LYP-IN-1

LYP-IN-1 is a potent, selective and specific LYP inhibitor with a K_i and an IC₅₀ of 110 nM and 0.259 μM, respectively. LYP-IN-1 also has selectivity for a large panel of PTPs, such as SHP1 (IC₅₀=5 μM) and SHP2 (IC₅₀=2.5 μM). LYP-IN-1 exhibits highly efficacious cellular activity in T- and mast cells. LYP-IN-1 can be used for the study of autoimmune disorders^[1]. LYP-IN-1 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. IC50 & Target:IC50: 0.259 μM (LYP)
Ki: 110 nM (LYP)^[1] In Vitro: LYP-IN-1 has inhibitory activity toward a panel of mammalian PTPs including SHP1, SHP2, PTP-Meg2, FAP1 and PTP-PEST, with IC₅₀ 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].