General Description
A cell-permeable biphenylsulfonylvaline compound that acts as a potent inhibitor against MMP-2, -3, and -13 (IC
50 = 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 (IC
50 = 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.
Biological Activity
Broad spectrum matrix metalloprotease (MMP) inhibitor. Displays high affinity for MMP-2, -3 and -13 (IC 50 values are 4, 7 and 8 nM respectively) and exhibits > 750-fold selectivity over MMP-1, -7 and -9. Attenuates left ventricular remodelling and dysfunction in rat model of heart failure.
