LTV-1 is a highly potent, cell-permeable and reversible LYP (lymphoid tyrosine phosphatase, PTPN22) inhibitor with IC50 of 508 nM.
LTV-1 shows 3-fold selectivity over TCPTP (IC50=1.52 uM) and PTP1B (IC50=1.59 uM), 46-fold over SHP1 (IC50=23.2 uM), and 59-fold over CD45 (IC50=30.1 uM), > 200-fold over PTP-PEST (IC50 >100 uM).
LTV-1 increases the phosphorylation levels of the direct physiological targets of LYP, augments calcium mobilization, activates the proximal IL-2 promoter, and enhances the expression of the early activation marker CD25 in T cells.
