GM 6001 is a broad spectrum MMP inhibitor with Ki values of 0.1nM, 0.2nM, 0.36nM, 0.4nM, 0.5nM, 3.6nM and 3.7nM for MMP-8, MMP-9, MMP-26, MMP-1, MMP-2, MMP-12 and MMP-7[1]. The tyrosine phosphorylation of EGFR induced by leptin could be significantly attenuated by treatment with 25μM GM6001 for 30min in rat aortic smooth muscle cells, due to the inhibition of proteolytic cleavage of transmembrane precursors via matrix metalloproteinase by GM6001[2]. Inhibition of MMP-2/MMP-9-mediated NCAM (Neural cell adhesion molecule) proteolysis by administration of 5μg GM6001 through intracerebroventricular route 30 minutes before and 2 h after ischemia attenuated the infarction, behavioral abnormalities of MCAO (middle cerebral artery occlusion) model mice, with suppression on the level of NCAM cleavage product by GM6001 observed[3].
Ilomastat/伊洛马司他 细胞实验
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
Ilomastat/伊洛马司他 动物实验
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.
United States, New Mexico
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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 收起 <<
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
human U251 cells
20 μM
Function assay
Protection against anthrax PA63-lethal toxin complex-induced cytotoxicity in human U251 cells at 20 uM at 400 ng/ml by MTT test
United States, New Mexico
... 展开 >>
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 收起 <<
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