| Identification | Back Directory | [Name]
1-((6,8-dimethyl-2-oxo-1,2-dihydroquinolin-3-yl)methyl)-3-(4-ethoxyphenyl)-1-(2-hydroxyethyl)thiourea | [CAS]
484006-66-8 | [Synonyms]
β-Glucuronidase-IN-1
β-Glucuronidase-IN-1
beta-Glucuronidase inhibitor 1
1-((6,8-dimethyl-2-oxo-1,2-dihydroquinolin-3-yl)methyl)-3-(4-ethoxyphenyl)-1-(2-hydroxyethyl)thiourea | [Molecular Formula]
C23H27N3O3S | [MDL Number]
MFCD02747821 | [MOL File]
484006-66-8.mol | [Molecular Weight]
425.544 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 100 mg/mL (235.00 mM; Need ultrasonic) | [form ]
Solid | [color ]
Light yellow to green yellow | [SMILES]
O=C(N1)C(CN(C(NC2=CC=C(C=C2)OCC)=S)CCO)=CC3=C1C(C)=CC(C)=C3 |
| Hazard Information | Back Directory | [Uses]
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]. | [Biological Activity]
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].
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].
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]. | [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: | 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. |
| [References]
[1]. Wallace BD, et al. Alleviating cancer drug toxicity by inhibiting a bacterial enzyme.Science. 2010 Nov 5;330(6005):831-5. |
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