LKY-047, a derivative of Decursin, is a highly effective and specific reversible competitive inhibitor of cytochrome P45022J2 (CYP2J2), with an IC 50 value of 1.7 μM. LKY-047 does not display inhibitory activity against other human P450 enzymes including CYPs 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, and 3A.

CYP2J2:1.7 μM (IC50)

LKY-047 is a potent inhibitor of CYP2J2, specifically targeting astemizole O-demethylase and terfenadine hydroxylase activities, with inhibition constants (K_i values) of 0.96 μM and 2.61 μM, respectively. It also serves as an uncompetitive inhibitor against CYP2J2-mediated ebastine hydroxylation, with a K_i of 3.61 μM[1]. At a concentration of 20 μM, significantly higher than its K_i values, LKY-047 inhibits CYP2J2 activity by 85.3%, demonstrating substantial selectivity by only minimally affecting the activities of other tested P450 enzymes. It exhibits a moderate inhibitory effect on CYP2D6, with 37.2% activity reduction at the same concentration[1].