Ilomastat (GM6001, Galardin)

Description: Ilomastat (GM-6001; GM6001; Galardin), a member of the hydroxamic acid class of reversible metallopeptidase inhibitors with important biological activity, is a potent, synthetic, and broad spectrum matrix metalloprotease (MMP) inhibitor. It inhibits MMP-1/23/7/8/9/12/14/26 with Ki values 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 inhibits human skin fibroblast collagenase with Ki of 0.4 nM using the synthetic thiol ester substrate Ac-Pro-Leu-Gly-SCH(i-Bu)CO-Leu-Gly-OEt at pH 6.5. Topical application of Ilomastat prevented corneal ulceration after severe alkali injury and that a combination containing Ilomastat, epidermal growth factor, fibronectin, and aprotinin promoted stable regeneration of corneal epithelium after moderate alkali injury.

References: Biochemistry. 1992 Aug 11; 31(31):7152-4; Invest Ophthalmol Vis Sci. 1992 Nov; 33(12):3325-31; J Am Coll Cardiol. 2002 Jun 5; 39(11):1852-8.

Chemical Name: (R)-N1-((S)-3-(1H-indol-3-yl)-1-(methylamino)-1-oxopropan-2-yl)-N4-hydroxy-2-isobutylsuccinamide

SMILES Code: O=C(NC)[CH](NC([CH](CC(NO)=O)CC(C)C)=O)CC1=CNC2=CC=CC=C21