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MG-101(ALLN)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
MG-101(ALLN)图片
CAS NO:110044-82-1
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
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.
理化性质和储存条件
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[C@H](NC(C)=O)C(N[C@@H](CC(C)C)C(N[C@H](CCCC)C=O)=O)=O
SynonymMG101; ALLN; AcLLnLCHO; Calpain Inhibitor I; MG-101; MG 101; Ac-Leu-Leu-Nle-Aldehyde.
实验参考方法
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.