PTP1B-IN-2

1919853-46-5

C34H36N2O9S2

DMSO : >= 100 mg/mL (146.89 mM)

Metabolic Enzyme/Protease

PTP1B-IN-2 is a potent protein tyrosine phosphatase 1B (PTP1B) inhibitor with an IC₅₀ of 50 nM. IC50 & Target: IC50: 50 nM (PTP1B)^[1] In Vitro: PTP1B-IN-2 displays more than 40-fold selectivity for PTP1B over SHP-2 and LAR and 15-fold higher selectivity for PTP1B over the highly homologous TCPTP. PTP1B-IN-2 extends deep into the active site pocket, forming several hydrogen bonds and hydrophobic interactions with key residues of the catalytic site. The binding characteristics between PTP1B domain and ligand shows that PTP1B-IN-2 is an ABC type inhibitor which not only interacted with catalytic site but also B site and C site. PTP1B-IN-2 greatly enhances insulin-mediated IRbeta phosphorylation at concentrations of 15 uM and 30 uM. Insulin-stimulated glucose uptake is also significantly increased in L6 myotubes treated with PTP1B-IN-2, and this increase is 16.0%, 19.0% and 38.1% at 5, 10 and 20 uM, respectively ^[1].