β-Glucuronidase-IN-1

• CAT Number: I015595
• CAS Number: 484006-66-8
• Molecular Formula: C₂₃H₂₇N₃O₃S
• Molecular Weight: 425.54
• Purity: ≥95%
• Target: Bacterial
• Storage: Store at -20°C
• IUPAC Name: 1-[(6,8-dimethyl-2-oxo-1H-quinolin-3-yl)methyl]-3-(4-ethoxyphenyl)-1-(2-hydroxyethyl)thiourea
• InChI: InChI=1S/C23H27N3O3S/c1-4-29-20-7-5-19(6-8-20)24-23(30)26(9-10-27)14-18-13-17-12-15(2)11-16(3)21(17)25-22(18)28/h5-8,11-13,27H,4,9-10,14H2,1-3H3,(H,24,30)(H,25,28)
• InChIKey: PSKUPWXOVUAUJD-UHFFFAOYSA-N
• SMILES: CCOC1=CC=C(C=C1)NC(=S)N(CCO)CC2=CC3=CC(=CC(=C3NC2=O)C)C

β-Glucuronidase-IN-1（Cat No.:I015595） is a highly potent and selective inhibitor of E. coli bacterial β-glucuronidase, demonstrating uncompetitive inhibition and oral bioavailability. It effectively inhibits the activity of the enzyme, with an IC50 value of 283 nM and a Ki value of 164 nM. By targeting β-glucuronidase, this compound shows promise in preventing the deglucuronidation of glucuronide-conjugated drugs, which can improve their bioavailability and efficacy. β-Glucuronidase-IN-1 presents potential applications in drug development and may aid in enhancing the therapeutic properties of glucuronide-conjugated compounds.

Reference

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