SB-3CT is a selective, mechanism-based inhibitor of the gelatinases, matrix metalloproteinase-2 (MMP-2) and MMP-9 (Kis = 28 and 400 nM, respectively). First pass metabolism of SB-3CT in vivo produces a monohydroxylated metabolite that has greater inhibitory activity (Kis = 6 and 160 nM for MMP-2 and MMP-9, respectively). Both SB-3CT and its active metabolite can cross the blood-brain barrier and have utility in diseases of the central nervous system, such as stroke and traumatic brain injury. SB-3CT may have applications in other pathologies involving gelatinases, including cancer, cardiovascular diseases, and inflammation.
