Biochem/physiol Actions

Reversible: no

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

Product does not compete with ATP.

Primary TargetMMP-1

Cell permeable: yes

General description

A potent, cell-permeable, broad-spectrum hydroxamic acid inhibitor of matrix metalloproteinases (MMPs); (K_i = 400 pM for MMP-1; K_i = 500 pM for MMP-2; K_i = 27 nM for MMP-3; K_i = 100 pM for MMP-8; and K_i = 200 pM for MMP-9). Prevents the release of TNF-α in vivo and in vitro and abrogates endotoxin-induced lethality in mice. A 10 mM (1 mg/257 µl) solution of GM6001 (Cat. No. 364206) in DMSO is also available.

A cell-permeable, potent broad-spectrum hydroxamic acid inhibitor of matrix metalloproteinases (MMPs). [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. 1993. Drugs Future18, 1109.Grobelny, D., et al. 1992. Biochemistry31, 7152.

Packaging

1, 5 mg in Plastic ampoule

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Warning

Toxicity: Standard Handling (A)