MMP-2/MMP-3 Inhibitor III; PD166793

Biochem/physiol Actions

Reversible: no

Product does not compete with ATP.

Cell permeable: yes

Primary TargetMMP-2, -3, and -13

Target IC₅₀: 47, 12, and 8 nM, against MMP-2, -3, and -13, respectively

General description

A cell-permeable biphenylsulfonylvaline compound that acts as a potent inhibitor against MMP-2, -3, and -13 (IC₅₀ = 47, 12, and 8 nM, respectively) and a weaker inhibitor against AMP deaminase (20% inhibition at 0.1 µM), MMP-1, -7, -9, and -14 (IC₅₀ = 6.1, 7.2, 7.9, and 0.24 µM, respectively). Shown to offer therapeutic benefits in vivo in various animal models of heart failure and diabetes.

Legal Information

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

Other Notes

Paolocci, N., et al. 2006. J. Pharm. Exp. Ther.317, 506.Zhou, Y.P., et al. 2005. Diabetes54, 2612.Peterson, J.T., et al. 2001. Circulation103, 2303.Spinale, F.G., et al. 1999. Circ. Res.85, 364.

Packaging

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: Irritant (B)