCC[C@H](NC([C@@H](NC([C@@H](NC(OCC1=CC=CC=C1)=O)CC(C)C)=O)CC(C)C)=O)C=O
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| InChi Key |
QEJRGURBLQWEOU-FKBYEOEOSA-N
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| InChi Code |
InChI=1S/C25H39N3O5/c1-6-10-20(15-29)26-23(30)21(13-17(2)3)27-24(31)22(14-18(4)5)28-25(32)33-16-19-11-8-7-9-12-19/h7-9,11-12,15,17-18,20-22H,6,10,13-14,16H2,1-5H3,(H,26,30)(H,27,31)(H,28,32)/t20-,21-,22-/m0/s1
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| 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
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| Synonyms |
MG115; MG-115; MG 115; Z-LL-Nva-CHO; ASD 4955; ASD-4955; ASD4955; Z-Leu-Leu-Norvalinal; Z-LLnV
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~216.64 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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