Biochem/physiol Actions

Target K_i: 400 pM for MMP-1; 500 pM for MMP-2; 27 nM for MMP-3; 100 pM for MMP-8; and 200 pM for MMP-9

Reversible: no

Product does not compete with ATP.

Primary TargetMMP-1

Cell permeable: yes

General description

A potent broad-spectrum hydroxamic acid inhibitor of matrix metalloproteinases (MMPs). Inhibits MMPs in vitro [K_i = 0.4 nM for skin fibroblast collagenase (MMP-1); K_i = 0.5 nM for gelatinase A (MMP-2); K_i = 27 nM for stromelysin (MMP-3); K_i = 0.1 nM for neutrophil collagenase (MMP-8); and K_i = 0.2 nM for gelatinase B (MMP-9)]. Also prevents the release of TNF-α in vivo and in vitro and abrogates endotoxin-induced lethality in mice.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Solorzano, C.C., et al. 1997. Shock7, 427.Galardy, R.E., et al. 1994. Ann. NY Acad. Sci.732, 315.Galardy, R.E., et al. 1994. Cancer Res.54, 4715.Galardy, R.E., et al. 1993. Drugs Future18, 1109.Grobelny, D., et al. 1992. Biochemistry31, 7152.

Packaging

1 mg in Plastic ampoule

Packaged under inert gas

Physical form

A 10 mM (1 mg/257 µl) solution of GM6001 (Cat. No. 364205) in DMSO.

Reconstitution

Following initial use, aliquot and refrigerate (4°C).

Warning

Toxicity: Irritant (B)