MedChemExpress - Model Ilomastat -142880-36-2

Ilomastat (GM6001) is a potent and broad spectrum matrix metalloprotease (MMP) inhibitor, inhibits MMPs (IC50s, 1.5 nM for MMP-1; 1.1 nM for MMP-2; 1.9 nM for MMP-3; 0.5 nM for MMP-9), with a Ki of 0.4 nM for human skin fibroblast collagenase (MMP-1).

Ilomastat

MCE China：Ilomastat

Brand：MedChemExpress (MCE)

Cat. No.HY-15768

CAS：142880-36-2

Synonyms：GM6001; Galardin

Purity：98.39%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Ilomastat (GM6001) is a potent and broad spectrum matrix metalloprotease (MMP) inhibitor, inhibits MMPs (IC50s, 1.5 nM for MMP-1; 1.1 nM for MMP-2; 1.9 nM for MMP-3; 0.5 nM for MMP-9), with a Ki of 0.4 nM for human skin fibroblast collagenase (MMP-1).

In Vitro：Ilomastat (GM6001) inhibits human skin fibroblast collagenase, thermolysin and elastase with Kis?of 0.4 nM, 20 nM, 20 nM, resepctively[1].?Ilomastat (0.1-10 nM) inhibits gelatinase A and gelatinase B produced by T-cells. Ilomastat inhibits T-cell homing[4].

In Vivo：Ilomastat (GM6001) (400 μg/mL) inhibits corneal ulceration after severe alkali injury in animals[2]. Ilomastat (GM6001) significantly suppresses intimal hyperplasia and intimalcollagen content. Ilomastat increases lumen area in stented arteries, shows no activity on proliferation rates in rabbit model after stenting[3].

Animal Administration：To assess the effects of MMP inhibition, animals are given daily injections of either vehicle (“placebo group”) or Ilomastat (GM6001) (100 mg/kg per day as subcutaneous suspension), beginning one day before the second injury until seven days after the procedure. Ilomastat (GM6001) is a nonspecific hydroxamic acid-based MMPI with potent inhibitory activity against collagenase, gelatinases and stromelysin. Animals are euthanized at either 1 week or 10 weeks after the second injury.

IC50 & Target：MMP-9 0.5 nM (IC50) MMP-2 1.1 nM (IC50) MMP-1 1.5 nM (IC50) MMP-3 1.9 nM (IC50) Fibroblast collagenase 0.4 nM (Ki, Human skin) Thermolysin 20 nM (Ki) Eastase 20 nM (Ki)

References：

[1]. Grobelny D, et al. Inhibition of human skin fibroblast collagenase, thermolysin, and Pseudomonas aeruginosa elastase by peptide hydroxamic acids. Biochemistry. 1992 Aug 11;31(31):7152-4. [Content Brief]

[2]. Schultz GS, et al. Treatment of alkali-injured rabbit corneas with a synthetic inhibitor of matrix metalloproteinases. Invest Ophthalmol Vis Sci. 1992 Nov;33(12):3325-31. [Content Brief]

[3]. Li C, et al. Arterial repair after stenting and the effects of GM6001, a matrix metalloproteinase inhibitor. J Am Coll Cardiol. 2002 Jun 5;39(11):1852-8. [Content Brief]

[4]. Leppert D, et al. T cell gelatinases mediate basement membrane transmigration in vitro. J Immunol. 1995 May 1;154(9):4379-89. [Content Brief]

[5]. Yamamoto M, et al. Inhibition of membrane-type 1 matrix metalloproteinase by hydroxamate inhibitors: an examination of the subsite pocket. J Med Chem. 1998 Apr 9;41(8):1209-17. [Content Brief]

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MedChemExpress - Model Ilomastat -142880-36-2

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Ilomastat