PTP1B inhibitor Ertiprotafib is also a potent inhibitor of IkappaB kinase beta (IKK-beta)

  • Bioorg Med Chem Lett. 2007 May 15;17(10):2728-30. doi: 10.1016/j.bmcl.2007.03.001.
Suja Shrestha  1 ,  Bharat Raj Bhattarai ,  Heeyeong Cho ,  Joong-Kwon Choi ,  Hyeongjin Cho
Affiliations
  • 1. Department of Chemistry and Institute of Molecular Cell Biology, Inha University, 253 Yonghyun-dong, Nam-ku, Incheon 402-751, Republic of Korea.
PMID: 17407812 DOI: 10.1016/j.bmcl.2007.03.001
Abstract

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 IkappaB kinase beta (IKK-beta), with an IC(50) of 400nM.

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