CPI1 is a multidrug resistance protein 1 ( MRP1 ) inhibitor with a K i value of 100 nM. CPI1 binds to the same substrate-binding site as leukotriene C 4 , stabilizes MRP1 in an apo-like inward-facing conformation, blocks the conformational changes required for ATP hydrolysis and substrate transport, and inhibits the ATPase activity of human and bovine MRP1 . CPI1 serves as a tool for investigating the substrate transport mechanism of MRP1 . CPI1 is applicable to research related to cancer multidrug resistance.
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