Drug intelligence / Profile preview

ML349

Development stage
Unknown
Lead developer
Sun Yat-sen University
Modality
Small Molecules
Administration
In Vitro Research Use
01

Overview

ML349 is a potent, selective small molecule inhibitor of acyl protein thioesterase 2 (APT2, also known as lysophospholipase 2 or LYPLA2). ML349 reversibly and competitively inhibits APT2 with a Ki of 120 nM and an IC50 of approximately 144 nM, displaying more than 20-fold selectivity over the related enzyme APT1. ML349 is primarily used as a biochemical tool in research settings to dissect the biological roles of APT2/LYPLA2 and protein depalmitoylation. Studies indicate that ML349 does not significantly impact downstream NRAS signaling or cell viability in tested melanoma models, underscoring its selectivity and intended use as a research probe.

02

Targets

LYPLA2 (Acyl-protein thioesterase 2 (APT2))PDXK (Pyridoxal kinase)RAB1A (Ras-related protein Rab-1A)NQO2 (Ribosyldihydronicotinamide dehydrogenase [quinone])

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