β-Glucuronidase-IN-1

β-Glucuronidase-IN-1 is a potent, selective, uncompetitive, and orally active E. coli bacterial β-glucuronidase inhibitor, exhibiting an IC50 and a Ki of 283 nM and 164 nM, respectively[1].

Research Areas >> Cancer

Research Areas >> Infection

Signaling Pathways >> Anti-infection >> Bacterial

IC50: 283 nM (E. coli β-glucuronidase) Ki: 164 nM (E. coli β-glucuronidase)[1]

β-Glucuronidase-IN-1 (Inhibitor 1) (0.01-100 μM) inhibits E. coli β-glucuronidase activity as a dose-dependent manner and exhibits an IC50 and a Ki value with 283 nM and 164 nM, respectively[1]. β-Glucuronidase-IN-1 (100 μM; 24-72 hours) maintains potent efficacy in living bacterial cells (EC50=17.7 nM), it does not affect bacterial cell growth under aerobic or anaerobic conditions or killing mammalian epithelial cells[1]. Cell Viability Assay[1] Cell Line: CMT93, CaCO-2, HCT116 cells Concentration: 100 μM Incubation Time: 24 hours, 48 hours and 72 hours Result: Did not impact mammalian cell survival and any reduction in cell viability were attributed to the presence of DMSO.

β-Glucuronidase-IN-1 (oral gavage; 10 μg; twice per day; 11 days) protects the mouse GI epithelium from CPT-11–induced damage and protects the glandular structure of CPT-11-treated intestinal tissues[1]. Animal Model: Healthy 6- to 8-week-old Balb/cJ mice[1] Dosage: 10 μg Administration: Oral gavage; twice per day; 11 days Result: Alleviated CPT-11-induced toxicity in mice.

[1]. Wallace BD, et al. Alleviating cancer drug toxicity by inhibiting a bacterial enzyme.Science. 2010 Nov 5;330(6005):831-5.