Figure 1.
DI-03 is a potent and selective PTP1B/TC-PTP dual competitive inhibitor. (A) Effect of DI-03 on PTP1B catalyzed pNPP hydrolysis. (B) Effect of DI-03 on TC-PTP catalyzed pNPP hydrolysis. The Lineweaver-Burk plot displayed the characteristic intersecting line pattern, consistent with competitive inhibition. DI-03 concentrations were 0 (●), 5 (■), and 10 nM (▲), respectively. DI-03 inhibit PTP1B and TC-PTP with values of 2.4 ± 0.1 and 3.6 ± 0.2 nM, respectively. (C) Selectivity of DI-03 over a panel of 12 mammalian PTPs.