MMP-17 Inhibitor

KP-457 is a selective a disintegrin and metalloproteinase 17 (ADAM17) inhibitor, with higher selectivity for ADAM17 than for other MMPs and ADAM10, and IC₅₀s are 11.1 nM (ADAM17), 748 nM (ADAM10), 717 nM (MMP2), 9760 nM (MMP3), 2200 nM (MMP8), 5410 nM (MMP9), 930 nM (MMP13), 2140 nM (MMP14), and 7100 nM (MMP17), respectively.

Anti-inflammatory agent 121 is a protease inhibitor, with IC₅₀ values against different targets as follows: 1.3 μM (Staphylococcus aureus type I staphylokinase), 2.2 μM (Staphylococcus aureus type II staphylokinase), 2.3 μM (human MMP-1), 2.7 μM (human MMP-2), 1.4 μM (human MMP-8), 4.6 μM (human MMP-9), and 79 μM (human ADAM17). Anti-inflammatory agent 121 inhibits the activities of staphylococcal serine protease glutamyl endopeptidase (V8 protease) and cysteine protease staphylococcal protease B in Staphylococcus aureus cultures. Anti-inflammatory agent 121 inhibits protease activity in skin wash samples, metalloprotease (staphylokinase) activity in Staphylococcus aureus culture supernatants, and staphylokinase-mediated activation of pro-urokinase-type plasminogen activator (pro-uPA). Anti-inflammatory agent 121 can be used in the research of atopic dermatitis.

LP07 is an antibacterial agent targeting Pseudomonas aeruginosa with MIC values for both wild-type and efflux pump-deficient P. aeruginosa PA14 of both 8 μg/mL. LP07 exerts its antibacterial effect by directly disrupting the structural integrity of the bacterial cell membrane. LP07 moderately inhibits MMP-17 and MMP-19, but has no significant inhibitory effect on other MMP subtypes. LP07 does not inhibit the activity of LpxC enzyme. LP07 can be used for research on Pseudomonas aeruginosa infections.