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Chemical Structure| 142880-36-2 Chemical Structure| 142880-36-2

Structure of Ilomastat
CAS No.: 142880-36-2

Chemical Structure| 142880-36-2

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Ilomastat (GM6001) is a potent broad-spectrum matrix metalloprotease (MMP) inhibitor, with IC50 values of 1.5 nM for MMP-1, 1.1 nM for MMP-2, 1.9 nM for MMP-3, and 0.5 nM for MMP-9, and a Ki of 0.4 nM for human skin fibroblast collagenase (MMP-1).

Synonyms: GM6001; Galardin

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Product Details of Ilomastat

CAS No. :142880-36-2
Formula : C20H28N4O4
M.W : 388.46
SMILES Code : O=C(N[C@@H](CC1=CNC2=C1C=CC=C2)C(NC)=O)[C@H](CC(C)C)CC(NO)=O
Synonyms :
GM6001; Galardin
MDL No. :MFCD00917040
InChI Key :NITYDPDXAAFEIT-DYVFJYSZSA-N
Pubchem ID :132519

Safety of Ilomastat

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

Target
  • MMP

    MMP-2, Ki:0.1 nM

    MMP-26, Ki:0.36 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
U87 glioblastoma cells 10 µM 24 hours Increased An2 internalization Int J Mol Sci. 2022 Nov 17;23(22):14214
Ly6G+ neutrophils 50 µM 8 hours To evaluate the effect of Ilomastat on the migration ability of Ly6G+ neutrophils from leukemic mice. Results showed that Ilomastat significantly inhibited the migration ability of neutrophils from leukemic mice, while having no effect on neutrophils from naive mice. Exp Hematol Oncol. 2024 May 10;13(1):49
C6 glioma cells 0, 25, 50, 75, or 100 μM 24 hours To evaluate the inhibitory effect of Ilomastat on MMP3 activity secreted by C6-Cx43 cells. Results showed that Ilomastat inhibited MMP3 activity in a concentration-dependent manner. J Enzyme Inhib Med Chem. 2020 Dec;35(1):672-681
juvenile equine tendon and ligament myofibroblasts 10 µg/mL and 20 µg/mL 24 hours To evaluate the effect of Ilomastat on the viability and proliferation capacity of juvenile equine tendon and ligament myofibroblasts. Results showed no significant negative impact on cell viability and proliferation at the tested concentrations. Sci Rep. 2025 May 6;15(1):15762
HrasA5 cells 10 µM 3 weeks Inhibition of MMP activity prevented invasive growth of HrasA5 cells Front Oncol. 2022 Jan 31;12:827985
Human Tenon fibroblast cells (HTFs) 0.01, 1, 10, 100 μM 7 days To evaluate the inhibitory effect of Ilomastat-CD on collagen gel contraction. Results showed that Ilomastat-CD significantly inhibited collagen gel contraction at concentrations ranging from 1 to 100 μM, similar to uncomplexed Ilomastat. Invest Ophthalmol Vis Sci. 2017 Jul 1;58(9):3425-3431

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice FGFR1-driven leukemia model Intraperitoneal injection 100 mg/kg 7 consecutive days To evaluate the effect of Ilomastat on survival and immune cell composition in leukemic mice. Results showed that Ilomastat treatment significantly prolonged survival of leukemic mice, reduced leukemic cells and PMN-MDSCs in peripheral blood, and increased T-cell levels. Exp Hematol Oncol. 2024 May 10;13(1):49
Mice CFTR knockout mice Intratracheal administration 50 µM and 150 µM Single dose, monitored at 4, 24, and 48 hours Evaluate the effect of Ilomastat on lung inflammation; results showed 150 μM Ilomastat significantly reduced inflammation in CF mice Virulence. 2018;9(1):1008-1018
New Zealand White rabbits Topical eye drop 100 μL (1 mg/mL) Single dose, sampled after 4 hours To assess the distribution of Ilomastat-CD in ocular tissues. Results showed therapeutic concentrations of Ilomastat in sclera, conjunctiva, and aqueous humor. Invest Ophthalmol Vis Sci. 2017 Jul 1;58(9):3425-3431
C57BL/6J wild-type and CFTR knockout mice Acute lung infection model Intratracheal administration 150 µM Administered 20 hours post-infection, monitored at 4 and 24 hours To evaluate the anti-inflammatory effects of Ilomastat in acute P. aeruginosa lung infection. Results showed that Ilomastat reduced IL-8-dependent bioluminescence signal, indicating reduced inflammation. Clin Exp Immunol. 2021 Jan;203(1):87-95
New Zealand white rabbits Experimental glaucoma filtration surgery model Subconjunctival injection 100 μM Single injection, lasted for 28 days To evaluate the safety of Ilomastat in glaucoma filtration surgery, results showed that Ilomastat had less toxicity on rabbit cornea, conjunctiva, and ciliary body compared to MMC. J Korean Med Sci. 2017 Apr;32(4):666-671

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT03297827 - Recruiting August 27, 2019 United States, New Mexico ... More >> Department of Neurology, University of New Mexico Recruiting Albuquerque, New Mexico, United States, 87131-0007 Contact: Asad Ikram, MD    505-272-9382    aikram@salud.unm.edu    Principal Investigator: Atif Zafar, MD          Sub-Investigator: Asad Ikram, MD Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.57mL

0.51mL

0.26mL

12.87mL

2.57mL

1.29mL

25.74mL

5.15mL

2.57mL

References

 

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