Home Proteases Cysteine Protease inhibitor MG-101 (ALLN) For research use only.

MG-101 (ALLN)

Synonyms: Calpain inhibitor-1, Ac-LLnL-CHO

MG-101 (ALLN, Calpain inhibitor-1, Ac-LLnL-CHO) is a cell-permeable and potent inhibitor of cysteine proteases including calpains and lysosomal cathepsins.

MG-101 (ALLN) Chemical Structure

MG-101 (ALLN) Chemical Structure

CAS No. 110044-82-1

Purity & Quality Control

MG-101 (ALLN) Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
L1210 Function assay Inhibitory concentration of the compound was determined against L1210 cells, IC50=3μM. 15634028
melanoma B16 Function assay Inhibitory concentration of the compound was determined against melanoma B16 cells, IC50=14.5μM. 15634028
HeLa Cytotoxicity assay 48 hrs Cytotoxicity against human HeLa cells assessed as growth inhibition after 48 hrs by MTS assay, CC50=25.1μM. 23357632
HEK293 Function assay Inhibition of proteasome expressed in HEK293 cells assessed as effect on CyclinD1-CDK4 interaction complexes by EYFP and/or YFP Venus fragment based reporter gene assay 16680159
HEK293 Function assay Inhibition of proteasome expressed in HEK293 cells assessed as effect on Pin1-Jun interaction complexes by EYFP and/or YFP Venus fragment based reporter gene assay 16680159
HEK293 Function assay Inhibition of proteasome expressed in HEK293 cells assessed as effect on p53-p53 interaction complexes by EYFP and/or YFP Venus fragment based reporter gene assay 16680159
HEK293 Function assay Effect on cofilin1 expressed in HEK293 cells assessed as effect on cofilin1; Limk2 interaction complexes by EYFP and/or YFP Venus fragment based reporter gene assay 16680159
HEK293 Function assay Inhibition of proteasome expressed in HEK293 cells assessed as effect on E6:E6AP interaction complexes by EYFP and/or YFP Venus fragment based reporter gene assay 16680159
HEK293 Function assay Inhibition of proteasome expressed in HEK293 cells assessed as effect on p53-Chk1 interaction complexes by EYFP and/or YFP Venus fragment based reporter gene assay 16680159
Click to View More Cell Line Experimental Data

Biological Activity

Description MG-101 (ALLN, Calpain inhibitor-1, Ac-LLnL-CHO) is a cell-permeable and potent inhibitor of cysteine proteases including calpains and lysosomal cathepsins.
Targets
Cysteine protease [1]
In vitro
In vitro 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. [1] MG-101, as an inhibitor of Ca(2+)-dependent cysteine proteases, inhibits the degradation of HMG-CoA reductase and HMGal in cholesterol biosynthesis. [2] In HCT116 cells, MG-101 decreases cell viability and tumor growth, and induces apoptosis response through Bax translocation from cytosol to mitochondria. [3]
Cell Research Cell lines HCT116, HCT116/p53−/−, and HCT116/Bax−/− cells
Concentrations ~26 μM
Incubation Time 24 hours
Method 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot Cyclin D3 / Cyclin D1 / CDK4 / CDK6 p21(WAF1/CIP1) 28130444
In Vivo
In vivo In mice bearing HCT116 xenografts, MG-101 (10 mg/kg i.p.) inhibits colon tumor formation. [3]
Animal Research Animal Models Female athymic nude mice bearing HCT116 xenografts
Dosages 10 mg/kg
Administration i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04987242 Completed
Hyperuricemia|Gout|Chronic Kidney Diseases
Allena Pharmaceuticals
 July 16 2021 Phase 2
NCT04829435 Completed
Hyperuricemia|Gout
Allena Pharmaceuticals
 April 21 2021 Phase 1
NCT04236219 Completed
Hyperuricemia
Allena Pharmaceuticals
 September 2 2020 Phase 1

Chemical Information & Solubility

Molecular Weight 383.53 Formula

C20H37N3O4
CAS No. 110044-82-1 SDF Download MG-101 (ALLN) SDF
Smiles CCCCC(C=O)NC(=O)C(CC(C)C)NC(=O)C(CC(C)C)NC(=O)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 77 mg/mL ( (200.76 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 39 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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