474917-81-2Relevant academic research and scientific papers
Identification of a monoacid-based, cell permeable, selective inhibitor of protein tyrosine phosphatase 1B
Xin, Zhili,Liu, Gang,Abad-Zapatero, Cele,Pei, Zhonghua,Szczepankiewicz, Bruce G.,Li, Xiaofeng,Zhang, Tianyuan,Hutchins, Charles W.,Hajduk, Philip J.,Ballaron, Stephen J.,Stashko, Michael A.,Lubben, Thomas H.,Trevillyan, James M.,Jirousek, Michael R.
, p. 3947 - 3950 (2007/10/03)
Monoacid-based PTP1B inhibitors with improved physiochemical properties have been investigated. A (2-hydroxy-phenoxy) acetic acid-based phosphotyrosyl mimetic has been linked with an optimized second arylphosphate binding site ligand to produce compound 20 with low micromolar potency against PTP1B, good selectivity over TCPTP (20-fold) and high cell permeability in the Caco-2 system.
