LYP-IN-1 is a powerful LYP inhibitor that demonstrates high potency, selectivity, and specificity, with a Ki of 110 nM and an IC 50 of 0.259 μM. Beyond its primary target, LYP-IN-1 also exhibits selectivity towards a wide range of PTPs, including SHP1 (IC 50 = 5 μM) and SHP2 (IC 50 = 2.5 μM). Additionally, LYP-IN-1 demonstrates remarkable efficacy in T- and mast cells, making it a valuable tool for investigating autoimmune disorders.

LYP:0.259 μM (IC50), LYP:110 nM (Ki)

LYP-IN-1 has inhibitory activity toward a panel of mammalian PTPs including SHP1, SHP2, PTP-Meg2, FAP1 and PTP-PEST, with IC 50 values of 5 μM, 2.5 μM, 0.59 μM, 0.39 μM, and 0.8 μM, respectively[1].

LYP-IN-1 (15 μM) increases both basal and TCR-stimulated phosphorylation of ZAP-70 on Tyr319 in JTAg cells[1].LYP-IN-1 (15 μM) treatment of mouse thymocytes effectively causes an increase in the activation of double-positive (DP) thymocytes, it increased surface expression of CD69 (a marker of T cell activation) and Nur77[1].