347423
β-Glucuronidase Inhibitor
The β-Glucuronidase Inhibitor controls the biological activity of β-Glucuronidase.
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Synonym(s):
β-Glucuronidase Inhibitor, 1-((6,8-Dimethyl-2-oxo-1,2-dihydroquinolin-3-yl)methyl)-3-(4-ethoxyphenyl)-1-(2-hydroxyethyl)thiourea
Empirical Formula (Hill Notation):
C23H27N3O3S
CAS Number:
Molecular Weight:
425.54
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.28
Recommended Products
Quality Level
Assay
≥99% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
white
solubility
DMSO: 50 mg/mL
shipped in
ambient
storage temp.
2-8°C
SMILES string
O=C(N1)C(CN(C(NC2=CC=C(C=C2)OCC)=S)CCO)=CC3=C1C(C)=CC(C)=C3
General description
An orally bioavailable trisubstituted thiourea compound that acts as a potent, uncompetitive and reversible inhibitor of bacterial β-glucuronidase activity (IC50 = 283 nM; kcat/Km = 0.0987 s-1µM-1; Ki = 164 nM in vitro assays against E coli β-glucuronidase; EC50 = 17.7 nM in β-glucuronidase expressing HB101 cells) with excellent selectivity over mammalian β-glucuronidases. Shown to directly target the 17-residue (360-376) loop structure that protects the active site of E coli β-glucuronidase and alter its conformation. Displays negligible cytotoxicity toward both bacterial and mammalian epithelial cells (>>100 µM for HCT116, Caco-2 and CMT93 colon cancer cells) and offers protection against CPT-11 (50 mg/kg, i.p., s.i.d. for 9 days)-induced toxicity in mice (10 µg, p.o., b.i.d).
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Wallace, B.D., et al. 2010. Science330, 831.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
WGK
WGK 2
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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