LKY-047 (LKY047) is a potent, highly selective and reversible competitive cytochrome P450 CYP2J2 (CYP2J2) inhibitor with IC50 of 1.7 uM.
LKY-047 is a strong competitive inhibitor of CYP2J2-mediated astemizole O-demethylase and terfenadine hydroxylase activity, with Ki values of 0.96 and 2.61 μM, respectively.
LKY-047 also acts as an uncompetitive inhibitor of CYP2J2-mediated ebastine hydroxylation with a Ki value of 3.61 μM.
LKY-047 displays no inhibitory effect on other human P450s, such as CYPs 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, and 3A (IC50 > 50 uM).
LKY-047 is useful as a selective CYP2J2 inhibitor in P450 reaction phenotyping studies and the biologic function study of this enzyme.
