MG-101 (ALLN) | 97%(HPLC) | In Stock | Cysteine Protease inhibitor

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

CAS: 110044-82-1

Selleck's MG-101 (ALLN) has been cited by 17 Publications

1 Customer Review

Purity & Quality Control

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Cell Data

Cell Lines	Assay Type	Incubation Time	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
Experimental Result Images	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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
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

References
[1] Hiwasa T, et al. Carcinogenesis. 1990, 11(1), 75-80. [2] Inoue S, et al. J Biol Chem. 1991, 266(20), 13311-13317. [3] Li SZ, et al. Biochem Biophys Res Commun. 2013, 437(2), 325-330.

References

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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

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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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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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