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Ilomastat (GM6001) MMP inhibitor

Name: Ilomastat (GM6001)
Brand: Selleck Chemicals
SKU: S7157
Availability: InStock
Rating: 5 (60 reviews)

Cat.No.S7157

Ilomastat (GM6001) is a broad spectrum matrix metalloprotease (MMP) inhibitor with K_i values of 0.4 nM, 0.5 nM, 27 nM, 3.7 nM, 0.1 nM, 0.2 nM, 3.6 nM, 13.4 nM, and 0.36 nM for MMP-1, MMP-2, MMP-3, MMP-7, MMP-8, MMP-9, MMP-12, MMP-14, and MMP-26, respectively.

Chemical Structure

Molecular Weight: 388.46

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.15%

99.15

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Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Activity Description	PMID
HEk293 cells	Function assay		Inhibition of human recombinant ADAMTS4 expressed in HEk293 cells using FAM-AEwLQGRPISIAK-TAMRA as substrate measured for 15 mins by fluorometric analysis, IC50=0.48 μM	23376997
U251 cells	Function assay	20 μM	Protection against anthrax PA63-lethal toxin complex-induced cytotoxicity in human U251 cells at 20 uM at 400 ng/ml by MTT test	17537721
HEk293 cells	Function assay		Inhibition of human recombinant ADAMTS5 expressed in HEK293 cells using Abz-TESEwSRGAIY-Dpa-KK as substrate measured for 2 hrs by fluorometric analysis, IC50=0.5 μM	23376997
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	388.46	Formula	C₂₀H₂₈N₄O₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	142880-36-2	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Galardin			Smiles	CC(C)CC(CC(=O)NO)C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)NC

Solubility

In vitro
Batch:

DMSO : 78 mg/mL ( (200.79 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 8 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

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.
Clear solution	2% DMSO 1 40% PEG 300 2 2% Tween 80 3 ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	11.000mg/ml (28.32mM)	Taking the 1 mL working solution as an example, add 20 μL of 550 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween-80 to the above system, mix evenly to clarify it; then continue adding Adjust the volume to 1 mL with 530 μL ddH2O. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG 300 2 5%Tween80 3 50% ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	27.500mg/ml (70.79mM)	Taking the 1 mL working solution as an example, add 50 μL of 550 mg/mL clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify; add 50 μL Tween-80 to the above system, mix evenly to clarify; Then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.400mg/ml (8.75mM)	Taking the 1 mL working solution as an example, add 50 μL of 68 mg/mL clarified DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
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.
Clear solution	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.	2.500mg/ml (6.44mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
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+ %

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.

Mechanism of Action

Targets/IC₅₀/Ki	MMP-8 ^[1] (Cell-free assay) 0.1 nM(Ki) MMP-9 ^[1] (Cell-free assay) 0.2 nM(Ki) MMP-26 ^[1] (Cell-free assay) 0.36 nM(Ki) MMP-1 ^[1] (Cell-free assay) 0.4 nM(Ki) MMP-2 ^[1] (Cell-free assay) 0.5 nM(Ki) MMP-12 ^[1] (Cell-free assay) 3.6 nM(Ki) MMP-7 ^[1] (Cell-free assay) 3.7 nM(Ki)
In vitro	Ilomastat (GM6001) inhibits human skin fibroblast collagenase with K_i of 0.4 nM when assayed with a synthetic thio ester substrate at pH 6.5, with 50-fold selectivity over two bacterial enzymes, thermolysin and Pseudomonas aeruginosa elastase. ^[1] This compound (0.1 nM - 10 nM) inhibits gelatinase A and gelatinase B produced by T-cells, thus inhibits T-cell homing. ^[2]
Kinase Assay	Collagenase assay
Kinase Assay	Ilomastat (GM6001) is assayed using the synthetic thiol ester substrate Ac-Pro-Leu-Gly-SCH(i-Bu)CO-Leu-Gly-OEt at pH 6.5. The collagenase concentration is 1-2 nM, and the substrate concentrations are from 0.1 to 0.7 nM. K_m is found to vary between 1.5 and 4 mM.
In vivo	Topical application of Ilomastat (GM6001) (400 μg/ml) prevents corneal ulceration after severe alkali injury. ^[3] In rabbit model after stenting, it significantly inhibits intimal hyperplasia and intimalcollagen content, and increases lumen area in stented arteries without effects on proliferation rates. ^[4]
References	https://pubmed.ncbi.nlm.nih.gov/1322694/ https://pubmed.ncbi.nlm.nih.gov/7722295/ https://pubmed.ncbi.nlm.nih.gov/1385350/ https://pubmed.ncbi.nlm.nih.gov/12039502/ https://pubmed.ncbi.nlm.nih.gov/35396375/

Applications

Methods	Biomarkers	Images	PMID
Western blot	MyoD / Myf5 / Myf6 / M-Cadherin / Notch1 CD34 / Sca1		23329998
Immunofluorescence	ZO-1 / Claudin-5 / occludin		21857898

Tech Support

Handling Instructions

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