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:110 nM (Ki), LYP:0.259 μM (IC50)

LYP-IN-1 demonstrates inhibitory effects on a spectrum of mammalian protein tyrosine phosphatases (PTPs), including SHP1, SHP2, PTP-Meg2, FAP1, and PTP-PEST, exhibiting IC50 values of 5 μM, 2.5 μM, 0.59 μM, 0.39 μM, and 0.8 μM, respectively[1]. At a concentration of 15 μM, LYP-IN-1 enhances both basal and TCR-induced phosphorylation of ZAP-70 on Tyr319 in JTAg cells, as well as significantly promoting the activation of mouse double-positive (DP) thymocytes, evidenced by increased surface expression of CD69 and Nur77, markers indicative of T cell activation[1].