β-Glucuronidase-IN-1_product_DataBase

Bioactivity

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].

Target

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

Invitro

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:

In Vivo

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:

Name

β-Glucuronidase-IN-1

CAS

484006-66-8

Formula

C23H27N3O3S

Molar Mass

425.54

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

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

PeptideDB

β-Glucuronidase-IN-1

CAS: 484006-66-8 F: C23H27N3O3S W: 425.54