Merck, 444284-5MG, MMP-2/MMP-3 Inhibitor III, PD166793

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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
MMP-2, -3, and -13
Product does not compete with ATP.
Reversible: no
Target IC₅₀: 47, 12, and 8 nM, against MMP-2, -3, and -13, respectively
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Irritant (B)