BCRP Inhbitor

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.

Packaged under inert gas

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Pick, A. et al. 2010. Chem. Med. Chem.5, 1498.
Klinkhammer, W., et al. 2009. Bioorg. Med. Chem.17, 2524.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Toxicity: Standard Handling (A)