GM6001, ilomastat, Galardin�
Molecular Formula: C20H28N4O4
FW 388.47
Prepared by the method of Grobelny et al (1).
Inhibits a wide varietyof matrix metalloproteases with Ki�s in the nanomolar range (1, 2).
Active in a number of animal models of diseases where matrixmetalloproteases are thought to be involved (2, 3, 4, 5, 6).
Purity is greater than 95 % as determined by HPLC.
Ki 1 nM or less against humanskin fibroblast collagenase, human 72 kd gelatinase, human 92 kdgelatinase and human neutrophil collagenase, Ki 27 nM against humanstromelysin (2).
References:
- (1.)Grobelny, D., Poncz, L. and Galardy, R. E. 1992. Inhibition of Human Skin Fibroblast Collagenase, Thermolysin, and PseudomonasAeruginosa Elastase by Peptide Hydroxamic Acids. Biochemistry 31:7152-7154.
- (2.) Galardy, R.E., M. E.Casabonne, C. Giese, J.H. Gilbert, F. Lapierre,H. Lopez, M.E. Schaefer, R. Stack, M. Sullivan, B. Summers, R. T. D.Tyrrell, J. Wee, S.D. Allen J.J. Castellot, J.P. Barletta, G.S. Schultz,L.A. Fernandez, S. Fisher, T.-.Y Cui, H.G. Foell-mer, D. Grobelny, andW.M. Holle-ran 1994. Low Molecular Weight Inhibitors in CornealUlceration, Ann NY Acad. Sci. 732: 315-323.
- (3.) Bendeck, M.P., Zempo. N., Clowes, A.W., Galardy, R.E., and Reidy,M.A.1994. Smooth Muscle Cell Migration and Matrix MetalloproteaseExpression After Arterial Injury in the Rat. Circ. Res. 75: 539-545.
- (4.) Gijbels, K., Galardy, R.E., and Steinman, L. 1994. Reversal ofExperimental Autoimmune Encephalomyelitis with a Hydroxamate Inhibitorof Matrix Metalloproteases. J. Clin. Invest. 94: 2177-2182.
- (5.) Wang, P., Ba, Z.F., Galardy, R.E., and Chaudry. I.H. 1996.Administration of a Matrix Metalloproteinase Inhibitor after HemorrhageImproves Cardiovascular and Hepatocellular Function. Shock 6: 377-382.
- (6.) Solorzano, C.C., Ksontini, R., Pruitt, J.H., Auffenberg, T.,Tannahill C., Galardy, R.E., Schultz, G.P., MacKay, S.L.D., Copeland,E.M., and Moldawer, L.L. 1997. A Matrix Metalloproteinase InhibitorPrevents Processing of Tumor Necrosis Factor a (TNFa) and Abrogates Endotoxin-Induced Lethality. Schock 7:427-431