ZAP-180013

• CAT Number: I015242
• CAS Number: 873080-25-2
• Molecular Formula: C19H17Cl2N3O4S
• Molecular Weight: 454.33
• Purity: ≥95%
• Synonyms: 5-chloro-N-[(4-chlorophenyl)methyl]-2-ethylsulfonyl-N-(furan-2-ylmethyl)pyrimidine-4-carboxamide
• InChI: InChI=1S/C19H17Cl2N3O4S/c1-2-29(26,27)19-22-10-16(21)17(23-19)18(25)24(12-15-4-3-9-28-15)11-13-5-7-14(20)8-6-13/h3-10H,2,11-12H2,1H3
• InChIKey: GTWKIPDKVRLUKN-UHFFFAOYSA-N
• SMILES: CCS(=O)(=O)C1=NC=C(C(=N1)C(=O)N(CC2=CC=C(C=C2)Cl)CC3=CC=CO3)Cl

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].
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].

Reference

[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.
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