Ilomastat (GM6001)

Synonyms: Galardin

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 Ki 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

Ilomastat (GM6001) Chemical Structure

CAS: 142880-36-2

Selleck's Ilomastat (GM6001) has been cited by 50 publications

Purity & Quality Control

Batch: Purity: 99.15%
99.15

Ilomastat (GM6001) Related Products

Signaling Pathway

Choose Selective MMP Inhibitors

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation 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
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Biological Activity

Description 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 Ki 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.
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)
In vitro
In vitro

GM6001 inhibits human skin fibroblast collagenase with Ki 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
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. Km 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

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)

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


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In vivo
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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.

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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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