nsc-87877

Description: NSC-87877 is a novel, potent, cell-permeable small molecule and competitive inhibitor of SHP-1 and SHP-2 PTP (protein tyrosine phosphatase) with IC50 of 55 and 318 nM, respectively. Protein phosphorylation plays critical roles in many regulatory mechanisms controlling cell activities and thus involved in various diseases. The cellular equilibrium of phosphorylation is regulated through the actions of protein kinases and phosphatases. Therefore, these regulatory proteins have emerged as promising targets for drug development. Phosphatase activity of dual-specificity protein phosphatase 26 (DUSP26) was decreased by NSC-87877 in a dose-dependent manner. Kinetic studies suggest that NSC-87877 is a potent competitive inhibitor of DUSP26. NSC-87877 effectively inhibited DUSP26-mediated dephosphorylation of p38, a member of mitogen-activated protein kinase (MAPK) family. Since DUSP26 is involved in survival of anaplastic thyroid cancer (ATC) cells, NSC-87877 could be a therapeutic reagent for treating DUSP26-related diseases such as ATC and neuroblastoma (NB), since Dual specificity protein phosphatase 26 (DUSP26) is overexpressed in high-risk neuroblastoma and contributes to chemoresistance by inhibiting p53 function.

References: Biochem Biophys Res Commun. 2009 Apr 17; 381(4):491-5; Cell Death Dis. 2015 Aug 6; 6:e1841.