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Purity: ≥98%
MG-101 (also known as MG101; Calpain Inhibitor I and ALLN) is a novel, cell-permeable and potent inhibitor of cysteine proteases, such as lysosomal cathepsins and calpains, that may have antitumor properties. In tumor cell lines, it triggers apoptosis that is dependent on p53. Calpain I, Calpain II, Cathepsin B, and Cathepsin L are all inhibited by MG-101, with corresponding Ki values of 190 nM, 220 nM, 150 nM, and 500 pM. In DLD1-TRAIL/R cells, MG-101 in conjunction with Ad/gTRAIL significantly increased cell death, whereas calpain by itself had very little effect on cell death. It can mitigate the toxicity caused by atractyloside-induced toxicity, overcome acquired resistance to TRAIL, and lessen the harm that dinitrobenzene sulphonic acid causes to the colon.
| Targets |
Cysteine protease
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|---|---|
| ln Vitro |
MG-101 (ALLN) efficiently inhibits cysteine proteinases, with an ID50 for cathepsins L of 7 nM and B of 13 nM, respectively. When it comes to subtilisin (serine protease) and cathepsin D (aspartic protease), MG-101 (ALLN) exhibits extremely weak inhibitory activities. As a result, MG-101 both changes NIH3T3 cells and causes PC12 pheochromocytoma cells to differentiate.[1] As an inhibitor of Ca(2+)-dependent cysteine proteases, MG-101 prevents HMG-CoA reductase and HMGal from being degraded during the biosynthesis of cholesterol.[2] Through the translocation of Bax from the cytosol to the mitochondria, MG-101 causes an apoptosis response in HCT116 cells by reducing tumor growth and cell viability.
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| ln Vivo |
MG-101 (10 mg/kg i.p.) prevents colon tumor development in mice with HCT116 xenografts.[3]
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| Enzyme Assay |
MG-101 (10 mg/kg i.p.) prevents colon tumor development in mice with HCT116 xenografts.[3] Strongly inhibiting calpain I, calpain II, cathepsin B, and cathepsin L with Kis of 190, 220, 150, and 500 pM, respectively, MG-101 is a cysteine protease inhibitor.
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| Cell Assay |
MG-101 (10 mg/kg i.p.) prevents colon tumor development in mice with HCT116 xenografts.[3] Strongly inhibiting calpain I, calpain II, cathepsin B, and cathepsin L with Kis of 190, 220, 150, and 500 pM, respectively, MG-101 is a cysteine protease inhibitor. Using the Cell Counting Kit-8 and the manufacturer's instructions, the viability of the cells is measured. Each well of a 96-well plate is seeded with one type of HCT116 cell, which is then cultured to 80% density and given varying doses of ALLN for a full day. After that, the medium is changed to 100 μl of fresh McCoy's 5A complete medium containing 10% CCK-8 reagent, and it is incubated for one hour. Using a microplate reader, absorbance is measured at 450 nm. Percentages of deaths are displayed as a result.
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| Animal Protocol |
Female athymic nude mice bearing HCT116 xenografts
10 mg/kg i.p. |
| References | |
| Additional Infomation |
Acetylleucyl-leucyl-norleucinal is a tripeptide composed of N-acetylleucyl, leucyl and norleucinal residues joined in sequence. It has a role as a cysteine protease inhibitor. It is a tripeptide and an aldehyde.
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| Molecular Formula |
C20H37N3O4
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|---|---|---|
| Molecular Weight |
383.53
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| Exact Mass |
383.278
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| Elemental Analysis |
C, 62.63; H, 9.72; N, 10.96; O, 16.69
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| CAS # |
110044-82-1
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| Related CAS # |
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| PubChem CID |
443118
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| Appearance |
white solid powder
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| Density |
1.0±0.1 g/cm3
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| Boiling Point |
632.2±50.0 °C at 760 mmHg
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| Flash Point |
192.9±30.3 °C
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| Vapour Pressure |
0.0±1.9 mmHg at 25°C
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| Index of Refraction |
1.474
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| LogP |
3.37
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
13
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| Heavy Atom Count |
27
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| Complexity |
492
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| Defined Atom Stereocenter Count |
3
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| SMILES |
O=C(N[C@H](C=O)CCCC)[C@@H](NC([C@@H](NC(C)=O)CC(C)C)=O)CC(C)C
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| InChi Key |
FMYKJLXRRQTBOR-BZSNNMDCSA-N
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| InChi Code |
InChI=1S/C20H37N3O4/c1-7-8-9-16(12-24)22-19(26)18(11-14(4)5)23-20(27)17(10-13(2)3)21-15(6)25/h12-14,16-18H,7-11H2,1-6H3,(H,21,25)(H,22,26)(H,23,27)/t16-,17-,18-/m0/s1
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| Chemical Name |
(2S)-2-acetamido-4-methyl-N-[(2S)-4-methyl-1-oxo-1-[[(2S)-1-oxohexan-2-yl]amino]pentan-2-yl]pentanamide
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| Synonyms |
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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 |
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| 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) |
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|---|---|---|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.67 mg/mL (4.35 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 1.67 mg/mL (4.35 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1.67 mg/mL (4.35 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6074 mL | 13.0368 mL | 26.0736 mL | |
| 5 mM | 0.5215 mL | 2.6074 mL | 5.2147 mL | |
| 10 mM | 0.2607 mL | 1.3037 mL | 2.6074 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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