PTP1B-IN-2

PTP1B-IN-2 (CAS No.: 1919853-46-5) is a potent and selective small-molecule inhibitor of protein tyrosine phosphatase 1B (PTP1B), a key negative regulator of insulin signaling and metabolic homeostasis, widely studied as a therapeutic target in metabolic disorders such as type 2 diabetes and obesity. This compound exhibits high inhibitory activity in the nanomolar range and demonstrates marked selectivity over related phosphatases, including TCPTP, SHP-1, SHP-2, and LAR, supporting its utility for dissecting PTP1B-specific signaling pathways. Mechanistically, PTP1B-IN-2 binds deeply within the catalytic pocket of PTP1B, engaging critical active-site residues through hydrogen bonding and hydrophobic interactions, thereby suppressing enzymatic activity. In cellular systems, it enhances insulin receptor β phosphorylation and promotes insulin-stimulated glucose uptake, indicating effective potentiation of insulin signaling cascades. These properties make PTP1B-IN-2 a valuable chemical probe for studying insulin resistance, metabolic regulation, and phosphatase biology, as well as a candidate scaffold for drug discovery efforts targeting metabolic diseases. Experimental applications typically involve micromolar concentrations in cell-based assays, with specific dosing regimens adjusted according to assay design and biological context.