LYP-IN-1

LYP-IN-1 is a potent, selective and specific LYP inhibitor with a Ki 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].

Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphatase

Research Areas >> Inflammation/Immunology

IC50: 0.259 μM (LYP) Ki: 110 nM (LYP)[1]

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].

[1]. A Potent and Selective Small-Molecule Inhibitor for the Lymphoid-Specific Tyrosine Phosphatase (LYP), a Target Associated With Autoimmune Diseases