BCRP Inhbitor

Toxicity: Standard Handling (A)

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.

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

Packaged under inert gas

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

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