General description
A non-tetrahydroisoquinoline BCRP specific inhibitor based on the anthranilic acid scaffold, that displays an IC50 of 1.39 µM in a Hoechst 33343 assay in stably transfected MDCK BCRP cells, which is ˜50-fold more potent than novobiocin (IC50 = 65 µM), and shows no effect towards other ATP binding cassette (ABC) transporters P-gp and MRP1 at up to a concentration of 10 µM. It is shown to be an allosteric inhibitor in enzyme kinetics assays in the presence of BCRP specific substrates pheophorbide A and imitanib, and does not lead to a decrease in cell viability up to a concentration of 10 µM.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Other Notes
Pick, A. et al. 2010. Chem. Med. Chem.5, 1498.Klinkhammer, W., et al. 2009. Bioorg. Med. Chem.17, 2524.
Packaging
Packaged under inert gas
10 mg in Glass bottle
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Warning
Toxicity: Standard Handling (A)
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