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Description: TCS-401 HCI is a novel, potent and selective inhibitor of protein-tyrosine phosphatase 1B (PTP1B) with Ki of 0.29 uM. PTP1B was expressed in the RPE layer of the normal retina. After retinal detachment, weak immunolabeling of PTP1B was seen in the RPE cells. TCS-401 promoted the proliferation and expression of cyclin A and cyclin D1 in RPE cells. TCS-401 induced RPE cells to differentiate toward better contractility and motility. A migration assay proved that inhibiting PTP1B improved the migratory activity of RPE cells. TCS-401 activated extracellular signal-regulated kinase (Erk) and protein kinase B (Akt) phosphorylation. Pretreatment with PD98059 and LY294002 abolished TCS-401-induced activation of Erk, Akt, cell proliferation, and cell migration.
References: Mol Vis. 2015 May 1; 21:523-31. eCollection 2015; Am J Physiol Renal Physiol. 2013 Mar 15; 304(6):F698-709.
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