PTP1B inhibitor Ertiprotafib is also a potent inhibitor of IκB kinase β (IKK-β)

Ertiprotafib was developed as an inhibitor of PTP1B for the treatment of type 2 diabetes. It normalized the plasma glucose and insulin levels in diabetic animal models, and progressed to a phase II clinical trial. Multiple in vivo targets of Ertiprotafib, in addition to PTP1B inhibition, have been suggested. In this study, Ertiprotafib was also shown to be a potent inhibitor of IκB kinase β (IKK-β), with an IC50 of 400 nM.