ZAP 180013

ZAP-180013 is a zeta-chain-associated protein kinase 70 (ZAP-70) inhibitor with an IC50 of 1.8 μM. ZAP-180013 inhibits the interaction of ZAP-70 SH2 domain with immunoreceptor tyrosine-based activation motif (ITAMs)[1].

Research Areas >> Inflammation/Immunology

Signaling Pathways >> Metabolic Enzyme/Protease >> Tyrosinase

IC50: 1.8 μM (ZAP-70)[1]

ZAP-70 is a critical molecule in the transduction of T cell antigen receptor signaling and the activation of T cells. Upon activation of the T cell antigen receptor, ZAP-70 is recruited to the intracellular ζ-chains of the T cell receptor, where ZAP-70 is activated and colocalized with its substrates. Inhibitors of ZAP-70 could potentially function as treatments for autoimmune diseases or organ transplantation. ZAP-180013 disrupts the interaction between ZAP-70 and the T cell antigen receptor. The IC50s in both FP and TR-FRET assays for ZAP-180013 are 9.6 μM and 16.841 μM, respectively[1].

[1]. Patrick R Visperas, et al. Identification of Inhibitors of the Association of ZAP-70 With the T Cell Receptor by High-Throughput Screen. SLAS Discov. 2017 Mar;22(3):324-331.