MG-101 (ALLN) | Cysteine Protease inhibitor | CAS 110044-82-1

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Quality Control

Batch: Purity: >97%

Cited in Nature Medicine for its top-tier quality
COA
NMR
Datasheet
SDS

Cited in Nature Medicine for its top-tier quality
COA
NMR
Datasheet
SDS

Cited in Nature Medicine for its top-tier quality
COA
NMR
Datasheet
SDS

Cited in Nature Medicine for its top-tier quality
COA
NMR
Datasheet
SDS

Cited in Nature Medicine for its top-tier quality
COA
NMR
Microanalysis

Why microanalysis?
Datasheet
SDS

97

Related Targets	HDAC Caspase Proteasome Secretase MMP HCV Protease DPP Tyrosinase HIV Protease Serine Protease
Other Cysteine Protease Inhibitors	Calpeptin MG132 SSS Aloxistatin (E64d) Odanacatib E-64 Z-FA-FMK N-Ethylmaleimide (NEM) Cathepsin Inhibitor 1 PD 151746 Loxistatin Acid (E-64C)

Cell Culture, Treatment & Working Concentration

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

Solubility

In vitro
Batch:

DMSO : 77 mg/mL (200.76 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 39 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.850mg/ml (10.04mM)
	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.900mg/ml (4.95mM)
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

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Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	383.53	Formula	C₂₀H₃₇N₃O₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	110044-82-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Calpain inhibitor-1, Ac-LLnL-CHO			Smiles	CCCCC(C=O)NC(=O)C(CC(C)C)NC(=O)C(CC(C)C)NC(=O)C

Mechanism of Action

Targets/IC₅₀/Ki	Cysteine protease
In vitro	MG-101 (ALLN) effectively inhibits cysteine proteinases with ID50 of 7 nM and 13 nM for cathepsins L and B, respectively. This compound shows very weak inhibitory activities towards cathepsin D (aspartic protease) and subtilisin (serine protease). It thus transforms NIH3T3 cells and also induces differentiation of PC12 pheochromocytoma cells. As an inhibitor of Ca(2+)-dependent cysteine proteases, this chemical inhibits the degradation of HMG-CoA reductase and HMGal in cholesterol biosynthesis. In HCT116 cells, it decreases cell viability and tumor growth, and induces apoptosis response through Bax translocation from cytosol to mitochondria.
In vivo	In mice bearing HCT116 xenografts, MG-101 (ALLN) (10 mg/kg i.p.) inhibits colon tumor formation. [3]
References	[1] https://pubmed.ncbi.nlm.nih.gov/2403861/ [2] https://pubmed.ncbi.nlm.nih.gov/1906466/ [3] https://pubmed.ncbi.nlm.nih.gov/23831472/

Applications

Methods	Biomarkers	Images	PMID
Western blot	Cyclin D3 / Cyclin D1 / CDK4 / CDK6 p21(WAF1/CIP1)		28130444

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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MG-101 (ALLN) Cysteine Protease inhibitor

Chemical Structure

Molecular Weight: 383.53