Competitive PTP1B inhibitor (IC50 = 0.781 μM). Binds catalytic P-loop of enzyme. Improves insulin sensitivity in obese mice in the glucose tolerance test and the homeostasis model assessment of insulin resistance index (HOMA-IR). Enhances insulin-induced glucose uptake in adipocytes and myotubes in vitro. Exhibits some selectivity for PTP1B over other protein tyrosine phosphatases, except TCPTP.
Zhang et al (2016) A novel protein tyrosine phosphatase 1B inhibitor with therapeutic potential for Ins resistance. Br.J.Pharmacol. 173 1939 PMID:26990621