Urease-IN-23

Urease-IN-23 (1.5-24 μM; 48 h) inhibits planktonic growth and urease activity of Cryptococcus neoformans and Cryptococcus gattii clinical isolates and reference strains, with IC₅₀ values ranging from 1.5-24 μM, IC₉₀ values ranging from 1.5-24 μM, IC_URE values ranging from 1.5-6 μM, and MFC values ranging from 1.5-24 μM^[1].
Urease-IN-23 (12-50 μM; 48-72 h) inhibits biofilm formation and growth of dispersed cells from mature biofilms of Cryptococcus neoformans H99 and Cryptococcus gattii R265, with IC₉₀ values of 12 μM (biofilm formation) and 25-50 μM (dispersed cells), but does not inhibit sessile cells from preformed biofilms^[1].
Urease-IN-23 (12 μM; 48 h) significantly reduces capsule thickness in Cryptococcus neoformans H99 and Cryptococcus gattii R265^[1].
Urease-IN-23 (6-12 μM; 96 h) completely inhibits melanin production in Cryptococcus neoformans H99 and Cryptococcus gattii R265 after 96 h of incubation^[1].
Urease-IN-23 (2×IC₉₀; up to 72 h) rapidly kills Cryptococcus neoformans H99 and Cryptococcus gattii R265 within 2 h of exposure, reducing viability to undetectable levels^[1].
Urease-IN-23 (IC₉₀, MFC, 4×MFC; 2 h) significantly increases plasma membrane permeability in Cryptococcus neoformans H99 and Cryptococcus gattii R265 after 2 h of exposure^[1].

Urease-IN-23 potently inhibits Cryptococcus neoformans urease in a cell-free assay with a IC₅₀ of 54.92 nM, acting as a mixed-type inhibitor with a K_i of 149.1 nM^[1].
Urease-IN-23 acts as a mixed-type inhibitor of Cryptococcus neoformans urease by simultaneously interacting with both the catalytic nickel center and the allosteric site via ionic interactions with Asp626, inducing dynamic conformational changes in the enzyme^[1].

Urease-IN-23 (72 h) exhibits cytotoxicity against metastatic breast cancer MCF-7 cells with a CC₅₀ of 75.4 μM after 72 h of incubation^[1].