899713-86-1

ML348 is a reversible LYPLA1 inhibitor. It is 14-fold selective for LYPLA1 over LYPLA2 and demonstrates little activity against a panel of more than 20 other serine hydrolases.

ML348 is a substrate-competitive, reversible and APT1-selective acyl-protein thioesterase (APT) inhibitor (IC50/Ki = 840 nM/300 nM against APT1; IC50 & Ki >10 μM against APT2). ML348 effectively inhibits cellular APT1 activity in cultures (by >95% in HEK293T & mouse T cells; 5 μM for 4 h) and in mice in vivo (by >90% in lung/heart/kidney and by ~50% in brain tissue 4 h post 50 mg/kg i.p. dosing) without affecting more than 15 cellular serine hydrolases and APT2.

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