WJM590

WJM590 (compound 7) potently inhibits purified Plasmodium falciparum aspartic protease X (IC₅₀ = 0.0005 μM), moderately inhibits aspartic proteases IX and V, and exerts differential inhibitory effects on human aspartic proteases^[1].
WJM590 (72 h) inhibits the growth of the asexual blood-stage P. falciparum 3D7, with an EC₅₀ of 0.031 μM^[1].
WJM590 inhibits asexual-stage P. knowlesi YH1 parasites (EC₅₀ = 0.008 μM) and exhibits high activity against P. falciparum PMX^S359P mutant parasites (EC₅₀ = 0.003 μM), with only a 2-fold reduction in potency against P. falciparum PMX^D245N/20x copy number variant parasites (EC₅₀ = 0.061 μM)^[1].
WJM590 (300 nM; 24 h) inhibits aspartic protease X-dependent substrate processing (SERA5 maturation), but not aspartic protease IX-dependent substrate processing (ASP maturation), in the Plasmodium falciparum 3D7 strain^[1].
WJM590 (300 nM; 48 h) arrests asexual-stage Plasmodium falciparum 3D7 parasites at the late schizont stage, thereby inhibiting parasite development and the elevation of parasitemia levels^[1].
WJM590 can inhibit human aspartic proteases renin, cathepsin D and BACE1, with corresponding IC₅₀s of 0.071 μM, 0.008 μM, and 0.226 μM respectively; it exhibits low cytotoxicity to human HepG2 cells, with a CC₅₀ of 8.95 μM^[1].
WJM590 exhibits moderate metabolic stability in human liver microsomes and rat hepatocytes, moderate water solubility at pH 7.4, high binding affinity to Albumax protein, and moderate lipophilicity^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.