TCS 401 is a selective inhibitor of protein-tyrosine phosphatase 1B (PTP1B; Ki = 0.29 μM)

PTP1B: 0.29 µM(Ki)

TCS 401促进了RPE细胞中cyclin A和cyclin D1的增殖和表达。TCS 401诱导RPE细胞向更好的收缩性和移动性分化。迁移实验证明，抑制PTP1B可提高RPE细胞的迁移活性。TCS 401激活了细胞外信号调节激酶(Erk)和蛋白激酶B(Akt)的磷酸化。用PD98059和LY294002预处理可以消除TCS 401诱导的Erk、Akt激活、细胞增殖和细胞迁移[1]。

From the cultured RPE cells treated with TCS 401, cell proliferation was assessed using a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetracolium bromide assay, and the protein expression levels of cyclin A and cyclin D1 were determined. The effect of TCS 401 on cell differentiation was confirmed by immunostaining for α-smooth muscle actin and by western blot. Cell migration activity and PTP1B signaling mechanism were determined. Migration Assay was used to evaluate cell migration activity. PTP1B signaling mechanism was determined by use of PD98059 and LY294002[1].