Product Data SheetProduct Name:CAS No.: Cat. No.:MWt:Formula:Purity :GM6001142880-36-2HY-15768388.46C20H28N4O4>98%Solubility:DMSOMechanisms: Pathways:Metabolism/Protease; Target:MMP Biological Activity:GM6001 (galardin, ilomastat) is a broad spectrum MMPs inhibitor for MMP1, MMP2, MMP3,GM6001(galardinilomastat)isabroadspectrumMMPsinhibitorforMMP-1MMP-2MMP-3MMP-7, MMP-8, MMP-9, MMP-12, MMP-14, and MMP-26 with Ki of 0.4-27 nM. IC50 Value: 0.4-27 nM (Ki) [1] Target: MMPs in vitro: GM6001 (galardin, ilomastat) is a broad spectrum matrix metalloprotease (MMP) inhibitor forMMP-1, MMP-2, MMP-3, MMP-7, MMP-8, MMP-9, MMP-12, MMP-14, and MMP-26 with Ki of 0.4nM, 0.5 nM, 27 nM, 3.7 nM, 0.1 nM, 0.2 nM, 3.6 nM, 13.4 nM, 0.36 nM, respectively. GM 6001 isone of the most potent inhibitors of human skin fibroblast collagenase yet reported. GM 6001 has aKi of 20 nM against thermolysin and Pseudomonas aeruginosa elastase. Isomer 6B has a Ki of 7 nMagainst thermolysin and 2 nM against the elastase [1]. Addition of galardin to cells stimulated withbombesin or LPA specifically inhibited total EGFR phosphorylation, as well as site-specificphosphory...References:[1]. Grobelny D, et al. Inhibition of human skin fibroblast collagenase, thermolysin, andPseudomonas aeruginosa elastase by peptide hydroxamic acids. Biochemistry. 1992 Aug11;31(31):7152-4.11;31(31):71524. [2]. Santiskulvong C, et al. Galardin (GM 6001), a broad-spectrum matrix metalloproteinase inhibitor,blocks bombesin- and LPA-induced EGF receptor transactivation and DNA synthesis in rat-1 cells.Exp Cell Res. 2003 Nov 1;290(2):437-46. [3]. Mirastschijski U, et al. Matrix metalloproteinase inhibitor GM 6001 attenuates keratinocytemigration, contraction and myofibroblast formation in skin wounds. Exp Cell Res. 2004 Oct1;299(2):465-75. [4]. Schultz GS, et al. Treatment of alkali-injured rabbit corneas with a synthetic inhibitor of matrixmetalloproteinases. Invest Ophthalmol Vis Sci. 1992 Nov;33(12):3325-31. ...Caution: Not fully tested. For research purposes onlyMedchemexpress LLCwww.medchemexpress.com18Wilkinson Way, Princeton, NJ 080,USAess.com Web: www.medchemexpress.comEmail: info@medchemexpr
