PTP1B inhibitor Ertiprotafib is also a potent inhibitor of IkappaB kinase beta (IKK-beta).
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.
Shrestha
Suja
S
Department of Chemistry and Institute of Molecular Cell Biology, Inha University, 253 Yonghyun-dong, Nam-ku, Incheon 402-751, Republic of Korea.
Bhattarai
Bharat Raj
BR
Cho
Heeyeong
H
Choi
Joong-Kwon
JK
Cho
Hyeongjin
H
D000818:Animals; D003924:Diabetes Mellitus, Type 2 / Q000188:drug therapy; D004195:Disease Models, Animal; D004305:Dose-Response Relationship, Drug; D006801:Humans; D051550:I-kappa B Kinase / Q000037:antagonists & inhibitors*; D010666:Phenylpropionates / Q000494:pharmacology* / Q000627:therapeutic use; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1; D017027:Protein Tyrosine Phosphatases / Q000037:antagonists & inhibitors*; D013876:Thiophenes / Q000494:pharmacology* / Q000627:therapeutic use
D010666:Phenylpropionates; D013876:Thiophenes; C498182:ertiprotafib; D051550:I-kappa B Kinase; C516607:PTPN1 protein, human; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1; D017027:Protein Tyrosine Phosphatases