product name MG-101 (ALLN)
Description: MG-101 (also known as Calpain Inhibitor I and ALLN) is a cell-permeable and potent inhibitor of cysteine proteases including calpains and lysosomal cathepsins. 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.
References: Carcinogenesis. 1990 Jan;11(1):75-80; J Biol Chem. 1991 Jul 15;266(20):13311-7.
383.53
Formula
C20H37N3O4
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)
Solubility (In vivo)
Synonyms
Calpain Inhibitor I and ALLN
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19409840
| 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: 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 Vivo | In mice bearing HCT116 xenografts, MG-101 (10 mg/kg i.p.) inhibits colon tumor formation |
| Animal model | Female athymic nude mice bearing HCT116 xenografts |
| Formulation & Dosage | Dissolved in saline; 10 mg/kg; i.p. injection |
| References | Carcinogenesis. 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. |
