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    MG-101 (ALLN)
    MG-101 (ALLN)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0705
    CAS #: 110044-82-1Purity ≥98%

    Description: MG-101 (also known as MG101; Calpain Inhibitor I and ALLN) is a novel, cell-permeable and potent inhibitor of cysteine proteases including calpains and lysosomal cathepsins with potential antitumor activity. It activates p53-dependent apoptosis in tumor cell lines. MG-101 inhibits calpain I, calpain II, cathepsin B and cathepsin L with Ki values of 190 nM, 220 nM, 150 nM and 500 pM, respectively. MG-101 combined with Ad/gTRAIL induced cell death dramatically in DLD1-TRAIL/R cells, while calpain alone had only minimal killing effects. It can reduce colon injury caused by dinitrobenzene sulphonic acid, overcome acquired resistance to TRAIL, protect against atractyloside-induced toxicity, and reduce colon injury caused by dinitrobenzene sulphonic acid.

    References: Carcinogenesis. 1990 Jan;11(1):75-80; J Biol Chem. 1991 Jul 15;266(20):13311-7.

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    Molecular Weight (MW)383.53
    FormulaC20H37N3O4
    CAS No.110044-82-1
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 76 mg/mL (198.2 mM)
    Water: <1 mg/mL
    Ethanol: 76 mg/mL (198.2 mM)
    Other infoChemical Name: (S)-2-acetamido-4-methyl-N-((S)-4-methyl-1-oxo-1-(((R)-1-oxohexan-2-yl)amino)pentan-2-yl)pentanamide
    InChi Key: FMYKJLXRRQTBOR-SQNIBIBYSA-N
    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+/m1/s1
    SMILES Code: CC(C)C[[email protected]](NC(C)=O)C(N[[email protected]@H](CC(C)C)C(N[[email protected]](CCCC)C=O)=O)=O
    SynonymMG101; ALLN; AcLLnLCHO; Calpain Inhibitor I; MG-101; MG 101; Ac-Leu-Leu-Nle-Aldehyde.


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    In Vitro

    In vitro activity: MG-101 (ALLN) effectively inhibits cysteine proteinases with ID50 of 7 nM and 13 nM for cathepsins L and B, respectively. MG-101 (ALLN) shows very weak inhibitory activities towards cathepsin D (aspartic protease) and subtilisin (serine protease). MG-101 thus transforms NIH3T3 cells and also induces differentiation of PC12 pheochromocytoma cells. MG-101, as an inhibitor of Ca(2+)-dependent cysteine proteases, inhibits the degradation of HMG-CoA reductase and HMGal in cholesterol biosynthesis. In HCT116 cells, MG-101 decreases cell viability and tumor growth, and induces apoptosis response through Bax translocation from cytosol to mitochondria.


    Kinase Assay: MG-101 is a potent inhibitor of cysteine proteases which inhibits calpain I, calpain II, cathepsin B and cathepsin L with Kis of 190, 220, 150 and 500 pM, respectively.


    Cell Assay: Cells viability is assayed using Cell Counting Kit-8 following manufacturer’s protocol. All HCT116 cell typesare seeded into each well of 96-well plate, cultured to 80% density and treated with different doses of ALLN for 24 h. Medium is then replaced by 100 μl fresh McCoy’s 5A complete medium with 10% CCK-8 reagent and incubated for 1 h. Absorbance is measured at 450 nm using a microplate reader. Results are shown as death percentages.

    In VivoIn mice bearing HCT116 xenografts, MG-101 (10 mg/kg i.p.) inhibits colon tumor formation
    Animal modelFemale athymic nude mice bearing HCT116 xenografts
    Formulation & DosageDissolved in saline; 10 mg/kg; i.p. injection
    ReferencesCarcinogenesis. 1990 Jan;11(1):75-80; J Biol Chem. 1991 Jul 15;266(20):13311-7; Biochem Biophys Res Commun. 2013 Jul 26;437(2):325-30.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

     Biological Activity-MG-101 (ALLN) 
    ALLN represses growth of colon cancer HCT116 cells and tumorigenicity in nude ...
    Biochem Biophys Res Commun. 2013 Jul 26;437(2):325-30.
     
    ALLN induces apoptosis in colon cancer cells. (A) Pro-caspase-3 and cleaved PARP ...
    Biochem Biophys Res Commun. 2013 Jul 26;437(2):325-30.
    ALLN-induced apoptosis by a Bax-dependent mechanism. (A) HCT116 (wild type), ...
    Biochem Biophys Res Commun. 2013 Jul 26;437(2):325-30.
     
    ALLN-induced Bax translocation from cytoplasm to mitochondria. (A) Bax–EGFP was ...
    Biochem Biophys Res Commun. 2013 Jul 26;437(2):325-30.
     MG-101 (ALLN)


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