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Ilomastat (GM6001)

Name: Ilomastat (GM6001)
Brand: Selleck Chemicals
SKU: S7157
Rating: 5 (55 reviews)

Synonyms: Galardin

Catalog No.S7157 Purity:99.15%

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

Ilomastat (GM6001) Chemical Structure

CAS No. 142880-36-2

Purity & Quality Control

Batch: Purity: 99.15%

99.15

Ilomastat (GM6001) Related Products

Related Targets	MMP1 MMP2 MMP3 MMP7 MMP8 MMP9 MMP12 MMP13 MMP14 MMP26	Click to Expand
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Related Compound Libraries	FDA-approved Drug Library Natural Product Library Bioactive Compound Library-I Protease Inhibitor Library Ubiquitination Compound Library	Click to Expand

Signaling Pathway

MMP Signaling Pathway

Cell Data

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

Biological Activity

Description

Targets

MMP-8 ^[1] (Cell-free assay)	MMP-9 ^[1] (Cell-free assay)	MMP-26 ^[1] (Cell-free assay)	MMP-1 ^[1] (Cell-free assay)	MMP-2 ^[1] (Cell-free assay)	Click to View More Targets
0.1 nM(Ki)	0.2 nM(Ki)	0.36 nM(Ki)	0.4 nM(Ki)	0.5 nM(Ki)	Click to View More Targets

In vitro
In vitro	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] GM 6001 (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	Collagenase assay uses 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.
Cell Research	Cell lines	MLL cells
	Concentrations	20 µM
	Incubation Time	72 h
	Method	Cell viability was measured after 72-h exposure to triapine with co-treatment of 20 µM ilomastat
Experimental Result Images	Methods	Biomarkers	Images	PMID
	Western blot	MyoD / Myf5 / Myf6 / M-Cadherin / Notch1 CD34 / Sca1		23329998
	Immunofluorescence	ZO-1 / Claudin-5 / occludin		21857898

In Vivo
In vivo	Topical application of GM6001 (400 μg/ml) prevents corneal ulceration after severe alkali injury. ^[3] In rabbit model after stenting, GM6001 significantly inhibits intimal hyperplasia and intimalcollagen content, and it increases lumen area in stented arteries without effects on proliferation rates. ^[4]
Animal Research	Animal Models	Rabbit
	Dosages	100 mg/kg/day
	Administration	subcutaneous

References

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Chemical Information & Solubility

Molecular Weight	388.46	Formula	C₂₀H₂₈N₄O₄
CAS No.	142880-36-2	SDF	Download Ilomastat (GM6001) SDF
Smiles	CC(C)CC(CC(=O)NO)C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)NC
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 : 78 mg/mL ( (200.79 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 8 mg/mL

Water : Insoluble

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.					In vivo Formulation Calculator
	Clear solution	5%DMSO 1 40%PEG 300 2 5%Tween80 3 50% ddH2O	27.5mg/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.	In vivo Formulation Calculator
Clear solution	2% DMSO 1 40% PEG 300 2 2% Tween 80 3 ddH2O	11.0mg/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 95% Corn oil	3.4mg/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.

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

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.

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

Tel: +1-832-582-8158 Ext:3
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