MBL-II-141 is potent ABCG2 inhibitor with an IC 50 of 0.11 μM. MBL-II-141 inhibits the transport function of ABCG2 in a non-competitive manner, preventing ABCG2 from pumping substrates (such as Irinotecan ( HY-16562 )) out of the cells, thereby increasing the accumulation of drugs within the cells. MBL-II-141 has no effect on ABCB1 (P-gp) and ABCC1 (MRP1) and has extremely low cytotoxicity ( IG 50 > 100 μM). MBL-II-141 can be used for the study of multidrug resistance (MDR) cancers.
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