GM 6001 - CAS 142880-36-2 - Calbiochem (C15-1215-086)

General description

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.

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.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
MMP-1

Product does not compete with ATP.

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

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

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.

Legal Information

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