xl-784

XL-784 is a selective inhibitor of matrix metalloproteinases (MMPs) with IC50 values of approximately 1900, 0.81, 120, 10.8, 18, and 0.56 nM for MMP-1, MMP-2, MMP-3, MMP-8, MMP-9, and MMP-13, respectively. XL-784 demonstrates potential in a broad range of cancer research applications due to its capability to modulate extracellular matrix remodeling, tumor invasion, and metastasis.

XL-784 free base is a selective inhibitor of matrix metalloproteinases (MMP) with IC50 values of ~1900, 0.81, 120, 10.8, 18, and 0.56 nM for MMP-1, MMP-2, MMP-3, MMP-8, MMP-9, and MMP-13, respectively.

DC-174 is an orally effective small molecule inhibitor of snake venom metalloproteinases (SVMPs) belonging to the hydroxamic acid class. As a candidate molecule optimized from the lead compound XL-784 through structure-activity relationship studies, it broadly inhibits the SVMP enzymatic activity of various snake venoms (e.g., saw-scaled viper, western diamondback rattlesnake, Malayan pit viper, etc.) with IC50 values below 10 nM by chelating the zinc ion in the SVMP active site via its hydroxamic acid group. It also neutralizes snake venom-induced procoagulant toxicity. Pharmacokinetic studies show that DC-174 reaches peak blood concentration approximately 30 minutes after oral administration but has a short half-life (approx. 1.41 hours). Optimized multi-dose regimens can prolong effective exposure time, demonstrating significant survival protection effects in severe snakebite mouse models, thus positioning it as a promising lead compound for developing oral emergency snakebite treatments.